Three new monoterpene indole alkaloids,3a-hydroxymethyl-ibogamine(1),3a-acetatemethoxyl-ibogamine(2),16a-hy-droxyl-ibogamine(3)together with six known alkaloids were isolated from the branches and leaves of Tabernaemo...Three new monoterpene indole alkaloids,3a-hydroxymethyl-ibogamine(1),3a-acetatemethoxyl-ibogamine(2),16a-hy-droxyl-ibogamine(3)together with six known alkaloids were isolated from the branches and leaves of Tabernaemontana divaricata(Apocynaceae).The structures of these alkaloids were determined by spectroscopic analyses.All isolated compounds showed no significant cytotoxicity against SGC-7901 gastric cancer,HeLa,and A-549 lung cancer cell lines(IC50>20μM).展开更多
Two hitherto unknown iboga-type indole alkaloids,namely(3R)-7,19-di-epi-3-methoxytabernoxidine(1)and(3R,19R)-19-hydroxy-3-(2-oxopropyl)voacangine(2),together with eight known alkaloids(3-10),were isolated from the twi...Two hitherto unknown iboga-type indole alkaloids,namely(3R)-7,19-di-epi-3-methoxytabernoxidine(1)and(3R,19R)-19-hydroxy-3-(2-oxopropyl)voacangine(2),together with eight known alkaloids(3-10),were isolated from the twigs and leaves of Tabernaemontana divaricata.Their structures were established on the basis of spectroscopic data interpretation,single crystal X-ray diffraction analysis and circular dichroism spectrum.展开更多
Objective:To investigate the antifertility effect of chronically administered Tabernaemontana divarkala(T.divaricata) leaf extract on male rats.Methods:The effect of 50%ethanol extract of T.divaricata leaves on reprod...Objective:To investigate the antifertility effect of chronically administered Tabernaemontana divarkala(T.divaricata) leaf extract on male rats.Methods:The effect of 50%ethanol extract of T.divaricata leaves on reproduction was studied on male rats.The study was divided into four groups of five animals each.The first groups(1) received vehicle alone to serve as control. The second,third and fourth groups(Ⅱ,ⅡandⅣ) of animals were administered the leaf extract daily at 50 mg/kg body weight,p.o.,100 nig/kg body weight,p.o.,and 200 mg/kg body weight, p.o.,respectively,for a period of 60 days.Results:Significant decreases in the weight of testes, epididymis,seminal vesicle and ventral prostate were observed.A dose related reduction in the testicular sperm count,epididymal sperm count and motility,number of fertile male,ratio between delivered and inseminated females and numbers of pups were observed.The testis showed a clear correlation between the dose and severity of lesions of seminiferous epithelium. In general,the seminiferous tubules appear reduced in size with a frequently filled eosinophilic material.Spermatogenesis arrested at the secondary spermatocyte stage.Pachytene spermatocytes were undergoing degeneration.Disorganisation and sloughing of immature germ cell were visible. Leydinf cells were atrophied.No morphological changes were observed in Sertoli cells.Significant reduction in serum concentration of luteinizing hormone and testosterone were observed.No distinct change in serum FSH concentration was recorded.The final body weights of all groups were elevated markedly.No alterations were recorded in any hematologiocal parameters. Conclusions:It is concluded that the 50%ethanol extract of T.divaricata leaf produced dose related effect on male reproduction without altering general bodv metabolism.展开更多
目的:对夹竹桃科狗牙花属植物中狗牙花的生物碱类化学成分进行分离并对分离得到的化合物进行结构鉴定。方法:将干燥狗牙花3.5 kg粉碎,加甲醇室温渗漉提取,收集渗滤液,将渗滤液减压浓缩得到浸膏。浸膏用2 mol·L^(-1)硫酸调节p H 2,...目的:对夹竹桃科狗牙花属植物中狗牙花的生物碱类化学成分进行分离并对分离得到的化合物进行结构鉴定。方法:将干燥狗牙花3.5 kg粉碎,加甲醇室温渗漉提取,收集渗滤液,将渗滤液减压浓缩得到浸膏。浸膏用2 mol·L^(-1)硫酸调节p H 2,加入乙酸乙酯萃取得到非碱性脂溶性成分浓缩物;萃取后的酸水液用氢氧化钠溶液调节p H 9~10,然后用三氯甲烷萃取,得到总生物碱10 g。通过硅胶柱色谱,小孔凝胶(MCI)柱色谱和LH-20羟丙基萄聚糖凝胶(Sephadex LH-20)柱色谱进行分离和重结晶技术纯化,应用TLC监测,分离得到纯度较高的单体化合物。利用现代波谱法结合理化分析对其化学结构进行进一步鉴定。结果:从狗牙花中共分离得到并鉴定了6个单吲哚生物碱,分别鉴定为ervaramine型:ervatamine(1),20-epiervatamine(3);vobasine型:tabernaemontanine(2),dregamine(4);aspidosperma型:(-)-mehranine(5),tetrahydroalstonine(6)。结论:化合物4,6为首次从该植物中分离得到。MTS法测定化合物的肿瘤细胞毒活性,化合物1~6对5种人体肿瘤细胞株(人早幼粒白血病细胞HL-60,人肝癌细胞SMMC-7721,人肺癌细胞A-549,人乳腺癌细胞MCF-7,人结肠癌细胞SW-480)未显示出细胞毒活性。展开更多
AIM:To study the in vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.METHODS:Aqueous decoction and methanol leaf extracts were tested for their ability to reduce croton oi...AIM:To study the in vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.METHODS:Aqueous decoction and methanol leaf extracts were tested for their ability to reduce croton oil-induced edema in the mouse ear after topical application.The methanol leaf extract dose-dependently inhibited the croton oil-induced ear edema in mice(ID50<500μg·cm 2).A bioassay-guided liquid–liquid fractionation of this methanol extract gave four active fractions:water insoluble(F1),hexane(F2),ethyl acetate(F3)and water(F4).RESULTS:The hexane fraction showed a very high activity(42.1%inhibition at0.7μg·cm 2)as compared to the control.The other fractions were less active(F1:56.1%at 506.2μg·cm-2;F3:57.3%at 289.3μg·cm 2;and F4:31.9%for 203.8μg·cm 2)while indomethacin gave 48.8%of inhibition at 90μg·cm 2.The activity of F1 and F3 may be at least in part explained by the presence of anti-inflammatory flavonoids,while the activity was not correlated to the tannin contents.No compounds were detected in the most active F2 fraction.CONCLUSIONS:The results give a rational support to the traditional use of T.divaricata in tropical India as anti-inflammatory agent.展开更多
AIM:To evaluate the anti-fertility effect of methanolic(MeTD) and aqueous(AqTD) flower extracts of Tabernaemon-tana divaricata in rats.METHODS:The anti-fertility activity of the extracts was evaluated using two experi...AIM:To evaluate the anti-fertility effect of methanolic(MeTD) and aqueous(AqTD) flower extracts of Tabernaemon-tana divaricata in rats.METHODS:The anti-fertility activity of the extracts was evaluated using two experimental animal models:1) Estrogenic activity was carried out in immature female rats using ethinyl estradiol as standard.The evaluation parameters includes changes in uterine weight and histopathology of uterus.2) Anti-implantation and early abortifacient activity was performed in female Wistar rats.The number of implants and resorbtions were compared to vehicle control.RESULTS:Phytochemical analysis of MeTD and AqTD revealed the presence of carbohydrates,amino acids,steroids,glycosides,flavonoids,alkaloids and tannins.In estrogenic activity,the MeTD and AqTD were offered significant estrogen-like activity at 500 mg?kg-1,p.o.by increasing the uterine weight com-pared to vehicle control group.In Anti-implantation and early abortifacient activity study,MeTD(500 mg?kg-1,p.o.) showed significant effect and it was evident by decrease in the number of implants and increase in the number of resorbtions compared to vehicle control group.CONCLUSION:The MeTD at 500 mg?kg-1,p.o.possess significant estrogenic,anti-implantation and early abortifacient activ-ity,while the AqTD at 500 mg?kg-1,p.o.was found to possess significant estrogenic activity and the results are in consistent with the literature reports related to anti-fertility effect of flower extracts of Tabernaemontana divaricata.展开更多
基金supported by the Applied Basic Research Programs of Yunnan Province(No.2016FA030)the National Natural Science Foundation of China(31370377).
文摘Three new monoterpene indole alkaloids,3a-hydroxymethyl-ibogamine(1),3a-acetatemethoxyl-ibogamine(2),16a-hy-droxyl-ibogamine(3)together with six known alkaloids were isolated from the branches and leaves of Tabernaemontana divaricata(Apocynaceae).The structures of these alkaloids were determined by spectroscopic analyses.All isolated compounds showed no significant cytotoxicity against SGC-7901 gastric cancer,HeLa,and A-549 lung cancer cell lines(IC50>20μM).
基金This work was financially supported by the“Large-scale Compound Library”project of National Development and Reform Commission of China.
文摘Two hitherto unknown iboga-type indole alkaloids,namely(3R)-7,19-di-epi-3-methoxytabernoxidine(1)and(3R,19R)-19-hydroxy-3-(2-oxopropyl)voacangine(2),together with eight known alkaloids(3-10),were isolated from the twigs and leaves of Tabernaemontana divaricata.Their structures were established on the basis of spectroscopic data interpretation,single crystal X-ray diffraction analysis and circular dichroism spectrum.
文摘Objective:To investigate the antifertility effect of chronically administered Tabernaemontana divarkala(T.divaricata) leaf extract on male rats.Methods:The effect of 50%ethanol extract of T.divaricata leaves on reproduction was studied on male rats.The study was divided into four groups of five animals each.The first groups(1) received vehicle alone to serve as control. The second,third and fourth groups(Ⅱ,ⅡandⅣ) of animals were administered the leaf extract daily at 50 mg/kg body weight,p.o.,100 nig/kg body weight,p.o.,and 200 mg/kg body weight, p.o.,respectively,for a period of 60 days.Results:Significant decreases in the weight of testes, epididymis,seminal vesicle and ventral prostate were observed.A dose related reduction in the testicular sperm count,epididymal sperm count and motility,number of fertile male,ratio between delivered and inseminated females and numbers of pups were observed.The testis showed a clear correlation between the dose and severity of lesions of seminiferous epithelium. In general,the seminiferous tubules appear reduced in size with a frequently filled eosinophilic material.Spermatogenesis arrested at the secondary spermatocyte stage.Pachytene spermatocytes were undergoing degeneration.Disorganisation and sloughing of immature germ cell were visible. Leydinf cells were atrophied.No morphological changes were observed in Sertoli cells.Significant reduction in serum concentration of luteinizing hormone and testosterone were observed.No distinct change in serum FSH concentration was recorded.The final body weights of all groups were elevated markedly.No alterations were recorded in any hematologiocal parameters. Conclusions:It is concluded that the 50%ethanol extract of T.divaricata leaf produced dose related effect on male reproduction without altering general bodv metabolism.
文摘目的:对夹竹桃科狗牙花属植物中狗牙花的生物碱类化学成分进行分离并对分离得到的化合物进行结构鉴定。方法:将干燥狗牙花3.5 kg粉碎,加甲醇室温渗漉提取,收集渗滤液,将渗滤液减压浓缩得到浸膏。浸膏用2 mol·L^(-1)硫酸调节p H 2,加入乙酸乙酯萃取得到非碱性脂溶性成分浓缩物;萃取后的酸水液用氢氧化钠溶液调节p H 9~10,然后用三氯甲烷萃取,得到总生物碱10 g。通过硅胶柱色谱,小孔凝胶(MCI)柱色谱和LH-20羟丙基萄聚糖凝胶(Sephadex LH-20)柱色谱进行分离和重结晶技术纯化,应用TLC监测,分离得到纯度较高的单体化合物。利用现代波谱法结合理化分析对其化学结构进行进一步鉴定。结果:从狗牙花中共分离得到并鉴定了6个单吲哚生物碱,分别鉴定为ervaramine型:ervatamine(1),20-epiervatamine(3);vobasine型:tabernaemontanine(2),dregamine(4);aspidosperma型:(-)-mehranine(5),tetrahydroalstonine(6)。结论:化合物4,6为首次从该植物中分离得到。MTS法测定化合物的肿瘤细胞毒活性,化合物1~6对5种人体肿瘤细胞株(人早幼粒白血病细胞HL-60,人肝癌细胞SMMC-7721,人肺癌细胞A-549,人乳腺癌细胞MCF-7,人结肠癌细胞SW-480)未显示出细胞毒活性。
文摘AIM:To study the in vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.METHODS:Aqueous decoction and methanol leaf extracts were tested for their ability to reduce croton oil-induced edema in the mouse ear after topical application.The methanol leaf extract dose-dependently inhibited the croton oil-induced ear edema in mice(ID50<500μg·cm 2).A bioassay-guided liquid–liquid fractionation of this methanol extract gave four active fractions:water insoluble(F1),hexane(F2),ethyl acetate(F3)and water(F4).RESULTS:The hexane fraction showed a very high activity(42.1%inhibition at0.7μg·cm 2)as compared to the control.The other fractions were less active(F1:56.1%at 506.2μg·cm-2;F3:57.3%at 289.3μg·cm 2;and F4:31.9%for 203.8μg·cm 2)while indomethacin gave 48.8%of inhibition at 90μg·cm 2.The activity of F1 and F3 may be at least in part explained by the presence of anti-inflammatory flavonoids,while the activity was not correlated to the tannin contents.No compounds were detected in the most active F2 fraction.CONCLUSIONS:The results give a rational support to the traditional use of T.divaricata in tropical India as anti-inflammatory agent.
文摘AIM:To evaluate the anti-fertility effect of methanolic(MeTD) and aqueous(AqTD) flower extracts of Tabernaemon-tana divaricata in rats.METHODS:The anti-fertility activity of the extracts was evaluated using two experimental animal models:1) Estrogenic activity was carried out in immature female rats using ethinyl estradiol as standard.The evaluation parameters includes changes in uterine weight and histopathology of uterus.2) Anti-implantation and early abortifacient activity was performed in female Wistar rats.The number of implants and resorbtions were compared to vehicle control.RESULTS:Phytochemical analysis of MeTD and AqTD revealed the presence of carbohydrates,amino acids,steroids,glycosides,flavonoids,alkaloids and tannins.In estrogenic activity,the MeTD and AqTD were offered significant estrogen-like activity at 500 mg?kg-1,p.o.by increasing the uterine weight com-pared to vehicle control group.In Anti-implantation and early abortifacient activity study,MeTD(500 mg?kg-1,p.o.) showed significant effect and it was evident by decrease in the number of implants and increase in the number of resorbtions compared to vehicle control group.CONCLUSION:The MeTD at 500 mg?kg-1,p.o.possess significant estrogenic,anti-implantation and early abortifacient activ-ity,while the AqTD at 500 mg?kg-1,p.o.was found to possess significant estrogenic activity and the results are in consistent with the literature reports related to anti-fertility effect of flower extracts of Tabernaemontana divaricata.
