Antinociceptive activity of steroid alkaloids isolated from Solanum trilobatum Linn.

Solasodine (1) was isolated for the first time from the roots of Solanum trilobatum Linn., a member of the Solanaceae, and assessed for its presumed antinociceptive activity using several experimental murine models, viz. the writhing, formalin, and hot plate tests. When used at doses of 2, 4, and 8 mg/kg, this steroidal alkaloid caused a significant and dose-dependent decrease in the nociception induced by an intraperitoneal injection of acetic acid (p < 0.001). It also led to a significant reduction of the painful sensation caused by formalin in both phases of the formalin test (p < 0.001). Furthermore, the alkaloid produced a significant increase in the reaction time in the hot plate test (p < 0.001). These results suggest that solasodine elicited antinociceptive activity through both central and peripheral mechanisms.     

Antitumor effects of total alkaloids isolated from Solanum nigrum in vitro and in vivo

This study demonstrated that the total alkaloids isolated from the traditional Chinese medicinal herb Solanum nigrum Linne (SNL-A) inhibited the growth of human cervical cancer HeLa cells in culture medium with much lower toxicity to human normal lymphocytes. By means of HE staining and TUNEL assay, our results further revealed that SNL-A induced cell death by apoptosis. An immunohistochemical assay showed down-regulation of the bcl-2 and p53 genes and no obvious change of bax gene in the SNL-A treated cells. Subcutaneous injection of HeLa cells induced tumor formation in nude mice, and SNL-A showed a significant inhibitory effect on tumor formation. These results suggested that SNL-A may be a potential, natural apoptosis-inducing agent for cervical cancer.     

酶法提取白英中总生物碱的工艺研究

目的研究纤维素酶在提取白英总生物碱中的应用。方法白英药材经纤维素酶处理后用乙醇回流提取总生物碱,通过正交实验优化酶处理工艺参数。结果酶解反应的最佳工艺条件为:温度50℃,酶反应时间3h,pH 4.5,酶质量浓度为1.6mg.mL-1,且酶法提取率为传统提取法的5倍。结论纤维素酶水解法适用于白英总生物碱的辅助提取。     

Biological activities of steroidal alkaloids isolated from Solanum leucocarpum

The alkaloids demissidine, dihydrosolacongestidine, solasodine and tomatidine were isolated and identified by spectroscopic methods and by comparison with literature data, from the aerial part of Solanum leucocarpum Dunal (Solanaceae) collected at the Regional Natural Park Ucumarí (Colombia). In order to examine topoisomerase I and II activities, the four isolated alkaloids were tested through a mechanism-based bioassay utilizing genetically engineered mutants of yeast Saccharomyces cerevisiae strains RS322N, R52Y and RS321. Dihydrosolacongestidine showed selective activity towards RS321 (249.8 μg/mL) strain rather than RS322N (1542.7 μg/mL), most probably indicating activity through inhibition of DNA topoisomerase II. In the same manner, tomatidine displayed activity through DNA topoisomerase II inhibition. Furthermore, solasodine showed DNA-damaging activity. In addition, the same isolated alkaloids were tested for antibacterial activity by using the agar well diffusion method. Solasodine and dihydrosolacongestidine showed MIC values of 62.5 and 125 μg/mL against Staphylococcus aureus, respectively. The isolation of these alkaloids and their biological activities are reported here for the first time for S. leucocarpum.     

镰形棘豆总生物碱抗肿瘤活性部位的体外筛选

目的 筛选出镰形棘豆总生物碱抗肿瘤的主要活性部位.方法 将镰形棘豆生物碱粗提部位经萃取后按照极性大小分为二氯甲烷部位、乙酸乙酯部位和正丁醇部位,采用四甲基偶氮唑盐(MTT)法观察各部位对人肝癌细胞SMMC-7721、人肺癌细胞A549、人胃癌细胞MKN-45、人结肠癌细胞LOVO、人宫颈癌细胞HeLa以及人乳腺癌细胞MDA-MB-231等6种人癌细胞株增殖的影响.结果 总生物碱的正丁醇部位几乎没有抑制细胞增殖的作用,乙酸乙酯部位抑制作用比较弱,而二氯甲烷部位显示有较明显地抑制肿瘤细胞增殖的活性,且对6种细胞都有效.此外,不同的肿瘤细胞株对同一药物的敏感性也各不相同,人肺癌细胞A549和人乳腺癌细胞MDA-MB-231对药物有较高的敏感性.结论 镰形棘豆抗肿瘤的活性部位为总生物碱的二氯甲烷部位.     

白英中总生物碱的含量测定

目的建立白英中总生物碱的含量测定方法。方法用酸性染料比色法测定白英中总生物碱的含量,以士的宁为对照,0.001mol·L-1的溴麝香草酚蓝为酸性染料,在pH4.0缓冲液中用三氯甲烷萃取,再用0.01mol·L-1KOH的乙醇液碱化,在600nm处测定吸光度值。结果士的宁在10.20～35.70mg·mL-1范围内与吸光度值呈良好线性关系(r=0.9998),方法的平均回收率为99.3%(n=9),RSD为1.3%。结论该方法操作简便、准确、灵敏、重现性好,可用于白英药材的质量控制。     

秦岭产4种乌头地上部分生物碱含量测定

目的测定秦岭产乌头属的松潘乌头、太白乌头、甘青乌头、铁棒锤地上部分总生物碱的含量,探讨种的化学资源分布,为该属资源有效利用研究提供依据。方法酸性染料比色法测定乌头属地上部分总生物碱。结果4种乌头地上部分的总生物碱为:花期-松潘乌头0.12%、太白乌头1.34%、甘青乌头0.54%、铁棒锤1.54%;果期-松潘乌头0.10%、太白乌头1.13%、甘青乌头0.60%、铁棒锤1.38%。结论花期太白乌头、甘青乌头及铁棒锤总生物碱含量较高,有一定的资源利用价值。     

白英总皂苷的抗炎活性研究

目的:观察白英总皂苷的抗炎活性。方法:培养人脐静脉内皮细胞(HUVEC),用200 μmol·L^-1H₂O₂损伤细胞;培养小鼠单核/巨噬细胞(RAW 264.7),用脂多糖(LPS)诱导;抽签法随机分成正常组、模型组、阳性对照组、白英总皂苷低、中、高剂量组。给药后,继续培养,应用CCK-8法观察细胞存活率;饲养SD大鼠,抽签法随机分为正常组、模型组、阳性对照组、白英总皂苷低、中、高剂量组,观察白英总皂苷对角叉菜胶诱导大鼠急性踝关节肿胀度的影响,测定前列腺素E₂(PGE₂)、环氧化物水解酶-2(COX-2)含量。结果:白英总皂苷中剂量对H₂O₂损伤的HUVEC细胞的影响以及高剂量组对LPS诱导的巨噬细胞RAW 264.7的影响,均和阳性对照组相当,无统计学差异(P>0.05);中、高剂量白英总皂苷能够明显降低大鼠急性踝关节肿胀度,降低大鼠足趾渗出液中PGE₂、血清中COX-2含量,且和模型组差别有统计学意义(P<0.01)。结论:白英总皂苷具有明显的抗炎作用,有必要进一步深入研究其药效及作用机制。     

Hepatoprotective Effect of the Total Alkaloid Fraction of Solanum pseudocapsicum Leaves

The total alkaloid fraction of the methanol extract of leaves of Solanum pseudocapsicum was tested for its hepatoprotective activity against CCl 4 induced toxicity in freshly isolated rat hepatocytes, HepG2 cells and animal models. The total alkaloid fraction was able to normalise the levels of aspartate amino transferase (ASAT), alanine aminotransferase (ALAT), alkaline phosphatase (ALP), triglycerides (TGL), total proteins, albumin, total bilirubin and direct bilirubin, which were altered due to CCl 4 intoxication in freshly isolated rat hepatocytes and also in animal models. The antihepatotoxic effect of the total alkaloid fraction was observed at very low concentrations (6–10µg/ml) and was found to be superior to that of the standard used. A dose dependent increase in the percentage viability was observed when CCl 4 exposed HepG2 cells were treated with different concentrations of the total alkaloid fraction. The highest percentage viability of HepG2 was observed at a concentration of 10µg/ml. Its in vivo hepatoprotective effect at 20 mg/kg body weight was comparable with that of the standard at 250mg/kg body weight. The total alkaloid fraction merits further investigation to identify the active principles responsible for the hepatoprotective properties. The results from the present investigation also indicate well correlation between the in vivo and in vitro studies.     

楮实子总生物碱抗肿瘤作用初步研究

目的研究楮实子总生物碱的抗肿瘤作用。方法建立小鼠H22,S180,ESC肿瘤模型,从整体水平上观察楮实子总生物碱对肿瘤生长的影响。结果60 mg/kg楮实子总生物碱对3种肿瘤小鼠的抑瘤率均在40%以上。结论楮实子总生物碱有一定的抗肿瘤活性。     

Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, alpha-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, including previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.     

Anti-herpes simplex virus activity of alkaloids isolated from Stephania cepharantha

By screening water and MeOH extracts of 30 Chinese medicinal plants for their anti-herpes simplex virus (HSV)-1 activity, a MeOH extract of the root tubers of Stephania cepharantha HAYATA showed the most potent activity on the plaque reduction assay with an IC50 value of 18.0 microg/ml. Of 49 alkaloids isolated from the MeOH extract, 17 alkaloids were found to be active against HSV-1, including 13 bisbenzylisoquinoline, 1 protoberberine, 2 morphinane and 1 proaporphine alkaloids, while benzylisoquinoline and hasubanane alkaloids were inactive. Although N-methylcrotsparine was active against HSV-1, as well as HSV-1 thymidine kinase deficient (acyclovir resistant type, HSV-1 TK-) and HSV-2 (IC50 values of 8.3, 7.7 and 6.7 microg/ml, respectively), it was cytotoxic. FK-3000 was found to be the most active against HSV-1, HSV-1 TK- and HSV-2 (IC50 values of 7.8, 9.9 and 8.7 microg/ml) with in vitro therapeutic indices of 90, 71 and 81, respectively. FK-3000 was found to be a promising candidate as an anti-HSV agent against HSV-1, acyclovir (ACV) resistant-type HSV-1 and HSV-2.     

不同产地楮实子生物碱含量比较

目的对不同产地的楮实子生物碱含量进行比较研究。方法采用酸性醇回流法提取了楮实中的总生物碱,依照酸性染料比色法的原理,在410 nm波长下测定生物碱的含量。结果取得良好的线性关系（r=0.999 5）和回收率（98.52%）,RSD为0.91%。不同产地的楮实子药材中所含生物碱的含量为7.98 mg/g至23.53 mg/g不等。结论楮实子生物碱含量显示出明显的地域性差异。     

Anticonvulsant activity of solasodine isolated from Solanum sisymbriifolium fruits in rodents

Context: Solanum sisymbriifolium Lam. (Solanaceae), commonly known as sticky nightshade, is traditionally used for central nervous system (CNS) disorders. Although solasodine has been isolated from this plant, little is known about its anticonvulsant and CNS depressant actions.

Objective: We investigated anticonvulsant and CNS depressant effects of solasodine isolated from S. sisymbriifolium using several experimental models.

Materials and methods: Swiss albino mice (n?=?6) were employed for pentylenetetrazole (PTZ) and picrotoxin (PCT)-induced convulsions and thiopental-induced sleep time. Different groups of Wistar albino rats (n?=?6) were subjected to maximal electroshock (MES) test. Solasodine, a steroidal glycoalkaloid, was isolated from dried fruits of S. sisymbriifolium and identified by GC-MS.

Results: The results showed that intraperitoneal (i.p.) injection of solasodine (25?mg/kg) significantly delayed (p < 0.01) latency of hind limb tonic extensor (HLTE) phase in the PCT-induced convulsions. In the MES model, solasodine significantly reduced (p < 0.001) duration of HLTE at 25, 50, and 100?mg/kg, i.p. in a dose-dependent manner. Interestingly, solasodine did not produce any significant reduction in PTZ-induced convulsions. Prior treatment of solasodine (25, 50, and 100?mg/kg, i.p.) significantly potentiated thiopental-provoked sleep in a dose-dependent manner (p < 0.001).

Discussion and conclusion: Our study, for the first time, shows potent anticonvulsant and CNS depressant activities of solasodine. It is likely that solasodine, in part, is responsible for the anticonvulsant and sedative properties of S. sisymbriifolium. The future study should focus on the exact mechanism of action of solasodine.     

Phytochemical study and cytotoxic activity of alkaloids from Uvaria chamae P. Beauv

Phytochemical study of leaves of Uvaria chamae resulted in the isolation for the first time for the genus Uvaria of benzylisoquinoline alkaloids (+)-armepavine (1) and racem. O,O-dimethylcoclaurine (2). The aporphines nornantenine (3), nantenine (4) and corydine (7) are new for the species. The alkaloids were found to express cytotoxic activity against L 929 transformed cells. The highest activity was shown by 1, 3, and 5. At a concentration corresponding to their IC50 against L929 cells, they were nontoxic against mouse thymocytes.     

Cytotoxic isoquinoline alkaloids from the aerial parts ofCorydalis incisa

Three known isoquinoline alkaloids were isolated from the chloroform-soluble fraction of the methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) through repeated column chromatography. Their chemical structures were elucidated as corynoline (1), corynoloxine (2) and 6-oxocorynoline (3) using spectroscopic analysis. Compounds 1-3 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2 and HCT15 tumor cells.