Antifertility effect of chronically administered Tabernaemontana divaricata leaf extract on male rats

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.

Three New Indole Alkaloids from Tabernaemontana divaricata

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).

New Iboga‑Type Indole Alkaloids from Tabernaemontana divaricata

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.

Antimicrobial indole alkaloids from Tabernaemontana corymbosa

Four unreported monoterpene indole alkaloids,tabernaecorymines B−E(1−4),together with twenty-one known indole alkaloids(5−25)were obtained from the stem bark of Tabernaemontana corymbosa.Their structures and absolute configurations were elucidated by extensive spectroscopy,quantum chemical calculations,DP4+probability analyses and Mo2(OAc)4-induced electronic circular dichroism experiment.The antibacterial and antifungal activities of these compounds were evaluated and some of them showed significant activity against Staphylococcus aureus,Bacillus subtilis,Streptococcus dysgalactiae and Candida albicans.

Tabernaesine J,a Novel Vincamine-Type Indole Alkaloid with 6/5/6/6/6/5/5 Heptacyclic-Ring System Scaffold from Tabernaemontana pachysiphon

Comprehensive Summary Tabernaesine J(1),an unprecedented vincamine-type indole alkaloid with 6/5/6/6/6/5/5 heptacyclic-ring system,as well as one new biogenetically related vincamine-type indole alkaloid(2),were isolated from leaves of Tabernaemontana pachysiphon.Their structures were established by a combination of HRESIMS,NMR,single crystal X-ray diffraction,and ECD calculation.The unprecedented pen-ta-lactone ring in tabernaesine J(1)was postulated to be derived from acetyl-CoA enolate anion.Alkaloid 2 combined with fluconazole has the potential to overcome fluconazole resistance in Candida albicans.

In vivo pharmacological activities of methanolic extract of Tabernaemontana recurva Roxb

Objective: To evaluate analgesic, hypoglycemic, anxiolytic, and anthelmintic activities with phytochemical screening of methanolic extract of Tabernaemontana recurva (T. recurva) whole plants. Methods: The plant parts of T. recurva were collected, dried, powdered and extracted with methanol. Then the extracts were subjected to in vivo analgesic, hypoglycemic, anxiolytic activity in mice model and in vitro anthelmintic activity. Results: The analysis of phytochemical screening confirmed the existence of alkaloid, saponin, tannins, carbohydrate, phytosterols, glycosides and phenol. In analgesic test, a significant level of percentage inhibition of abdominal constriction was observed with concentration of 200 and 400 mg/kg of body weight of extract and this was found better with formalin induced hind paw licking test rather than acetic acid induced writhing test. In hypoglycemic test, it was observed that concentration 200 mg/kg reduced blood sugar level slightly while concentration 400 mg/kg increased glucose level by 22.95%. A significant level of anxiolytic activity was observed for the study plant extract. The extract revealed potent anthelmintic activity at different concentrations. Conclusions: In light, the methanolic extract of T. recurva exhibited excellent anthelmintic, anxiolytic and analgesic activity. This plant showed moderate hypoglycemic effect at lower concentration but higher concentration increased blood glucose level.

云南狗牙花中Ibogan型生物碱类成分的研究

目的:对夹竹桃科狗牙花属植物云南狗牙花Tabernaemontana yunnanensis Tsiang的Ibogan型生物碱类化学成分进行研究。方法:利用硅胶柱色谱、凝胶柱色谱、高速逆流色谱、HPLC等对云南狗牙花95%乙醇提取物进行化学成分的分离纯化,采用质谱、NMR等方法确定化合物结构。结果:从云南狗牙花中分离得到12个Ibogan型生物碱类化合物,分别鉴定为:3-(2-oxopropyl)voacangine(1)、voacangine-7-hydroxyindolenine(2)、(3S)-3-cyanoisovoacangine(3)、3-(2-oxopropyl)-coronaridine(4)、obovatine(5)、3-(β-hydroxyethyl)-coronaridine(6)、19-epi-heyneanine(7)、19-epi-isovoacristine(8)、3-oxo-voacangine(9)、ibogamine(10)、coronaridine pseudoindoxyl(11)、voacangine pseudoindoxyl(12)。结论:其中,化合物1、3~6、9、11和12为首次从该植物中分离得到,化合物11为首次从该属植物中分离得到。

药用狗牙花中单萜吲哚生物碱的研究

目的:研究药用狗牙花Tabernaemontana bovina Loureiro中的单萜吲哚生物碱类化学成分。方法:综合运用硅胶、反相、凝胶等柱色谱技术以及高速逆流色谱、高效液相色谱等方法对药用狗牙花中的单萜吲哚生物碱进行分离纯化,并根据化合物的理化性质及波谱数据鉴定其化学结构。结果:从药用狗牙花中的总生物碱部位中分离纯化得到12个单萜吲哚生物碱,分别鉴定为:tabernaebovine A(1)、dregamine(2)、tabernaemontanine(3)、16-epi-19,20(S)-dihydroperivine(4)、vobasine(5)、vobasidine C(6)、apparicine(7)、isovoacangine(8)、voacangine(9)、19-epi-heyneanine(10)、19-epi-isovoacristine(11)、voacristine(12)。结论:其中,化合物1为新化合物,化合物4为首次从该属植物中分离得到,化合物6~8、11为首次从药用狗牙花中分离得到。

二杈狗牙花化学成分的研究(Ⅱ)

目的:对二杈狗牙花根茎的化学成分进行分离及结构鉴定。方法:利用各种色谱技术进行分离,根据理化性质及波谱学方法进行结构鉴定。结果:分离得到6个化合物,二十八酸二甘油酯[bis(2,3-dihydroxypropyl)octacosanedioate,1],正三十四垸醇(tetratriacontanol,2),棕榈酸(palmitic acid,3),单棕榈酸甘油酯(glycerol monopalmitate,4),β-谷甾醇(β-sitosterol, 5),β-胡萝卜苷(daucosterol,6)。结论:化合物1为新化合物,化合物2～4均为首次从该属植物中分离得到。

二杈狗牙花化学成分研究

目的：对二杈狗牙花根茎的化学成分进行分离及结构鉴定。方法：利用硅胶柱、凝胶柱及反相硅胶柱等色谱柱技术进行分离，根据理化性质及波谱学方法进行结构鉴定。结果：分离得到7个化合物：α-香树醇（α-amyrin，1），α-香树醇乙酸酯（α-amyrin acetate，2），α-香树醇棕榈酯（α-amyryl palmitate，3），蒲公英甾醇乙酸酯（taraxasterol acetate，4），毛蕊异黄酮（calycosin，5），芒柄花素（formononetin，6），farnisin（7，3＇-dihydroxy-4’methoxyflavone，7）。结论：化合物1，3～7均为首次从本植物中分离得到，化合物3～7为首次从该属植物中分得。

PEG胁迫对柳叶水甘草种子萌发及幼苗的影响

采用不同质量分数的聚乙二醇(PEG-6000)模拟干旱胁迫的方法,研究干旱胁迫对柳叶水甘草(Amsoniatabernaemontana)种子萌发及幼苗生长的影响。结果表明,1)5%PEG处理种子其萌发率、萌发速率系数、萌发指数和活力指数均高于对照组,随着胁迫质量分数递增,萌发率下降,复水后,仍能萌发,种子具有一定的抗旱性。2)幼苗处理随着胁迫质量分数递增及胁迫时间延长,其叶片相对电导率、MDA含量显著增加;脯氨酸含量与叶片相对电导率和MDA含量呈极显著正相关,高质量分数PEG胁迫处理,脯氨酸含量增加;抗氧化酶SOD和POD活性先上升后下降。

不同处理对柳叶水甘草种子萌发的影响

通过采用不同温度处理、预先浸泡处理、不同浓度GA3处理等3种种子预处理方法进行柳叶水甘草种子萌发试验,结果表明:柳叶水甘草能够萌发的温度范围为15~30℃,最适萌发温度为25℃;预先浸泡处理对种子萌发率影响不显著,但显著提高种子发芽指数,浸泡时间为24时,种子发芽指数最高;预先用GA3浸泡有利于柳叶水甘草种子快速、整齐发芽,最适浓度为1 500×10^(-6)。

伞房狗牙花枝干化学成分的研究

从伞房狗牙花(Tabernaemontana corymbosa)枝干的甲醇提取物中分离得到6个吲哚类生物碱和2个非生物碱,经波谱技术和理化性质对化合物结构进行鉴定为:17-demethoxy-hydroisorhynchophylline(1)、voachalotine(2)、voachalotine oxindole(3)、voacristine(4)、14,15-dehydrovincamine(5)、16R-descarbomethoxytacamine(6)、α-amyrin acetate(7)和β-sitosterol(8),其中化合物2、3、5-7首次从该植物中分离得到。

药用狗牙花化学成分及其抑制滑膜成纤维细胞增殖活性研究

目的研究夹竹桃科狗牙花属植物药用狗牙花Tabernaemontana bovina枝叶中的化学成分及其抑制滑膜成纤维细胞增殖活性。方法综合运用硅胶柱色谱、ODS柱色谱、SephadexLH-20凝胶柱色谱以及制备型HPLC等色谱方法进行系统分离和纯化,根据分离得到化合物的理化性质及其波谱数据,并通过与文献中报道的相应化合物的波谱数据进行对比,鉴定分离得到化合物的化学结构;通过对分离得到化合物的体外抑制滑膜细胞增殖的活性测试以评价其抗类风湿性关节炎活性。结果从药用狗牙花枝叶的85%乙醇提取物中分离得到了19个化合物,分别鉴定为苏门树脂酸(1)、2α,19α-dihydroxy-3-oxo-12-ursen-28-oic acid(2)、6α-羟基齐墩果酮酸(3)、19α-羟基齐墩果酮酸(4)、garcinielliptone Q(5)、阿里二醇(6)、款冬二醇(7)、taraxast-20-ene-3β,30-diol(8)、马尼拉二醇(9)、16β-羟基羽扇豆烷-20(29)-烯-3-酮(10)、eupha-8,24-diene-3β,11β-diol-7-one(11)、2α,3β-二羟基-12-烯-28-乌苏酸(12)、busaliol(13)、tripterygiol(14)、polystachyol(15)、rosalaevin B(16)、cephafortin B(17)、burselignan(18)和latifoliamide A(19)。对分离得到的化合物的抑制滑膜成纤维细胞增殖活性研究评价结果表明,化合物13~18对MH7A滑膜成纤维细胞增殖抑制活性的IC50值为(6.49±0.08)~(123.58±0.23)μmol/L。结论所有化合物均为首次从药用狗牙花中分离得到,化合物13~18表现出了较为显著的抗类风湿性关节炎活性。

狗牙花生物碱成分分析

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。

马蹄花叶提取物在雄性白化病小鼠体内的抗炎作用(英文)

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.

海南尖峰岭热带山地雨林2种夹竹桃科植物的空间分布格局与关联性

根类药用植物在生产栽培过程中常产生连作障碍,原因之一是其容易产生化感作用,而化感作用是密度制约产生的主要原因之一。夹竹桃科植物是重要的药用植物,也是热带植物区系的主要科。为探究自然条件下密度制约是否存在于根类药用植物中,本文以海南尖峰岭60 ha森林动态监测样地中两种常见的夹竹桃科根类药用植物盆架树(Alstonia rostrata)和尖蕾狗牙花(Tabernaemontana bufalina)为研究对象,采用点格局分析的成对相关函数Ripley’s g(r),结合完全随机零模型和异质泊松零模型,分析了它们的空间分布格局、种内和种间空间关联,并采用Berman-test方法分析了地形因子对其种群分布的影响。结果表明:(1)盆架树和尖蕾狗牙花在0–100 m的研究尺度上主要表现为聚集分布,但随着尺度的增大,聚集程度降低,逐渐变为随机分布。(2)盆架树和尖蕾狗牙花各龄级的分布特征类似:幼树和中龄树个体在较大尺度范围内为聚集分布,而成年树个体在0–100 m尺度上为随机分布或均匀分布。(3)在小尺度上,盆架树的幼树与中龄树呈空间正关联,与成年树呈空间负关联,而中龄树与成年树空间无关联。尖蕾狗牙花各龄级间在0–65 m的尺度范围内以空间正关联为主。(4)在0–49 m尺度内盆架树与尖蕾狗牙花呈显著空间正相关。盆架树的中龄树和成年树与同龄级的尖蕾狗牙花都表现为空间无显著关联,而幼树与尖蕾狗牙花幼树存在明显的空间正关联。(5)盆架树和尖蕾狗牙花幼树的分布与海拔、凹凸度显著正相关,中龄树的分布与凹凸度显著正相关,而成年树中只有盆架树的分布与海拔正相关。从现有格局推断:生境异质性和扩散限制影响盆架树和尖蕾狗牙花空间格局的形成,相对于尖蕾狗牙花,密度制约对盆架树空间格局形成的影响更显著。

普约狗牙花枝叶的生物碱类成分研究

目的研究夹竹桃科普约狗牙花Tabernaemontana sananho枝叶的化学成分。方法利用硅胶、ODS、Sephadex LH-20等柱色谱技术及薄层色谱、制备液相色谱等方法进行分离、纯化,根据化合物的理化性质及波谱学数据鉴定其化学结构。结果从普约狗牙花枝叶的总生物碱部位中分离得到12个生物碱类成分,分别鉴定为冠狗牙花碱氮氧化物(1)、3-羰基冠狗牙花碱(2)、3-羰基冠狗牙花羟基伪吲哚碱(3)、柳叶水甘草碱(4)、柳叶水甘草碱氮氧化物(5)、3-羰基柳叶水甘草碱(6)、5β-羟基-3-羰基柳叶水甘草碱(7)、lochnericine(8)、(+)-voaphylline(9)、deacetylakuammiline(10)、去氢骆驼蓬碱(11)和咖啡因(12)。结论化合物1为新的天然产物,化合物7和12为首次从该属植物中分离得到,化合物2~6、8~11为首次从该植物中分离得到。

马蹄花提取物对大鼠的抗生育作用(英文)

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.