Objective:To investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius(A.ilicifolius).Methods:Antioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil(D...Objective:To investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius(A.ilicifolius).Methods:Antioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil(DPPH)method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test.Results:A.ilicifolius flower contained terpenoid,phenolic compounds,and alkaloid.The methanol extract of A.ilicifolius flower showed the highest antiradical efficiency(AE=1.41×10^(-3))against DPPH radicals and the highest cytotoxicity(LC_(50)=22μg/mL)against brine shrimp nauplii.Conclusions:It is suggested that active compounds of A.ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii.The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.展开更多
Objective: To isolate and evaluate the cytotoxic activity of different actinomycetes species isolated from the Red Sea coast in Sharm el-Sheikh, Egypt.Methods: Forty actinomycetes strains were isolated from different ...Objective: To isolate and evaluate the cytotoxic activity of different actinomycetes species isolated from the Red Sea coast in Sharm el-Sheikh, Egypt.Methods: Forty actinomycetes strains were isolated from different sediments and seawater samples collected from the Red Sea coast in Egypt. Actinomycetes were recognized by morphological and microscopic examinations. Cell viability and cytotoxicity induced by the crude extracts on breast cancer cell lines MDA-MB-231 were assessed using methylene blue assay. The strains with promising cytotoxic activity were identified by sequencing and amplifying the 16 S r RNA genes. The antibacterial activities of the crude extracts were performed using Kirby–Bauer disc diffusion method.Results: The results indicated that five ethyl acetate extracts exhibited cytotoxicity towards breast cancer cell lines MDA-MB-231. The highest cytotoxic activity was found for the ethyl acetate extracts of EGY2 and EGY39. The isolate EGY3 was identified as a new Streptomyces species, while the actinomycete EGY22 was found to be a member of the genus Nocardiopsis sp. The crude extract of the isolate EGY8 showed slightly high antimicrobial activity against different test microorganisms.Conclusions: The results of the present study reveal that marine sediments of the Red Sea are a potent source of novel species of actinomycetes. The isolates may be useful in discovery of novel bioactive compounds and an important step in the development of microbial natural product research.展开更多
The NAN-190 analogue 2-(2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethoxy)ethyl)isoindoline-1,3-dione(1, C23H27N3O4, Mr = 409.48) was synthesized via a three-step reaction and characterized by 1H NMR, 13 C NMR, ESIMS and...The NAN-190 analogue 2-(2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethoxy)ethyl)isoindoline-1,3-dione(1, C23H27N3O4, Mr = 409.48) was synthesized via a three-step reaction and characterized by 1H NMR, 13 C NMR, ESIMS and single-crystal X-ray diffraction. The crystal belongs to orthorhombic, space group Pna21 with a = 7.6445(15), b = 38.851(8), c = 7.1316(14) A, V = 2118.0(7) A3, Z = 4, Dc = 1.2840 mg/mm3, μ = 0.089 mm-1, F(000) = 872.4, R = 0.0545 and w R = 0.1681. The single-crystal X-ray structural analysis reveals that the piperazine ring in compound 1 presents a stable and minimum energy chair conformation. In addition, the preliminary cytotoxic assay shows that the title compound exhibits strong and selective inhibitory activity against DU145 cells(IC50 = 5.88 ± 1.02 μM).展开更多
A novel copper(Ⅱ) complex based on chiral amino-alcohol derived Schiff base ligand,[Cu_4(R-L)_4(H_2O)_2]·(CH_3COOH)_2·(H_2O)(1,(R)-H_2 L =(R)-3-phenyl-2-(2-hydroxy-3-methoxybenzylideneamino) propane-1-ol),w...A novel copper(Ⅱ) complex based on chiral amino-alcohol derived Schiff base ligand,[Cu_4(R-L)_4(H_2O)_2]·(CH_3COOH)_2·(H_2O)(1,(R)-H_2 L =(R)-3-phenyl-2-(2-hydroxy-3-methoxybenzylideneamino) propane-1-ol),was synthesized and characterized by EA,IR,UV-Vis,ESI-MS,circular dichroism spectra and single-crystal X-ray diffraction.Complex 1 crystallizes in orthorhombic,space group Ρ2_12_12 with a = 15.7660(14),b = 49.526(3),c = 10.4213(9) ?,V = 8137.2(12) ?~3,Ζ = 4,C_(72)H_(81)Cu_4N_4O_(19),Mr = 1560.57,μ = 1.096 mm^(-1),F(000) = 3244,Flack = 0.06(3),the final R = 0.0924 and w R = 0.2451(I > 2σ(I)) for 41108 observed reflections.The interactions of the complex with calf thymus DNA(CT-DNA) were investigated by some spectroscopic technique methods.The results show the complex exhibits strong binding with CT-DNA.In addition,in vitro cytotoxicity test of 1 towards four kinds of human cancerous cell lines(He La,HL-60,Caco-2 and A549) showed substantial cytotoxic activity.The experimental investigations indicated that the chirality of complex 1 play an important role in cytotoxicity and interactions with DNA.展开更多
Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effec...Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effect of isolated compound（β-Sitosterol triacontenate） was investigated by MTT assay on A549 solid tumor cells.Results:IC<sub>50</sub> value of theβ-Sitosterol triacontenate was found to be 1μM.The cytotoxic activity increased in a dose dependent manner in case ofβ-Sitosterol triacontenate.Conclusions:The data therefore provide direct evidence for the role ofβ-Sitosterol triacontenate as a potent antimetastatic agent,which can markedly inhibit the metastatic and invasive capacity of malignant cells.展开更多
Objective: To evaluate the in vitro cytotoxic activity of the fractionated extract as well as isolated compounds of Arum palaestinum Boiss.(A. palaestinum)(black calla lily), and to identify the volatile components wh...Objective: To evaluate the in vitro cytotoxic activity of the fractionated extract as well as isolated compounds of Arum palaestinum Boiss.(A. palaestinum)(black calla lily), and to identify the volatile components which may be responsible for the potential antitumor activity.Methods: A. palaestinum was collected from its natural habitats and subjected to phytochemical analysis for separation of pure compounds. In vitro cytotoxic activity was investigated against four human carcinoma cell lines Hep2, He La, Hep G2 and MCF7 for the fractionated extract and isolated compounds. While, the diethyl ether fraction was subjected to GC–MS analysis as it exhibited the most potent cytotoxic effect to evaluate the active constituents responsible for the cytotoxic activities.Results: Four flavonoid compounds were isolated(luteolin, chrysoeriol, isoorientin,isovitexin) from the diethyl ether and ethyl acetate. The extracts and the pure isolated compounds showed a significant high antiproliferative activity against all investigated cell lines. The GC–MS analysis revealed the separation and identification of 15 compounds representing 95.01% of the extract and belonging to different groups of chemical compounds.Conclusions: The present study is considered to be the first report on the cytotoxic activities carried out on different selected fractions and pure compounds of A. palaestinum to provide evidences for its strong antitumor activities. In addition,chrysoeriol and isovitexin compounds were isolated for the first time from the studied taxa.展开更多
The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were comb...The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were combined and concentrated under reduced pressure to yield residue,which was suspended in water and successively partitioned with chloroform.The chloroform extraction was isolated and purified by silica gel and Sephadex LH-20 column chromatography.Six compounds were isolated and elucidated as delelatine(1),isodelpheline(2),3-acetylaconitine(3),isoatisine(4),nordhagenine A(5)and yunaconitine(6).Compounds 1-5 were obtained from Aconitum Brunneum for the first time.Compound(1)showed significant cytotoxic activities(IC50=4.36 μM)against the human tumor cell line P388.展开更多
A novel Schiff base complex with π-conjugated system, [Ni(L1)2(py)2] 1 (L1 = (E)-N'-(2,4-dichlorobenzylidene)-2-oxidobenzohydraizide), was synthesized and characterized by elemental analysis and single-crystal X-...A novel Schiff base complex with π-conjugated system, [Ni(L1)2(py)2] 1 (L1 = (E)-N'-(2,4-dichlorobenzylidene)-2-oxidobenzohydraizide), was synthesized and characterized by elemental analysis and single-crystal X-ray determination. Complex 1 crystallizes in the monoclinic system, space group P21/n with a = 12.8286(10), b = 16.3573(13), c = 19.0206(14) , β = 108.2920(10)o, V = 3789.6(5) 3, Z = 4, Mr = 833.17, Dc = 1.460 g/cm3, μ = 0.843 mm-1, F(000) = 1704, the final R = 0.0537 and wR = 0.0640 for 3836 observed reflections with I > 2σ(I). In the molecular structure of 1, the NiII atoms are six-coordinated by two N and two O atoms from two Schiff base ligands (L1) and two N atoms from two pyridine solvent molecules to form a distorted octahedral geometry. The cytotoxic activities of complex 1 have been experimentally studied against a human HeLa cell in vitro.展开更多
Three new minor prenylated flavonoids,named macadenanthins A–C(1–3),together with three known ones(4–6),were isolated from the twigs of Macaranga adenantha.Their structures were elucidated on the basis of extensive...Three new minor prenylated flavonoids,named macadenanthins A–C(1–3),together with three known ones(4–6),were isolated from the twigs of Macaranga adenantha.Their structures were elucidated on the basis of extensive spectroscopic analysis including NMR,UV and MS.The prenyl moieties in compounds 1–3 were further modified by cyclization and hydroxylation.The new compounds were tested for their cytotoxicity against four cancer cell lines(MCF-7,Hep G2,Hela and P388)and showed IC50 values in the range of 13.76–22.27 lM.展开更多
The title compound(C29H33NO2,3)was synthesized and structurally characterized by elemental analysis,IR,MS,1H-and13C-NMR and single-crystal X-ray diffraction.The crystal is of monoclinic system,space group P21with a=14...The title compound(C29H33NO2,3)was synthesized and structurally characterized by elemental analysis,IR,MS,1H-and13C-NMR and single-crystal X-ray diffraction.The crystal is of monoclinic system,space group P21with a=14.428(3),b=7.3440(15),c=22.768(5),β=95.17(3),V=2402.7(8)3,Z=4,Mr=427.56,Dc=1.182 g/cm3,F(000)=920,λ(MoKα)=0.71073,μ=0.073 mm-1,the final R=0.0670 and wR=0.1002 for 2437 reflections with I>2σ(I).Two crystallographically independent molecules with different conformations co-exist in the structure.The crystal structure is stabilized by intermolecular C Hπinteractions which make the molecules stack along the b axis.In addition,the preliminary cytotoxic assay showed that the title compound exhibited moderate inhibitory activity against KB and SW1116 cells.展开更多
Objective:To evaluate the cytotoxic activities of Premna odorata(P.odorata)leaves and bark,Artocarpus camansi(A.camansi)and Gliricidia sepium against selected human cancer cell lines by using 3-(4,5-dimethylthiazol-2-...Objective:To evaluate the cytotoxic activities of Premna odorata(P.odorata)leaves and bark,Artocarpus camansi(A.camansi)and Gliricidia sepium against selected human cancer cell lines by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)assay.Methods:The crude extracts of P.odorata,A.camansi and Gliricidia sepium were subjected to liquid–liquid partitioning by using hexane and ethyl acetate to separate compounds based on their polarity.The fractions were tested for their cytotoxic activity against human colon cancer cell line(HCT116),breast cancer cell line(MCF-7),lung adenocarcinoma cell line(A549)and Chinese hamster ovary cell line(AA8)by using MTT assay.Results:Based on the standard values of toxicity set by the study of Suffness and Pezzuto,P.odorata leaves and P.odorata bark hexane fractions and A.camansi leaves were all considered highly cytotoxic against the selected human cancer cell lines.P.odorata bark hexane extract exhibited the highest selectivity index for HCT116,MCF-7 and A549 cancer cell lines.Conclusions:The results obtained indicated that P.odorata leaves and bark and A.camansi leaves have excellent cytotoxic activity and warrant further studies to isolate novel compounds for chemotherapeutic use.展开更多
The preliminary study is aimed at evaluating the cytotoxic activity of crude extracts from the stem bark of Canarium odontophyllum against colorectal carcinoma cell HCT 116. Result of the extraction yield showed that ...The preliminary study is aimed at evaluating the cytotoxic activity of crude extracts from the stem bark of Canarium odontophyllum against colorectal carcinoma cell HCT 116. Result of the extraction yield showed that distilled water produced the highest yield (10.58%) followed by methanol (6.55%) whereas acetone extracted the lowest yield (4.58%) from C. odontophyllum stem bark. Phytochemical screening test revealed the presence of terpenoid, flavonoid, tannin, saponin and phenolic compound in all the stem bark extracts of C. odontophyllum. Acetone extract of C. odontophyllum stem bark showed significantly higher (p < 0.05) cytotoxic effect with IC50 of 0.062 ± 1.04 mg/ml compared to methanol extract with IC50 0.122 ± 4.92 mg/ml. No cytotoxic effect was observed by the aqueous extract despite its high extraction yield. In conclusion, acetone and methanol extracts from C. odontophyllum stem bark exhibited promising cytotoxic activity against human colorectal cancer cell line HCT 116 and paves way for further investigation in view of its mode of cancer cell death.展开更多
N-Aryl-C-ethoxycarbonylnitrile imines (3a-g) react with ethyl cyanoacetate 1 in 1,3-dipolar cycloaddition to yield novel pyrazole-3,4-dicarboxylates (4a-g) in moderate yields. The reaction of pyrazole-3,4-dicarboxylat...N-Aryl-C-ethoxycarbonylnitrile imines (3a-g) react with ethyl cyanoacetate 1 in 1,3-dipolar cycloaddition to yield novel pyrazole-3,4-dicarboxylates (4a-g) in moderate yields. The reaction of pyrazole-3,4-dicarboxylates (4a, d) with hydrazine afforded pyrazolo[4,3-d]pyridazine-4,7-diones (5a, d) in good yields. All compounds were fully characterized by spectroscopic methods. Some of the newly synthesized compounds were evaluated for their cytotoxic activity against murine P815 mastocytoma cell line.展开更多
Most of marine sponges harbor dense and diverse microbial communities of bioactivity importance. Four Gram positive bacterial cultures (HA-21, HA-68, HA- MS-105 and HA-MS-119) were isolated from the sponge Amphimedon ...Most of marine sponges harbor dense and diverse microbial communities of bioactivity importance. Four Gram positive bacterial cultures (HA-21, HA-68, HA- MS-105 and HA-MS-119) were isolated from the sponge Amphimedon ochracea, collected from the Red Sea coast of Egypt. Bacterial species were identified based on the phylogenetic analysis of the nucleotide sequences of their 16S rDNA genes. The Sequences similarity values of 98% - 100% to other strains in the NCBI database showed strong similarities with the 16S rDNA genes of firmicutes (Bacillus sp.). The four bacterial species were submitted to the GenBank database and had accession numbers of: HA-21 [JQ-768238];HA-68 [JQ751264];HA-MS-105 [JQ768239];HAMS-119 [JQ768240]. The cytotoxic activities of the bacterial isolates were tested against three established human cancer cell lines;HepG2 (hepatocellular carcinoma), HCT (colon carcinoma) and MCF-7 (breast carcinoma). The inhibitory effect on these cell lines, measured by MTT cell assay protocol, revealed promising cytotoxic activity of the four isolates (IC50 values (μg/mL) were: HA-21: 13.2, 9.3 and 12.2;HA-68: 10.42, 4.3 and 5.5;HA-MS-105: 46.9, 28.6 and 21.3;HAMS-119: 10.42, 6.3 and 22.1;respectively). The recovery of bacterial strains with cytotoxic activity suggests that marine invertebrates remain a rich source for the isolation of culturable isolates capable of producing novel bioactive secondary metabolites.展开更多
Novel water-soluble prodrugs of combretastatin A-4 (5-8) were synthesized and evaluated for their in vitro cytotoxicity against lung carcinoma A549. Compound 5, bearing phosphoryl choline (PC) moiety, showed 90% inhib...Novel water-soluble prodrugs of combretastatin A-4 (5-8) were synthesized and evaluated for their in vitro cytotoxicity against lung carcinoma A549. Compound 5, bearing phosphoryl choline (PC) moiety, showed 90% inhibition at 32 μg/mL concentration after 24 h. The findings showed the PC derivative would be a promising candidate for the development of new water-soluble prodrug of cytotoxic combretastatin A-4.展开更多
The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosom...The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).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
Phytochemical investigations of the ethanolic extract of leaves of Clutia lanceolata(Family:Euphorbiaceae)resulted in the isolation of four compounds viz.3,4-dihydroxy-2-methylbenzoic acid(1),2,20-dihydroxy-1,10-binap...Phytochemical investigations of the ethanolic extract of leaves of Clutia lanceolata(Family:Euphorbiaceae)resulted in the isolation of four compounds viz.3,4-dihydroxy-2-methylbenzoic acid(1),2,20-dihydroxy-1,10-binaphthyl(2),1,3,8-trihydroxy-6-methylanthracene-9,10-dione(3)and 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one(4).Although all the isolated compounds were known but this was the first report from this plant source.Their structures were established on the basis of chemical and physical evidences viz.elemental analysis,FT-IR,1 H-NMR,13CNMR and mass spectral analysis.Structure of compound 2 and 4 was further authenticated by single-crystal X-ray analysis and density functional theory calculations.The isolated compounds(1–4)were screened for AChE enzyme inhibition assay in which compound 3 and 4 were found to be more potent AChE inhibitor.Molecular docking study of potent AChE inhibitor was performed to find the probable binding mode of the compounds into the active site of receptor.Moreover,the isolated compounds were also screened for in vivo cytotoxicity by brine shrimp lethality assay.展开更多
基金Supported by Directorate of Higher Education.Ministry of National EducationRepublic of Indonesia(DIPA Brawijaya University No.190/SK/2010)
文摘Objective:To investigate the antioxidant and cytotoxic activity of the flower of Acanthus ilicifolius(A.ilicifolius).Methods:Antioxidant activity was determined as antiradical efficiency with diphenyl picrylhydrazil(DPPH)method and cytotoxic assay was undertaken using brine shrimp lethal toxicity test.Results:A.ilicifolius flower contained terpenoid,phenolic compounds,and alkaloid.The methanol extract of A.ilicifolius flower showed the highest antiradical efficiency(AE=1.41×10^(-3))against DPPH radicals and the highest cytotoxicity(LC_(50)=22μg/mL)against brine shrimp nauplii.Conclusions:It is suggested that active compounds of A.ilicifolius flower solved in methanol play a role to inhibit free radical activity and kill Artemia salina nauplii.The substances can be considered as potential antioxidant and cytotoxic agents as well as imminent candidate for cancer therapy.
基金Supported by the Egyptian Science and Technology Development fund(STDF)(Grant No.4930)
文摘Objective: To isolate and evaluate the cytotoxic activity of different actinomycetes species isolated from the Red Sea coast in Sharm el-Sheikh, Egypt.Methods: Forty actinomycetes strains were isolated from different sediments and seawater samples collected from the Red Sea coast in Egypt. Actinomycetes were recognized by morphological and microscopic examinations. Cell viability and cytotoxicity induced by the crude extracts on breast cancer cell lines MDA-MB-231 were assessed using methylene blue assay. The strains with promising cytotoxic activity were identified by sequencing and amplifying the 16 S r RNA genes. The antibacterial activities of the crude extracts were performed using Kirby–Bauer disc diffusion method.Results: The results indicated that five ethyl acetate extracts exhibited cytotoxicity towards breast cancer cell lines MDA-MB-231. The highest cytotoxic activity was found for the ethyl acetate extracts of EGY2 and EGY39. The isolate EGY3 was identified as a new Streptomyces species, while the actinomycete EGY22 was found to be a member of the genus Nocardiopsis sp. The crude extract of the isolate EGY8 showed slightly high antimicrobial activity against different test microorganisms.Conclusions: The results of the present study reveal that marine sediments of the Red Sea are a potent source of novel species of actinomycetes. The isolates may be useful in discovery of novel bioactive compounds and an important step in the development of microbial natural product research.
基金supported by the Technological Innovation Project of Colleges and Universities in Guangdong Province(No.cx2d1127)the China Postdoctoral Science Foundation(Nos.2013M542165 and 2013M531837)+1 种基金the Guangzhou Postdoctoral Scientific Research Foundation(Nos.Q130 and Q074)the Natural Science Foundation of Guangdong Province(No.S2013040014088)
文摘The NAN-190 analogue 2-(2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethoxy)ethyl)isoindoline-1,3-dione(1, C23H27N3O4, Mr = 409.48) was synthesized via a three-step reaction and characterized by 1H NMR, 13 C NMR, ESIMS and single-crystal X-ray diffraction. The crystal belongs to orthorhombic, space group Pna21 with a = 7.6445(15), b = 38.851(8), c = 7.1316(14) A, V = 2118.0(7) A3, Z = 4, Dc = 1.2840 mg/mm3, μ = 0.089 mm-1, F(000) = 872.4, R = 0.0545 and w R = 0.1681. The single-crystal X-ray structural analysis reveals that the piperazine ring in compound 1 presents a stable and minimum energy chair conformation. In addition, the preliminary cytotoxic assay shows that the title compound exhibits strong and selective inhibitory activity against DU145 cells(IC50 = 5.88 ± 1.02 μM).
基金supported by the Natural Science Foundation of Shandong Province(No.ZR2013BM017)the Natural Science Foundation of China(No.21105042)
文摘A novel copper(Ⅱ) complex based on chiral amino-alcohol derived Schiff base ligand,[Cu_4(R-L)_4(H_2O)_2]·(CH_3COOH)_2·(H_2O)(1,(R)-H_2 L =(R)-3-phenyl-2-(2-hydroxy-3-methoxybenzylideneamino) propane-1-ol),was synthesized and characterized by EA,IR,UV-Vis,ESI-MS,circular dichroism spectra and single-crystal X-ray diffraction.Complex 1 crystallizes in orthorhombic,space group Ρ2_12_12 with a = 15.7660(14),b = 49.526(3),c = 10.4213(9) ?,V = 8137.2(12) ?~3,Ζ = 4,C_(72)H_(81)Cu_4N_4O_(19),Mr = 1560.57,μ = 1.096 mm^(-1),F(000) = 3244,Flack = 0.06(3),the final R = 0.0924 and w R = 0.2451(I > 2σ(I)) for 41108 observed reflections.The interactions of the complex with calf thymus DNA(CT-DNA) were investigated by some spectroscopic technique methods.The results show the complex exhibits strong binding with CT-DNA.In addition,in vitro cytotoxicity test of 1 towards four kinds of human cancerous cell lines(He La,HL-60,Caco-2 and A549) showed substantial cytotoxic activity.The experimental investigations indicated that the chirality of complex 1 play an important role in cytotoxicity and interactions with DNA.
文摘Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effect of isolated compound（β-Sitosterol triacontenate） was investigated by MTT assay on A549 solid tumor cells.Results:IC<sub>50</sub> value of theβ-Sitosterol triacontenate was found to be 1μM.The cytotoxic activity increased in a dose dependent manner in case ofβ-Sitosterol triacontenate.Conclusions:The data therefore provide direct evidence for the role ofβ-Sitosterol triacontenate as a potent antimetastatic agent,which can markedly inhibit the metastatic and invasive capacity of malignant cells.
基金Support by Science and Technology Development Fund,with Grant No.4402
文摘Objective: To evaluate the in vitro cytotoxic activity of the fractionated extract as well as isolated compounds of Arum palaestinum Boiss.(A. palaestinum)(black calla lily), and to identify the volatile components which may be responsible for the potential antitumor activity.Methods: A. palaestinum was collected from its natural habitats and subjected to phytochemical analysis for separation of pure compounds. In vitro cytotoxic activity was investigated against four human carcinoma cell lines Hep2, He La, Hep G2 and MCF7 for the fractionated extract and isolated compounds. While, the diethyl ether fraction was subjected to GC–MS analysis as it exhibited the most potent cytotoxic effect to evaluate the active constituents responsible for the cytotoxic activities.Results: Four flavonoid compounds were isolated(luteolin, chrysoeriol, isoorientin,isovitexin) from the diethyl ether and ethyl acetate. The extracts and the pure isolated compounds showed a significant high antiproliferative activity against all investigated cell lines. The GC–MS analysis revealed the separation and identification of 15 compounds representing 95.01% of the extract and belonging to different groups of chemical compounds.Conclusions: The present study is considered to be the first report on the cytotoxic activities carried out on different selected fractions and pure compounds of A. palaestinum to provide evidences for its strong antitumor activities. In addition,chrysoeriol and isovitexin compounds were isolated for the first time from the studied taxa.
基金financially supported by the Scientific Research Program Funded by Shaanxi Provincial Department(2010JK74909JK672)+1 种基金by the Special Research Fund for the Doctoral Program of Higher Education(20096118110008)the Natural Science Foundation of Shaanxi Province(SJ08B16)
文摘The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were combined and concentrated under reduced pressure to yield residue,which was suspended in water and successively partitioned with chloroform.The chloroform extraction was isolated and purified by silica gel and Sephadex LH-20 column chromatography.Six compounds were isolated and elucidated as delelatine(1),isodelpheline(2),3-acetylaconitine(3),isoatisine(4),nordhagenine A(5)and yunaconitine(6).Compounds 1-5 were obtained from Aconitum Brunneum for the first time.Compound(1)showed significant cytotoxic activities(IC50=4.36 μM)against the human tumor cell line P388.
基金supported by the National Natural Science Foundation of China (No. 30672516)
文摘A novel Schiff base complex with π-conjugated system, [Ni(L1)2(py)2] 1 (L1 = (E)-N'-(2,4-dichlorobenzylidene)-2-oxidobenzohydraizide), was synthesized and characterized by elemental analysis and single-crystal X-ray determination. Complex 1 crystallizes in the monoclinic system, space group P21/n with a = 12.8286(10), b = 16.3573(13), c = 19.0206(14) , β = 108.2920(10)o, V = 3789.6(5) 3, Z = 4, Mr = 833.17, Dc = 1.460 g/cm3, μ = 0.843 mm-1, F(000) = 1704, the final R = 0.0537 and wR = 0.0640 for 3836 observed reflections with I > 2σ(I). In the molecular structure of 1, the NiII atoms are six-coordinated by two N and two O atoms from two Schiff base ligands (L1) and two N atoms from two pyridine solvent molecules to form a distorted octahedral geometry. The cytotoxic activities of complex 1 have been experimentally studied against a human HeLa cell in vitro.
基金National Natural Science Foundation of China(31300293 and 81422046)General Project of Applied Foundation Research,Yunnan Province(2013FB067)+1 种基金Basic Research Project of Ministry of Science and Technology of China(2012FY110300)Major State Basic Research Development Program(2010CB951704).
文摘Three new minor prenylated flavonoids,named macadenanthins A–C(1–3),together with three known ones(4–6),were isolated from the twigs of Macaranga adenantha.Their structures were elucidated on the basis of extensive spectroscopic analysis including NMR,UV and MS.The prenyl moieties in compounds 1–3 were further modified by cyclization and hydroxylation.The new compounds were tested for their cytotoxicity against four cancer cell lines(MCF-7,Hep G2,Hela and P388)and showed IC50 values in the range of 13.76–22.27 lM.
基金Supported by the National Natural Science Foundation of China(Project:31000273)Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘The title compound(C29H33NO2,3)was synthesized and structurally characterized by elemental analysis,IR,MS,1H-and13C-NMR and single-crystal X-ray diffraction.The crystal is of monoclinic system,space group P21with a=14.428(3),b=7.3440(15),c=22.768(5),β=95.17(3),V=2402.7(8)3,Z=4,Mr=427.56,Dc=1.182 g/cm3,F(000)=920,λ(MoKα)=0.71073,μ=0.073 mm-1,the final R=0.0670 and wR=0.1002 for 2437 reflections with I>2σ(I).Two crystallographically independent molecules with different conformations co-exist in the structure.The crystal structure is stabilized by intermolecular C Hπinteractions which make the molecules stack along the b axis.In addition,the preliminary cytotoxic assay showed that the title compound exhibited moderate inhibitory activity against KB and SW1116 cells.
基金Supported by the Institute of Biology IB Trust Fund9774197-499-439 of the University of the Philippines Diliman
文摘Objective:To evaluate the cytotoxic activities of Premna odorata(P.odorata)leaves and bark,Artocarpus camansi(A.camansi)and Gliricidia sepium against selected human cancer cell lines by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)assay.Methods:The crude extracts of P.odorata,A.camansi and Gliricidia sepium were subjected to liquid–liquid partitioning by using hexane and ethyl acetate to separate compounds based on their polarity.The fractions were tested for their cytotoxic activity against human colon cancer cell line(HCT116),breast cancer cell line(MCF-7),lung adenocarcinoma cell line(A549)and Chinese hamster ovary cell line(AA8)by using MTT assay.Results:Based on the standard values of toxicity set by the study of Suffness and Pezzuto,P.odorata leaves and P.odorata bark hexane fractions and A.camansi leaves were all considered highly cytotoxic against the selected human cancer cell lines.P.odorata bark hexane extract exhibited the highest selectivity index for HCT116,MCF-7 and A549 cancer cell lines.Conclusions:The results obtained indicated that P.odorata leaves and bark and A.camansi leaves have excellent cytotoxic activity and warrant further studies to isolate novel compounds for chemotherapeutic use.
文摘The preliminary study is aimed at evaluating the cytotoxic activity of crude extracts from the stem bark of Canarium odontophyllum against colorectal carcinoma cell HCT 116. Result of the extraction yield showed that distilled water produced the highest yield (10.58%) followed by methanol (6.55%) whereas acetone extracted the lowest yield (4.58%) from C. odontophyllum stem bark. Phytochemical screening test revealed the presence of terpenoid, flavonoid, tannin, saponin and phenolic compound in all the stem bark extracts of C. odontophyllum. Acetone extract of C. odontophyllum stem bark showed significantly higher (p < 0.05) cytotoxic effect with IC50 of 0.062 ± 1.04 mg/ml compared to methanol extract with IC50 0.122 ± 4.92 mg/ml. No cytotoxic effect was observed by the aqueous extract despite its high extraction yield. In conclusion, acetone and methanol extracts from C. odontophyllum stem bark exhibited promising cytotoxic activity against human colorectal cancer cell line HCT 116 and paves way for further investigation in view of its mode of cancer cell death.
文摘N-Aryl-C-ethoxycarbonylnitrile imines (3a-g) react with ethyl cyanoacetate 1 in 1,3-dipolar cycloaddition to yield novel pyrazole-3,4-dicarboxylates (4a-g) in moderate yields. The reaction of pyrazole-3,4-dicarboxylates (4a, d) with hydrazine afforded pyrazolo[4,3-d]pyridazine-4,7-diones (5a, d) in good yields. All compounds were fully characterized by spectroscopic methods. Some of the newly synthesized compounds were evaluated for their cytotoxic activity against murine P815 mastocytoma cell line.
文摘Most of marine sponges harbor dense and diverse microbial communities of bioactivity importance. Four Gram positive bacterial cultures (HA-21, HA-68, HA- MS-105 and HA-MS-119) were isolated from the sponge Amphimedon ochracea, collected from the Red Sea coast of Egypt. Bacterial species were identified based on the phylogenetic analysis of the nucleotide sequences of their 16S rDNA genes. The Sequences similarity values of 98% - 100% to other strains in the NCBI database showed strong similarities with the 16S rDNA genes of firmicutes (Bacillus sp.). The four bacterial species were submitted to the GenBank database and had accession numbers of: HA-21 [JQ-768238];HA-68 [JQ751264];HA-MS-105 [JQ768239];HAMS-119 [JQ768240]. The cytotoxic activities of the bacterial isolates were tested against three established human cancer cell lines;HepG2 (hepatocellular carcinoma), HCT (colon carcinoma) and MCF-7 (breast carcinoma). The inhibitory effect on these cell lines, measured by MTT cell assay protocol, revealed promising cytotoxic activity of the four isolates (IC50 values (μg/mL) were: HA-21: 13.2, 9.3 and 12.2;HA-68: 10.42, 4.3 and 5.5;HA-MS-105: 46.9, 28.6 and 21.3;HAMS-119: 10.42, 6.3 and 22.1;respectively). The recovery of bacterial strains with cytotoxic activity suggests that marine invertebrates remain a rich source for the isolation of culturable isolates capable of producing novel bioactive secondary metabolites.
文摘Novel water-soluble prodrugs of combretastatin A-4 (5-8) were synthesized and evaluated for their in vitro cytotoxicity against lung carcinoma A549. Compound 5, bearing phosphoryl choline (PC) moiety, showed 90% inhibition at 32 μg/mL concentration after 24 h. The findings showed the PC derivative would be a promising candidate for the development of new water-soluble prodrug of cytotoxic combretastatin A-4.
文摘The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).
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.
文摘Phytochemical investigations of the ethanolic extract of leaves of Clutia lanceolata(Family:Euphorbiaceae)resulted in the isolation of four compounds viz.3,4-dihydroxy-2-methylbenzoic acid(1),2,20-dihydroxy-1,10-binaphthyl(2),1,3,8-trihydroxy-6-methylanthracene-9,10-dione(3)and 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one(4).Although all the isolated compounds were known but this was the first report from this plant source.Their structures were established on the basis of chemical and physical evidences viz.elemental analysis,FT-IR,1 H-NMR,13CNMR and mass spectral analysis.Structure of compound 2 and 4 was further authenticated by single-crystal X-ray analysis and density functional theory calculations.The isolated compounds(1–4)were screened for AChE enzyme inhibition assay in which compound 3 and 4 were found to be more potent AChE inhibitor.Molecular docking study of potent AChE inhibitor was performed to find the probable binding mode of the compounds into the active site of receptor.Moreover,the isolated compounds were also screened for in vivo cytotoxicity by brine shrimp lethality assay.
