A new water-soluble heteropolysaccharide with a molecular weight of 15 k Da was isolated from the fruiting bodies of Boletus reticulatus Schaeff.Structural characterization results revealed that B.reticulatus Schaeff ...A new water-soluble heteropolysaccharide with a molecular weight of 15 k Da was isolated from the fruiting bodies of Boletus reticulatus Schaeff.Structural characterization results revealed that B.reticulatus Schaeff polysaccharide(BRS-X)had a backbone of 1,6-linkedα-D-galactose and 1,2,6-linkedα-D-galactose which branches were mainly composed of a terminal 4-linkedβ-D-glucose and the ratio of D-galactose and D-glucose was 5:1.Bioactivity assays indicated that BRS-X displayed a strong proliferative activity in T cells and B cells and promoted the secretion of immunoglobulin G(Ig G),Ig E,Ig D and Ig M.In addition,BRS-X could facilitate the proliferation and phagocytosis of RAW264.7 cells and could significantly inhibit the growth of tumors in S180-bearing mice.The results of transcriptome sequencing analysis illustrated that total 46 genes enriched in MAPK and total 34 genes enriched in PI3 K/Akt signaling pathways in BRS-X group.The protein VEGF and VEGFR expression were significantly reduced under the treatment with BRS-X.These findings provide a scientific basis for the edible and medicinal value of BRS-X.展开更多
A novel lectin(termed PML)was purified from fruiting bodies of the edible mushroom Phellodon melaleucus(division Basidiomycota)by ion exchange,hydrophobic interaction,and gel filtration chromatographies,with overall t...A novel lectin(termed PML)was purified from fruiting bodies of the edible mushroom Phellodon melaleucus(division Basidiomycota)by ion exchange,hydrophobic interaction,and gel filtration chromatographies,with overall titer recovery~60%and 20-fold purification.PML displayed hemagglutination activity 13319 units/mg toward rabbit erythrocytes.SDS-PAGE and gel filtration analyses revealed that PML is a homodimeric lectin with a molecular weight of 28.8 kDa.PML hemagglutination activity was not inhibited by various simple sugars or their derivatives,but was enhanced by cations Ca^(2+),Mg^(2+),Zn^(2+),and Cu^(2+).The activity was stable in pH range 6–9 and in the temperature range 20–60°C.Circular dichroism(CD)spectroscopic analysis showed that PML was composed primarily ofβ-sheets with lowα-helix content.In a B16 melanoma mouse model,PML treatment significantly inhibited tumor growth,and increased cytokine IL-10 content.Our findings suggest that PML is a potential anticancer therapeutic agent.展开更多
Objective:The main chemical components of galangal(Alpinia officinarum Hance)are flavonoids and diarylheptanes.In the previous work,the total heptane and total flavonoid components of galangal were isolated.In this pa...Objective:The main chemical components of galangal(Alpinia officinarum Hance)are flavonoids and diarylheptanes.In the previous work,the total heptane and total flavonoid components of galangal were isolated.In this paper,the two components were separated.The monomeric compound was purified and its cytotoxic activity was determined.Methods:Silica gel column chromatography,ODS column chromatography,preparative thin layer chromatography,preparative and semi-preparative HPLC methods were used to separate and purify the total heptane components and total flavonoid components of galangal.Structures of compounds were identified by 1H-NMR,13C-NMR modern spectroscopic techniques combined with literature.The cytotoxic activity of the isolated compounds against MDA-MB-231(breast cancer),HepG-2(liver cancer)and MKN-45(gastric cancer)cells was tested by CCK-8 method.Results:Six compounds were isolated from the total heptane fractions of galangal,and three compounds were isolated from the total flavonoids of galangal.Their structures were identified as:5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenylheptan-3-one(1),(E)-7-(4-hydr-oxy-3-methoxyphenyl)-1-phenylhept-4-en-3-one(2),5-hydroxy-1,7-diphenylheptan-3-one(3)7-(4-hydroxyphenyl)-5-methoxy-1-phenylheptan-3-one(4),(E)-7-(4-hydroxyphenyl)-1-phenylhept-4-en-3-one(5),(E)-1,7-diphenylhept-4-en-3-one(6),pinocembrin(7),galangin(8),3-O-methylgalangin(9).Conclusion:Compounds 1-6 were isolated from the total heptane components of galangal,and compounds 7-9 were isolated from the total flavonoids of galangal.The results of CCK-8 showed that compounds 2,3,5,6,7 and 8 had weak antitumor activity.展开更多
[Objectives]To compare the effects of molecular distillation on the flavor and antitumor activity of Ganoderma lucidum spore oil.[Methods]G.lucidum spore oil was separated and purified by molecular distillation techno...[Objectives]To compare the effects of molecular distillation on the flavor and antitumor activity of Ganoderma lucidum spore oil.[Methods]G.lucidum spore oil was separated and purified by molecular distillation technology,and the volatile components of different components of molecular distillation were analyzed by gas chromatography-ion mobility spectrometry(GC-IMS)technology.Human liver carcinoma cells(HepG2),human breast cancer cells(MCF-7),and human cervical cancer cells(Hela)were selected as the tumor cell lines to be tested,and the cell viability was detected by the MTT assay.[Results]Molecular distillation effectively reduced small molecular substances produced by oil oxidation in G.lucidum spore oil,such as heptanal,octanal,linalool,hexanal,E-2-octanal,3-ethylpyridine,etc.Among the heavy components,the content of esters was relatively high,mainly including ethyl levulinate,ethyl crotonate,and amyl butyrate.The MTT cytotoxicity test indicated that G.lucidum spore oil and its molecular distillation components had certain inhibitory effects on the growth of three tumor cells,and G.lucidum spore oil crude oil had the most significant antitumor activity.G.lucidum spore oil crude oil,heavy component,and light component had the most significant antitumor activity on HepG2 cells,followed by MCF-7 cells,and the weakest antitumor activity on Hela cells.The quality of G.lucidum spore oil became higher after molecular distillation,and the rancid smell was reduced,and molecular distillation had little effect on the antitumor activity of G.lucidum spores.[Conclusions]Molecular distillation technology can be applied to the refining of G.lucidum spore oil to improve product quality.展开更多
A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characteriz...A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.展开更多
A novel Zn(Ⅱ) complex, [ZnL_2(H_2O)_4]·H_2O(1, HL = 2-(nicotinoyloxy)acetic acid), was synthesized using Zn(OAc)_2·2H_2O and 2-(nicotinoyloxy)acetic acid as raw materials. Its structure has been elucidated ...A novel Zn(Ⅱ) complex, [ZnL_2(H_2O)_4]·H_2O(1, HL = 2-(nicotinoyloxy)acetic acid), was synthesized using Zn(OAc)_2·2H_2O and 2-(nicotinoyloxy)acetic acid as raw materials. Its structure has been elucidated by elemental analysis, IR and single-crystal X-ray diffraction. The structural analysis revealed that complex 1 crystallizes in triclinic, space group P1 and the Zn(Ⅱ) atom is six-coordinated with two N atoms from two different 2-(nicotinoyloxy)acetate anion ligands and four O atoms from coordinated water molecules. Complex 1 forms a 3D network structure by O–H···O hydrogen bonds. The antitumor activities of 2-(nicotinoyloxy)acetic acid ligand and its Zn(Ⅱ) complex were evaluated against human lung adenocarcinoma A549 cells, human hepatoma SMMC-7721 cells and human colon carcinoma Wi Dr cells.展开更多
Despite therapeutic advances in recent decades, colorectal cancer is still the third most frequent neoplasm worldwide, with significant morbidity and mortality in young and middle-aged adults. Therefore, advance in tr...Despite therapeutic advances in recent decades, colorectal cancer is still the third most frequent neoplasm worldwide, with significant morbidity and mortality in young and middle-aged adults. Therefore, advance in treatment options for patients who are afflicted with tumor subtypes without effective therapies is needed. Antarctica macroalgae are substances-producing organisms with important biological activities, in which antitumor properties are investigated, showing promising cytotoxic results. There are no reports so far showing antitumor activity of macroalgae Palmaria decipiens extracts against colorectal tumors. This study aims to evaluate the effect of macroalgae P. decipiens extract from Antarctic on tumor cell HCT-116 and non-tumor cell HaCaT lines. The phenolic compounds present were identified by high performance liquid chromatography. The antioxidant activity of the extracts was determined by the DPPH radical inhibition method and cytotoxicity was evaluated through MTT assay. Cell death events were identified using dual staining with acridine orange/ethidium bromide and flow cytometry. The quantification of phenolic compounds present in the extracts identified the presence of three main compounds among them is kaempferol. The metanolic extract showed inhibition within 72 h of treatment in HCT-116 and potential antioxidant activity. The results presented in this study point out an imbalance in the redox metabolism and also a loss of mitochondrial membrane potential integrity, most likely inducing cell death mechanisms after 72 h exposure to treatment with metanolic extract. These events could be observed by penetration of propidium iodide through membrane damage. The results indicate that the extract of the Antarctic macroalgae P. decipiens interferes in the mechanisms of action of colorectal cancer tumor cells, acting as a potential antitumor and antioxidant agent.展开更多
Topical 5-fluorouracil(5-FU)is approved for the treatment of superficial basal cell carcinoma and actinic keratosis.However,5-FU suffers from poor skin permeation.Microneedles have been successfully applied to improve...Topical 5-fluorouracil(5-FU)is approved for the treatment of superficial basal cell carcinoma and actinic keratosis.However,5-FU suffers from poor skin permeation.Microneedles have been successfully applied to improve the skin permeability of small and large molecules,and even nanoparticles,by creating micron-sized pores in the stratum corneum layer of the skin.In this report,the feasibility of using microneedles to increase the skin permeability of 5-FU was tested.Using full thickness mouse skin mounted on Franz diffusion apparatus,it was shown that the flux of 5-FU through the skin was increased by up to 4.5-fold when the skin was pretreated with microneedles(500μm in length,50μm in base diameter).In a mouse model with B16-F10 mouse melanoma cells implanted in the subcutaneous space,the antitumor activity of a commercially available 5-FU topical cream(5%)was significantly enhanced when the cream was applied on a skin area that was pretreated with microneedles,as compared to when the cream was simply applied on a skin area,underneath which the tumor cells were implanted,and without pretreatment of the skin with microneedles.Fluorouracil is not approved for melanoma therapy,but the clinical efficacy of topical 5-FU against tumors such as basal cell carcinoma may be improved by integrating microneedle technology into the therapy.展开更多
A great challenge in multi-targetingdrug discovery is to identify drug-like lead compounds with therapeutic advantages over single target inhibitors and drug combinations.Inspired by our previous efforts in designing ...A great challenge in multi-targetingdrug discovery is to identify drug-like lead compounds with therapeutic advantages over single target inhibitors and drug combinations.Inspired by our previous efforts in designing antitumor evodiamine derivatives,herein selective histone deacetylase 1(HDAC1)and topoisomerase 2(TOP2)dual inhibitors were successfully identified,which showed potent in vitro and in vivo antitumor potency.Particularly,compound 30 a was orally active and possessed excellent in vivo antitumor activity in the HCT116 xenograft model(TGI=75.2%,150 mg/kg,p.o.)without significant toxicity,which was more potent than HDAC inhibitor vorinostat,TOP inhibitor evodiamine and their combination.Taken together,this study highlights the therapeutic advantages of evodiamine-based HDAC1/TOP2 dual inhibitors and provides valuable leads for the development of novel multi-targeting antitumor agents.展开更多
Objective To study the antitumor activity of extract from Salvia plebeia and investigate whether the extract induce apoptosis of K562 cells.Methods The aqueous,petroleum ether,dichloromethane(CH2Cl2),ethyl acetate,and...Objective To study the antitumor activity of extract from Salvia plebeia and investigate whether the extract induce apoptosis of K562 cells.Methods The aqueous,petroleum ether,dichloromethane(CH2Cl2),ethyl acetate,and butanol extracts were prepared from the aerial parts of S.plebeia.Taking fluorouracil as reference,the cytotoxic activities of these extracts on HeLa,A549,SGC-7901,HCT-116,K562,LoVo,DU-145,and HepG2 cells were evaluated.To clarify the apoptosis of K562 cells induced by CH2Cl2 extract,the methods of Hoechst 33258 staining,flow cytometry assay,and DNA ladder assay were investigated.Results The CH2Cl2 extract showed the most potent cytotoxic effect against K562 cells,with an IC50<15μg/mL for 3 d treatment.The characteristic apoptotic symptoms such as DNA fragmentation and chromatin condensation were also observed in the K562 cells.Conclusion The CH2Cl2 extract from S.plebeia may inhibit the cancer cell proliferation by inducing cell apoptosis.展开更多
HYL derived from the venom of the solitary bee Hylaeus signatus(Hymenoptera:Colletidae)is anα-helical antimicrobial peptide with 16 residues.To explore whether HYL can be applied in anti-tumor therapy,we synthesized ...HYL derived from the venom of the solitary bee Hylaeus signatus(Hymenoptera:Colletidae)is anα-helical antimicrobial peptide with 16 residues.To explore whether HYL can be applied in anti-tumor therapy,we synthesized HYL and further modified its structure by using a solid-phase synthesis method,and then evaluated their antitumor activities.Firstly,we identified the key residues of HYL by alanine scanning strategy,and then a series of stapled peptides were synthesized by hydrocarbon stapling strategy without destroying the key residues.All the stapled peptides of HYL showed significant improvement not only inα-helicity,but also in antitumor activity and protease resistance when compared to the parent peptide HYL.The results showed that hydrophobicity and amphiphilicity are important factors affecting the antitumor activity of HYL,and the stapling strategy can significantly affect the proteolytic stability and helicity of HYL.What’s more,we find that the stapled peptides HYL-14,HYL-16 and HYL-18 show a promising prospect for novel anti-tumor drug development.展开更多
Objective:Nonsmall-cell lung cancer(NSCLC)is an aggressive,highly chemoresistant disease.Taxol is an effective chemotherapeutic drug widely used for the treatment of NSCLC.However,the clinical use of Taxol is limited ...Objective:Nonsmall-cell lung cancer(NSCLC)is an aggressive,highly chemoresistant disease.Taxol is an effective chemotherapeutic drug widely used for the treatment of NSCLC.However,the clinical use of Taxol is limited due to the occurrence of adverse side effects under high therapeutic doses.Therefore,it is desirable to explore combination therapy to reduce the dose of chemotherapeutic drugs and achieve excellent outcomes.A biosynthetic ginsenoside,3-O-β-D-glucopyranosyl-dammar-24-ene-3β,20 S-diol(3β-O-Glc-DM,C3 DM)is obtained from microbial fermentation by metabolic engineering.Based on previous study findings,we aimed to explore the mechanism of combination therapy with C3 DM and Taxol and its increasing antitumor effect on Lewis lung cancer(LLC)in this study.Materials and Methods:A thiazolyl blue tetrazolium bromide(MTT)assay was performed to evaluate cell viability;the apoptotic effect was studied using cell apoptosis assay.The Lewis tumor xenograft experiment was performed to determine the effects of C3 DM combined with Taxol on tumor growth in vivo,and western blotting was performed to analyze protein expressions.Results:C3 DM effectively inhibited the proliferation of NSCLC cells.Moreover,C3 DM increased the antiproliferative activity of Taxol and significantly enhanced cell apoptosis induced by Taxol in Lewis lung cancer cells.C3 DM alone also suppressed Lewis tumor growth and enhanced the antitumor activity of Taxol in vivo.Western blot analysis revealed that the effects of the antiproliferation and apoptosis induction of C3 DM treatment alone or in combination with Taxol on Lewis lung cancer were mediated by inhibiting the interleukin-6(IL-6)/Jak2/STAT3 and IL-6/AKT signaling pathways.Conclusions:The results showed that C3 DM has the potential to be used in combination therapy with Taxol against NSCLC.展开更多
A novel Ca(Ⅱ) coordination polymer,[Ca L_(2)(H_(2)O)_(2)]_(n) (1,HL=4-acetylphenoxyacetic acid) has been synthesized with 4-acetylphenoxyacetic acid,Ca(ClO_4)_(2)·4H_(2)O and Na OH as raw materials.Complex 1 was...A novel Ca(Ⅱ) coordination polymer,[Ca L_(2)(H_(2)O)_(2)]_(n) (1,HL=4-acetylphenoxyacetic acid) has been synthesized with 4-acetylphenoxyacetic acid,Ca(ClO_4)_(2)·4H_(2)O and Na OH as raw materials.Complex 1 was characterized by elemental analysis and single-crystal X-ray diffraction analysis.The results show that the Ca(Ⅱ)ion is eight-coordinated in a distorted triangular dodecahedral geometric configuration with six carboxylate Oatoms of four L ligands and two O atoms of two coordinated water molecules.Complex 1 forms a one-dimensional chained structure by the bridging effect of carboxylate O atoms.The antitumor activity of HLligand and complex 1 has also been investigated.展开更多
In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-h...In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.展开更多
In this study, arsenic trioxide(ATO) was encapsulated in liposomes via copper acetate(Cu(OAc)2) gradients and high entrapment efficiency of over 80% was obtained. The average particle size and the zeta-potential of th...In this study, arsenic trioxide(ATO) was encapsulated in liposomes via copper acetate(Cu(OAc)2) gradients and high entrapment efficiency of over 80% was obtained. The average particle size and the zeta-potential of the liposomes were detected to be 115.1 ± 29.1 nm and-21.97 ± 0.6 m V, respectively. The TEM images showed rod-like precipitates in the inner aqueous phase, which was supposed be due to the formation of insoluble ATO–Cu complex.The in vitro drug release of ATO–Cu liposomes exhibited a sustained release over 72 h, and the release rates decreased with the increase of the p H of release media. Pharmacokinetic and tissue distribution studies of ATO liposomes showed significantly reduced plasma clearance rate, increased AUC0–12h and T1/2, and improved tumor distribution of As compared to iv administration of ATO solution. The anti-tumor effect of ATO loaded liposomes to S180 tumor-bearing mice was significantly improved with a tumor inhibition rate of 61.2%,meanwhile the toxicity of encapsulated ATO was greatly decreased. In conclusion, ATO can be effectively encapsulated into liposomes by remote loading method via Cu(OAc)2 gradients;the co-administration of ATO and Cu(Ⅱ) via liposomal formulation may find wide applications in the treatment of various tumors.展开更多
<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span>&...<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] a route in a simple and reproducible synthesis for a novel compound of coordinating Ru</span><sup><span style="font-family:Verdana;">+3</span></sup><span style="font-family:Verdana;"> with bipy and L-trip. The spectroscopic characterization in the mi</span><span style="font-family:Verdana;">ddle infrared region (FTIR) shows the interactions between Ru-(L-trip), evidenced by the displacement of the carboxylate ion band for</span><span><span style="font-family:Verdana;"> higher energies, and also by the displacements of aliphatic amine bands, suggesting that bidentate coordination of the L-trip ligand occurred. Analysis of the results obtained with thermoanalytical techniques showed that the minimum formula of the compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)]1/2H</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">O. Evaluation of the</span></span><span><span style="font-family:Verdana;"> antitumor potential of precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] showed the toxic effects on MCF-7 cell line, but </span></span><span style="font-family:Verdana;">did not show selectivity and not reached PBMC cells to the same extent. The evaluation of the antitumor potential of the newly synthesized compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)], demonstrated that the insertion of an L-tryptophan molecule into the precursor coordination sphere made it selective when compared to PBMC cells, for MCF-7 type tumor cells.</span>展开更多
Background/Aim: Antarctic seaweeds are considered a promising source of compounds with anticancer activity. Colorectal cancer (CRC) is one of the most incident cancers with high mortality rates worldwide. This work ai...Background/Aim: Antarctic seaweeds are considered a promising source of compounds with anticancer activity. Colorectal cancer (CRC) is one of the most incident cancers with high mortality rates worldwide. This work aimed to characterize chemically extracts of the Antarctic macroalgae Iridaea cordata, Cystosphaera jacquinotii and Desmarestia anceps and to evaluate the cytotoxic effects against human colon cancer HCT 116 cell line. Materials and Methods: The extracts were obtained by depletion using an ultrasound probe and were identified by High-Performance Liquid Chromatography (HPLC) and Gas Chromatography coupled with Mass Spectrometry (GC-MS). Cell viability was determined by MTT assay. Results: Hexanic and chloroform extracts of the I. cordata and the hexanic, chloroform and methanolic extracts of D. anceps were able to inhibit growth of colorectal cancer cells in the three different incubation times (24, 48 and 72 h). Through GC analysis, 01 compounds were identified in the hexane extract and 02 compounds in the chloroform extract of the algae I. cordata. The hexane extract of D. anceps macroalgae presented 5 compounds, chloroform extract 10 and methanolic extract 3 respectively, with special highlight to fucosterol. Carotenoid analysis by HPLC identified β-carotene in all species, while zeaxanthin was present in the spectrum of I. cordata and C. jacquinotii. Fucoxanthin and violaxanthin were confirmed in the brown seaweeds C. jacquinotii and D. anceps. Conclusion: Extracts of macroalgae I. Cordata and D. anceps may be a source of therapeutic agents against CRC.展开更多
The reaction of 5-hydroxyl-7-methoxyflavone(tectochrysin) with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one(1), which was characterized by FT-IR, 1 H-NMR, ^(13)C-NMR, elemental anal...The reaction of 5-hydroxyl-7-methoxyflavone(tectochrysin) with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one(1), which was characterized by FT-IR, 1 H-NMR, ^(13)C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673(8), b = 17.9938(15), c = 21.2004(17) ?, V = 3611.5(5) ?~3, Z = 8, μ = 0.6726 mm^(-1), Dc = 1.795 g/cm3, F(000) = 2080, the final R = 0.0358 and wR = 0.0644 with I > 2σ(I). The results show that the addition reaction occurs at the carbon-carbon double bond(C2 and C3) of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells(K562), human breast cancer cells(MCF-7) and human lung cancer cells(A549). 1 exhibited potent antitumor activities against human leukemia cells(K562) with the IC50 values of 18.9 μmol/L.展开更多
In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. ...In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1 Hbenzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) ?, Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702.展开更多
基金supported by the Open Project Program of Irradiation Preservation Technology Key Laboratory of Sichuan Province,Sichuan Institute of Atomic Energy(FZBC2020009)the Open Research Fund Program of Departmental and Municipal Co-construction of Crops Genetic Improvement of Hill Land Key Laboratory of Sichuan Province(2021CGIHL02)+2 种基金Science and Technology Support Project of Nanchong Science and Technology Bureau of Sichuan Province(20YFZJ0053 and 20YFZJ0054)the Sericulture Innovation Team of Sichuan Province(SCCXTD-2021-17)Laboratory of Sichuan Province(2021CGIHL02)。
文摘A new water-soluble heteropolysaccharide with a molecular weight of 15 k Da was isolated from the fruiting bodies of Boletus reticulatus Schaeff.Structural characterization results revealed that B.reticulatus Schaeff polysaccharide(BRS-X)had a backbone of 1,6-linkedα-D-galactose and 1,2,6-linkedα-D-galactose which branches were mainly composed of a terminal 4-linkedβ-D-glucose and the ratio of D-galactose and D-glucose was 5:1.Bioactivity assays indicated that BRS-X displayed a strong proliferative activity in T cells and B cells and promoted the secretion of immunoglobulin G(Ig G),Ig E,Ig D and Ig M.In addition,BRS-X could facilitate the proliferation and phagocytosis of RAW264.7 cells and could significantly inhibit the growth of tumors in S180-bearing mice.The results of transcriptome sequencing analysis illustrated that total 46 genes enriched in MAPK and total 34 genes enriched in PI3 K/Akt signaling pathways in BRS-X group.The protein VEGF and VEGFR expression were significantly reduced under the treatment with BRS-X.These findings provide a scientific basis for the edible and medicinal value of BRS-X.
基金supported by grants from the China Agriculture Research System(CARS-20-01A)。
文摘A novel lectin(termed PML)was purified from fruiting bodies of the edible mushroom Phellodon melaleucus(division Basidiomycota)by ion exchange,hydrophobic interaction,and gel filtration chromatographies,with overall titer recovery~60%and 20-fold purification.PML displayed hemagglutination activity 13319 units/mg toward rabbit erythrocytes.SDS-PAGE and gel filtration analyses revealed that PML is a homodimeric lectin with a molecular weight of 28.8 kDa.PML hemagglutination activity was not inhibited by various simple sugars or their derivatives,but was enhanced by cations Ca^(2+),Mg^(2+),Zn^(2+),and Cu^(2+).The activity was stable in pH range 6–9 and in the temperature range 20–60°C.Circular dichroism(CD)spectroscopic analysis showed that PML was composed primarily ofβ-sheets with lowα-helix content.In a B16 melanoma mouse model,PML treatment significantly inhibited tumor growth,and increased cytokine IL-10 content.Our findings suggest that PML is a potential anticancer therapeutic agent.
基金Key R&D Projects in Hainan Province(ZDYF2022SHFZ127)National Natural Science Foundation of China(No.81660649)。
文摘Objective:The main chemical components of galangal(Alpinia officinarum Hance)are flavonoids and diarylheptanes.In the previous work,the total heptane and total flavonoid components of galangal were isolated.In this paper,the two components were separated.The monomeric compound was purified and its cytotoxic activity was determined.Methods:Silica gel column chromatography,ODS column chromatography,preparative thin layer chromatography,preparative and semi-preparative HPLC methods were used to separate and purify the total heptane components and total flavonoid components of galangal.Structures of compounds were identified by 1H-NMR,13C-NMR modern spectroscopic techniques combined with literature.The cytotoxic activity of the isolated compounds against MDA-MB-231(breast cancer),HepG-2(liver cancer)and MKN-45(gastric cancer)cells was tested by CCK-8 method.Results:Six compounds were isolated from the total heptane fractions of galangal,and three compounds were isolated from the total flavonoids of galangal.Their structures were identified as:5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenylheptan-3-one(1),(E)-7-(4-hydr-oxy-3-methoxyphenyl)-1-phenylhept-4-en-3-one(2),5-hydroxy-1,7-diphenylheptan-3-one(3)7-(4-hydroxyphenyl)-5-methoxy-1-phenylheptan-3-one(4),(E)-7-(4-hydroxyphenyl)-1-phenylhept-4-en-3-one(5),(E)-1,7-diphenylhept-4-en-3-one(6),pinocembrin(7),galangin(8),3-O-methylgalangin(9).Conclusion:Compounds 1-6 were isolated from the total heptane components of galangal,and compounds 7-9 were isolated from the total flavonoids of galangal.The results of CCK-8 showed that compounds 2,3,5,6,7 and 8 had weak antitumor activity.
基金Supported by Taishan Industrial Leading Talent Project(Efficient Ecological Agriculture Innovation)(LJNY202105)。
文摘[Objectives]To compare the effects of molecular distillation on the flavor and antitumor activity of Ganoderma lucidum spore oil.[Methods]G.lucidum spore oil was separated and purified by molecular distillation technology,and the volatile components of different components of molecular distillation were analyzed by gas chromatography-ion mobility spectrometry(GC-IMS)technology.Human liver carcinoma cells(HepG2),human breast cancer cells(MCF-7),and human cervical cancer cells(Hela)were selected as the tumor cell lines to be tested,and the cell viability was detected by the MTT assay.[Results]Molecular distillation effectively reduced small molecular substances produced by oil oxidation in G.lucidum spore oil,such as heptanal,octanal,linalool,hexanal,E-2-octanal,3-ethylpyridine,etc.Among the heavy components,the content of esters was relatively high,mainly including ethyl levulinate,ethyl crotonate,and amyl butyrate.The MTT cytotoxicity test indicated that G.lucidum spore oil and its molecular distillation components had certain inhibitory effects on the growth of three tumor cells,and G.lucidum spore oil crude oil had the most significant antitumor activity.G.lucidum spore oil crude oil,heavy component,and light component had the most significant antitumor activity on HepG2 cells,followed by MCF-7 cells,and the weakest antitumor activity on Hela cells.The quality of G.lucidum spore oil became higher after molecular distillation,and the rancid smell was reduced,and molecular distillation had little effect on the antitumor activity of G.lucidum spores.[Conclusions]Molecular distillation technology can be applied to the refining of G.lucidum spore oil to improve product quality.
文摘A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.
基金supported by the National Natural Science Foundation of China(No.21171132)the Project of Shandong Province Higher Educational Science and Technology Program(J14LC01)Science Foundation of Weifang
文摘A novel Zn(Ⅱ) complex, [ZnL_2(H_2O)_4]·H_2O(1, HL = 2-(nicotinoyloxy)acetic acid), was synthesized using Zn(OAc)_2·2H_2O and 2-(nicotinoyloxy)acetic acid as raw materials. Its structure has been elucidated by elemental analysis, IR and single-crystal X-ray diffraction. The structural analysis revealed that complex 1 crystallizes in triclinic, space group P1 and the Zn(Ⅱ) atom is six-coordinated with two N atoms from two different 2-(nicotinoyloxy)acetate anion ligands and four O atoms from coordinated water molecules. Complex 1 forms a 3D network structure by O–H···O hydrogen bonds. The antitumor activities of 2-(nicotinoyloxy)acetic acid ligand and its Zn(Ⅱ) complex were evaluated against human lung adenocarcinoma A549 cells, human hepatoma SMMC-7721 cells and human colon carcinoma Wi Dr cells.
文摘Despite therapeutic advances in recent decades, colorectal cancer is still the third most frequent neoplasm worldwide, with significant morbidity and mortality in young and middle-aged adults. Therefore, advance in treatment options for patients who are afflicted with tumor subtypes without effective therapies is needed. Antarctica macroalgae are substances-producing organisms with important biological activities, in which antitumor properties are investigated, showing promising cytotoxic results. There are no reports so far showing antitumor activity of macroalgae Palmaria decipiens extracts against colorectal tumors. This study aims to evaluate the effect of macroalgae P. decipiens extract from Antarctic on tumor cell HCT-116 and non-tumor cell HaCaT lines. The phenolic compounds present were identified by high performance liquid chromatography. The antioxidant activity of the extracts was determined by the DPPH radical inhibition method and cytotoxicity was evaluated through MTT assay. Cell death events were identified using dual staining with acridine orange/ethidium bromide and flow cytometry. The quantification of phenolic compounds present in the extracts identified the presence of three main compounds among them is kaempferol. The metanolic extract showed inhibition within 72 h of treatment in HCT-116 and potential antioxidant activity. The results presented in this study point out an imbalance in the redox metabolism and also a loss of mitochondrial membrane potential integrity, most likely inducing cell death mechanisms after 72 h exposure to treatment with metanolic extract. These events could be observed by penetration of propidium iodide through membrane damage. The results indicate that the extract of the Antarctic macroalgae P. decipiens interferes in the mechanisms of action of colorectal cancer tumor cells, acting as a potential antitumor and antioxidant agent.
基金This work was supported in part by the University of Texas at Austin,College of Pharmacy and a grant from the National Institutes of Health(CA135274)to Z.CuiYoussef Naguib was supported by a doctoral scholarship from the Egyptian Ministry of Higher EducationThe authors acknowledge Cynergy,LLC(Carson City,NV)for generously providing Dermaroller s micro-needle rollers,free of charge.
文摘Topical 5-fluorouracil(5-FU)is approved for the treatment of superficial basal cell carcinoma and actinic keratosis.However,5-FU suffers from poor skin permeation.Microneedles have been successfully applied to improve the skin permeability of small and large molecules,and even nanoparticles,by creating micron-sized pores in the stratum corneum layer of the skin.In this report,the feasibility of using microneedles to increase the skin permeability of 5-FU was tested.Using full thickness mouse skin mounted on Franz diffusion apparatus,it was shown that the flux of 5-FU through the skin was increased by up to 4.5-fold when the skin was pretreated with microneedles(500μm in length,50μm in base diameter).In a mouse model with B16-F10 mouse melanoma cells implanted in the subcutaneous space,the antitumor activity of a commercially available 5-FU topical cream(5%)was significantly enhanced when the cream was applied on a skin area that was pretreated with microneedles,as compared to when the cream was simply applied on a skin area,underneath which the tumor cells were implanted,and without pretreatment of the skin with microneedles.Fluorouracil is not approved for melanoma therapy,but the clinical efficacy of topical 5-FU against tumors such as basal cell carcinoma may be improved by integrating microneedle technology into the therapy.
基金supported by National Natural Science Foundation of China(grants 81872742 to Guoqiang Dong and 81725020 to Chunquan Sheng)the National Key R&D Program of China(grant 2017YFA0506000 to Chunquan Sheng)the Innovation Program of Shanghai Municipal Education Commission(Grant 2019-01-07-00-07-E00073 to Chunquan Sheng,China)
文摘A great challenge in multi-targetingdrug discovery is to identify drug-like lead compounds with therapeutic advantages over single target inhibitors and drug combinations.Inspired by our previous efforts in designing antitumor evodiamine derivatives,herein selective histone deacetylase 1(HDAC1)and topoisomerase 2(TOP2)dual inhibitors were successfully identified,which showed potent in vitro and in vivo antitumor potency.Particularly,compound 30 a was orally active and possessed excellent in vivo antitumor activity in the HCT116 xenograft model(TGI=75.2%,150 mg/kg,p.o.)without significant toxicity,which was more potent than HDAC inhibitor vorinostat,TOP inhibitor evodiamine and their combination.Taken together,this study highlights the therapeutic advantages of evodiamine-based HDAC1/TOP2 dual inhibitors and provides valuable leads for the development of novel multi-targeting antitumor agents.
基金Natural Science Foundation of Jiangsu Province(BK2009549)School Funds of Changzhou University(ZMF07020020)
文摘Objective To study the antitumor activity of extract from Salvia plebeia and investigate whether the extract induce apoptosis of K562 cells.Methods The aqueous,petroleum ether,dichloromethane(CH2Cl2),ethyl acetate,and butanol extracts were prepared from the aerial parts of S.plebeia.Taking fluorouracil as reference,the cytotoxic activities of these extracts on HeLa,A549,SGC-7901,HCT-116,K562,LoVo,DU-145,and HepG2 cells were evaluated.To clarify the apoptosis of K562 cells induced by CH2Cl2 extract,the methods of Hoechst 33258 staining,flow cytometry assay,and DNA ladder assay were investigated.Results The CH2Cl2 extract showed the most potent cytotoxic effect against K562 cells,with an IC50<15μg/mL for 3 d treatment.The characteristic apoptotic symptoms such as DNA fragmentation and chromatin condensation were also observed in the K562 cells.Conclusion The CH2Cl2 extract from S.plebeia may inhibit the cancer cell proliferation by inducing cell apoptosis.
基金supported by NSFC-Shandong Joint Fund(No.U1606403)Innovation Project of Qingdao National Laboratory for Marine Science and Technology(No.2015ASKJ02)。
文摘HYL derived from the venom of the solitary bee Hylaeus signatus(Hymenoptera:Colletidae)is anα-helical antimicrobial peptide with 16 residues.To explore whether HYL can be applied in anti-tumor therapy,we synthesized HYL and further modified its structure by using a solid-phase synthesis method,and then evaluated their antitumor activities.Firstly,we identified the key residues of HYL by alanine scanning strategy,and then a series of stapled peptides were synthesized by hydrocarbon stapling strategy without destroying the key residues.All the stapled peptides of HYL showed significant improvement not only inα-helicity,but also in antitumor activity and protease resistance when compared to the parent peptide HYL.The results showed that hydrophobicity and amphiphilicity are important factors affecting the antitumor activity of HYL,and the stapling strategy can significantly affect the proteolytic stability and helicity of HYL.What’s more,we find that the stapled peptides HYL-14,HYL-16 and HYL-18 show a promising prospect for novel anti-tumor drug development.
基金supported by the Chinese Academy of Medical Sciences(CAMS)Initiation fund for Medical Science(2016-I2M-1-008)the National Natural Science Foundation of China(Approval no.81673341)
文摘Objective:Nonsmall-cell lung cancer(NSCLC)is an aggressive,highly chemoresistant disease.Taxol is an effective chemotherapeutic drug widely used for the treatment of NSCLC.However,the clinical use of Taxol is limited due to the occurrence of adverse side effects under high therapeutic doses.Therefore,it is desirable to explore combination therapy to reduce the dose of chemotherapeutic drugs and achieve excellent outcomes.A biosynthetic ginsenoside,3-O-β-D-glucopyranosyl-dammar-24-ene-3β,20 S-diol(3β-O-Glc-DM,C3 DM)is obtained from microbial fermentation by metabolic engineering.Based on previous study findings,we aimed to explore the mechanism of combination therapy with C3 DM and Taxol and its increasing antitumor effect on Lewis lung cancer(LLC)in this study.Materials and Methods:A thiazolyl blue tetrazolium bromide(MTT)assay was performed to evaluate cell viability;the apoptotic effect was studied using cell apoptosis assay.The Lewis tumor xenograft experiment was performed to determine the effects of C3 DM combined with Taxol on tumor growth in vivo,and western blotting was performed to analyze protein expressions.Results:C3 DM effectively inhibited the proliferation of NSCLC cells.Moreover,C3 DM increased the antiproliferative activity of Taxol and significantly enhanced cell apoptosis induced by Taxol in Lewis lung cancer cells.C3 DM alone also suppressed Lewis tumor growth and enhanced the antitumor activity of Taxol in vivo.Western blot analysis revealed that the effects of the antiproliferation and apoptosis induction of C3 DM treatment alone or in combination with Taxol on Lewis lung cancer were mediated by inhibiting the interleukin-6(IL-6)/Jak2/STAT3 and IL-6/AKT signaling pathways.Conclusions:The results showed that C3 DM has the potential to be used in combination therapy with Taxol against NSCLC.
基金supported by the National Natural Science Foundation of China(No.21171132)the Natural Science Foundation Joint Project of Shandong Province(ZR2017LB025)Science Foundation of Weifang。
文摘A novel Ca(Ⅱ) coordination polymer,[Ca L_(2)(H_(2)O)_(2)]_(n) (1,HL=4-acetylphenoxyacetic acid) has been synthesized with 4-acetylphenoxyacetic acid,Ca(ClO_4)_(2)·4H_(2)O and Na OH as raw materials.Complex 1 was characterized by elemental analysis and single-crystal X-ray diffraction analysis.The results show that the Ca(Ⅱ)ion is eight-coordinated in a distorted triangular dodecahedral geometric configuration with six carboxylate Oatoms of four L ligands and two O atoms of two coordinated water molecules.Complex 1 forms a one-dimensional chained structure by the bridging effect of carboxylate O atoms.The antitumor activity of HLligand and complex 1 has also been investigated.
基金Scientific Research Program Funded by Shaanxi Provincial Education Department(No.18JK0837)Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2018JM2045)+2 种基金Science and Technology Projects of Xianyang City(No.2017k02-19)Scientific Research Project Funded by Xianyang Normal University(No.XSYK18006)Qing-Lan Talents Project Funded by Xianyang Normal University(No.XSYQL201904)。
文摘In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.
基金Research Grant from Liaoning Province Office of EducationChina(No.L2014395)+1 种基金the Natural Science Foundation of Liaoning Province(No.201602711)Supporting Program for Young Researchers from Sheyang Pharmaceutical University。
文摘In this study, arsenic trioxide(ATO) was encapsulated in liposomes via copper acetate(Cu(OAc)2) gradients and high entrapment efficiency of over 80% was obtained. The average particle size and the zeta-potential of the liposomes were detected to be 115.1 ± 29.1 nm and-21.97 ± 0.6 m V, respectively. The TEM images showed rod-like precipitates in the inner aqueous phase, which was supposed be due to the formation of insoluble ATO–Cu complex.The in vitro drug release of ATO–Cu liposomes exhibited a sustained release over 72 h, and the release rates decreased with the increase of the p H of release media. Pharmacokinetic and tissue distribution studies of ATO liposomes showed significantly reduced plasma clearance rate, increased AUC0–12h and T1/2, and improved tumor distribution of As compared to iv administration of ATO solution. The anti-tumor effect of ATO loaded liposomes to S180 tumor-bearing mice was significantly improved with a tumor inhibition rate of 61.2%,meanwhile the toxicity of encapsulated ATO was greatly decreased. In conclusion, ATO can be effectively encapsulated into liposomes by remote loading method via Cu(OAc)2 gradients;the co-administration of ATO and Cu(Ⅱ) via liposomal formulation may find wide applications in the treatment of various tumors.
文摘<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] a route in a simple and reproducible synthesis for a novel compound of coordinating Ru</span><sup><span style="font-family:Verdana;">+3</span></sup><span style="font-family:Verdana;"> with bipy and L-trip. The spectroscopic characterization in the mi</span><span style="font-family:Verdana;">ddle infrared region (FTIR) shows the interactions between Ru-(L-trip), evidenced by the displacement of the carboxylate ion band for</span><span><span style="font-family:Verdana;"> higher energies, and also by the displacements of aliphatic amine bands, suggesting that bidentate coordination of the L-trip ligand occurred. Analysis of the results obtained with thermoanalytical techniques showed that the minimum formula of the compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)]1/2H</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">O. Evaluation of the</span></span><span><span style="font-family:Verdana;"> antitumor potential of precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] showed the toxic effects on MCF-7 cell line, but </span></span><span style="font-family:Verdana;">did not show selectivity and not reached PBMC cells to the same extent. The evaluation of the antitumor potential of the newly synthesized compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)], demonstrated that the insertion of an L-tryptophan molecule into the precursor coordination sphere made it selective when compared to PBMC cells, for MCF-7 type tumor cells.</span>
基金Brazilian Research Funding Program(CAPES),University of Caxias do Sul(UCS),Brazilian Algae Research Group(RedeAlgas),Antarctic Brazilian Program(PROANTAR)for financial support for the development of this work.
文摘Background/Aim: Antarctic seaweeds are considered a promising source of compounds with anticancer activity. Colorectal cancer (CRC) is one of the most incident cancers with high mortality rates worldwide. This work aimed to characterize chemically extracts of the Antarctic macroalgae Iridaea cordata, Cystosphaera jacquinotii and Desmarestia anceps and to evaluate the cytotoxic effects against human colon cancer HCT 116 cell line. Materials and Methods: The extracts were obtained by depletion using an ultrasound probe and were identified by High-Performance Liquid Chromatography (HPLC) and Gas Chromatography coupled with Mass Spectrometry (GC-MS). Cell viability was determined by MTT assay. Results: Hexanic and chloroform extracts of the I. cordata and the hexanic, chloroform and methanolic extracts of D. anceps were able to inhibit growth of colorectal cancer cells in the three different incubation times (24, 48 and 72 h). Through GC analysis, 01 compounds were identified in the hexane extract and 02 compounds in the chloroform extract of the algae I. cordata. The hexane extract of D. anceps macroalgae presented 5 compounds, chloroform extract 10 and methanolic extract 3 respectively, with special highlight to fucosterol. Carotenoid analysis by HPLC identified β-carotene in all species, while zeaxanthin was present in the spectrum of I. cordata and C. jacquinotii. Fucoxanthin and violaxanthin were confirmed in the brown seaweeds C. jacquinotii and D. anceps. Conclusion: Extracts of macroalgae I. Cordata and D. anceps may be a source of therapeutic agents against CRC.
基金supported by Youth Backbone Teachers Project Funded by Xianyang Normal University(No.XSYGG201606)Scientific Research Program Funded by Shaanxi Provincial Education Department(No.16JK1822)+3 种基金Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2016JM5024)Science and Technology Projects of Xianyang City(No.2017k02-19)University Students Research and Innovation Training Program of Xianyang Normal University(No.2017060&201710722003)University Students Research and Innovation Training Program of Shaanxi Province(No.2490)
文摘The reaction of 5-hydroxyl-7-methoxyflavone(tectochrysin) with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one(1), which was characterized by FT-IR, 1 H-NMR, ^(13)C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673(8), b = 17.9938(15), c = 21.2004(17) ?, V = 3611.5(5) ?~3, Z = 8, μ = 0.6726 mm^(-1), Dc = 1.795 g/cm3, F(000) = 2080, the final R = 0.0358 and wR = 0.0644 with I > 2σ(I). The results show that the addition reaction occurs at the carbon-carbon double bond(C2 and C3) of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells(K562), human breast cancer cells(MCF-7) and human lung cancer cells(A549). 1 exhibited potent antitumor activities against human leukemia cells(K562) with the IC50 values of 18.9 μmol/L.
基金supported by the National Natural Science Foundation of China(No.21342006)the Program for Innovative Research Team of the Ministry of Education of China(No.IRT_14R36)
文摘In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1 Hbenzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) ?, Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702.
