Assessment of the cytotoxicity and genotoxicity properties of Uvaria chamae P. Beauv (Annonaceae) and Morinda lucida Benth (Rubiaceae) in mice

The toxicity profile of medicinal plants is an important preclinical requirement in the development of phytomedicines. The cytotoxic and genotoxic effects of the leaf of Uvaria chamae P. Beauv (Annonaceae) and stem bark of Morinda lucida Benth (Rubiaceae) were investigated in order to provide information on their safety as antimalarial plants. The methanol extract of U. chamae and ethanol (70%) extract of M. lucida were separately orally administered (125, 250, and 750?mg/kg/day) to mice for 10 consecutive days. Cyclophosphamide (50?mg/kg, single dose) and distilled water were used as positive and negative controls, respectively. The mice were injected with colchicine (0.04%) intra-peritoneally 24?h after the last administration of the extracts and the bone marrows harvested. Giemsa-stained slides of bone marrow cells were microscopically assessed for dividing cells to determine the mitotic index (MI) and scored for chromosomal aberrations (CA) according to standard methods. chamae exhibited dose-dependent cytotoxicity. At 750?mg/kg, the MI was significantly (p?M. lucida was not significantly different (p?>?0.05) from that of the negative control. The total CA observed from treatment with both plants at all doses were significantly (p?U. chamae showed both cytotoxicity and genotoxicity while M. lucida exerted only genotoxic effect. Nevertheless, the two plants should be used with caution in antimalarial therapy.     

紫玉盘茎的化学成分

目的：研究紫玉盘茎枝的化学成分。方法：采用95%乙醇渗漉提取,硅胶柱,Sephadex LH-20柱和反相硅胶柱层析分离纯化,根据理化性质和波谱学方法进行结构鉴定。结果：从该植物中分离鉴定了6个化合物,分别为：clemochinenosideB（1）,（＋）-异落叶松树脂醇3α-O-β-D-葡萄糖苷（2）,grandiuvarinC（3）,uvamalolG（4）,因特洛卡内酰胺-I（5）,胡椒内酰胺D（6）。结论：化合物1和2为首次从番荔枝科植物中分离得到,化合物1～6均为首次从该植物中分离得到。     

大花紫玉盘中的新抗肿瘤活性番荔枝内酯及其绝对构型研究

从番荔枝科紫玉盘属植物大花紫玉盘(Uvaria grandiflora Roxb.)根茎中分得两种新的抗肿瘤活性番荔枝内酯(1和3),用X-ray衍射分析和Mosher方法对1的绝对构型进行了研究,全部6个手性碳的构型分别是15S,17R,18R,21R,22R,36S。命名为大花紫玉盘素(uvarigrin)。用Mosher方法对3的绝对构型也进行了测定,命名为大花紫玉盘素A(uvarigrandin A)。对以前得到的大花紫玉盘脂素(uvarigranin,2)的相对构型进行了修正。     

大花紫玉盘中新多氧取代环己烯类的结构鉴定

从番荔枝科紫玉盘属植物大花紫玉盘( Uvaria grandiflora Roxb.)根茎中分得4种新的多氧取代环己烯及已知化合物zeylenol,应用波谱分析、X-射线衍射、园二色谱和 Mosher 酯制备等手段确定了全部新化合物的结构及其绝对构型,分别命名为大花紫玉盘醇A(1),B(2),E(3)和F(4)。     

Zeylenone抑制人前列腺癌PC-3细胞增殖及诱导凋亡作用研究

目的研究(4R,5S,6S)-4-苯甲酰氧基-6-[(苯甲酰氧基)甲基]-5,6-二羟基-2-环己烯-1-酮Zeylenone(Zey)对人前列腺癌PC-3细胞的生长抑制和诱导凋亡作用。方法采用MTT法观察Zey对PC-3细胞和正常前列腺基质细胞WPMY-1的增殖抑制作用,应用平板克隆形成实验观察Zey对PC-3细胞克隆形成的作用,AO/EB荧光染色观察细胞形态、JC-1染色观察Zey对细胞内线粒体膜电位的影响,An-nexin V-FITC/PI双染检测凋亡细胞比率,Western blot检测凋亡相关蛋白Caspase-9、Caspase-8、Caspase-3、Caspase-7和PARP的激活及Bcl-2、Bax、Bid、Bcl-xL蛋白的表达。结果Zey可以明显抑制人前列腺癌PC-3细胞的增殖并诱导其凋亡,而对正常前列腺基质细胞WPMY-1的抑制作用显著低于PC-3细胞。Zey抑制PC-3细胞克隆形成并明显诱导其凋亡。线粒体膜电位检测结果显示Zey导致细胞内线粒体膜电位的明显降低,Western blot检测结果表明Caspase-8、Caspase-9、Caspase-7、Caspase-3被激活,PARP和Bid被剪切活化,Bcl-2、Bcl-xL表达下降,而Bax表达上调。结论 Zey可选择性抑制人非激素依赖性前列腺癌PC-3细胞的增殖并诱导其凋亡,作用机制与其对Bcl-2和Caspase家族蛋白的影响,从而诱导PC-3细胞发生内源性和外源性凋亡相关。Zey有望成为治疗前列腺癌的候选药物。     

Antihepatotoxic and Trypanocidal Effects of the Root Bark Extract of Uvaria chamae

Antihepatotoxic and trypanocidal activities of a root bark extract derived from Uvaria chamae were tested in vivo and in vitro. The plant material was defatted with n -hexane and extracted with 70% ethanol. The ethanol extract was recovered in a 6.13% w/w yield. The LD 50 of the ethanol extract in mice at 24 hr was 166 mg/kg (i.p.). Intraperitoneal injection of the ethanol extract into mice showed no significant effect on pentobarbitone-induced hypnosis. Pentobarbitone-induced sleep in CCl 4 -poisoned rats was significantly reduced (p<0.005) by oral administration of the extract (60 mg/kg). The elevation of serum GOT, GPT, alkaline phosphatase and urea induced by CCl 4 intoxication in rats was also significantly reduced (p<0.005) by the ethanol extract. Uvaria chamae ethanol extract showed a significant (p<0.005) trypanocidal effect which was comparable to that of diminazine aceturate (r= 0.89). Reduction of existing parasitaemia in mice experimentally infected with Trypanasoma brucei brucei was dose-dependent.     

A new cerebroside from Uvaria tonkinensis var. subglabra

A new cerebroside, subglain A (1), together with five known compounds (2–6) have been isolated from the stems of Uvaria tonkinensis var. subglabra. The structure of 1 has been determined to be 1-O-β-D-glucopyranosyl-(2S,3S,4R,8Z,2′R)-2-[N-(2′-hydroxytetracosanyl)-N-(1″,2″-dihydroxyethyl)-amide]-8-tetradecene-1,3,4-triol by spectroscopic evidence. The known compounds were identified as schisandriside (2), erythritol (3), β-D-glucopyranose (4), kaempferol-3,7-O-α-L-dirhamnoside (5), and (+)-lyoniresinol (6).     

Two new polyoxygenated cyclohexenes from Uvaria kweichowensis

Two new polyoxygenated cyclohexenes, kweichowenols C and D, were isolated from the leaves of Uvaria kweichowensis, and their structures were established on the basis of their spectral data. The two new compounds showed some antitumor activity by the MTT assay.     

Four new compounds from the roots of Uvaria macrophylla

Four new compounds, uvamalols A–C (1–3) and uvarimacrophin A (4), have been isolated from the roots of Uvaria macrophylla. Their structures have been elucidated by spectroscopic methods. The relative configurations of uvamalols A–C have been established by NOE experiments, and the relative stereochemistry of uvarimacrophin A inferred from the diagnostic NMR data by comparison with known model compounds.     

大花紫玉盘的化学成分

通过正相硅胶、反相硅胶、大孔吸附树脂、Sephadex LH-20和高效液相色谱等多种现代色谱技术对番荔枝科紫玉盘属植物大花紫玉盘(Uvaria grandiflora)干燥根的化学成分进行系统地分离纯化,得到12个化合物,用现代波谱技术确定化合物的结构分别为:epicatechin-(4β→1′,2→O→2′)-phloroglucinol(1),proanthocyanidin A-1(2),proanthocyanidin A-2(3),表儿茶素(epicatechin)(4),phlorizin(5),圣草酚(eriodictyol)(6),erythro-guaiacylglycerol-8-O-4′-(coniferyl alcohol)ether(7),threo-guaiacylglycerol-8-O-4′-(coniferyl alcohol)ether(8),erythro-guaiacylglycerol-8-O-4′-(sinapyl alcohol)ether(9),threo-syringylglycerol-8-O-4′-(sinapyl alcohol)ether(10),burselignan(11),icariol A₂(12)。化合物1~12均为首次从该植物中分离得到,其中化合物1为新天然化合物。