In vivo Antimalarial Activity of a Labdane Diterpenoid from the Leaves of Otostegia integrifolia Benth

In Ethiopian traditional medicine, the leaves of Otostegia integrifolia Benth. are used for the treatment of several diseases including malaria. In an ongoing search for effective, safe and cheap antimalarial agents from plants, the 80% methanol leaf extract O. integrifolia was tested for its in vivo antimalarial activity, in a 4‐day suppressive assay against Plasmodium berghei. Activity‐guided fractionation of this extract which showed potent antiplasmodial activity resulted in the isolation of a labdane diterpenoid identified as otostegindiol. Otostegindiol displayed a significant (P < 0.001) antimalarial activity at doses of 25, 50 and 100 mg/kg with chemosuppression values of 50.13, 65.58 and 73.16%, respectively. Acute toxicity studies revealed that the crude extract possesses no toxicity in mice up to a maximum dose of 5000 mg/kg suggesting the relative safety of the plant when administered orally. The results of the present study indicate that otostegindiol is among the antimalarial principles in this medicinal plant, and further support claims for the traditional medicinal use of the plant for the treatment of malaria. Copyright © 2013 John Wiley & Sons, Ltd.     

附子的化学成分研究

目的:研究附子的化学成分.方法:通过反复硅胶柱色谱和重结晶的方法分离纯化,根据化合物的理化性质和波谱数据鉴定结构.结果:分离得到9个化合物,分别为美沙乌头碱(1)、海帕乌头碱(2)、宋果灵(3)、去氢松果灵(4)、一枝蒿乙素(5)、penduline(6)、β-谷甾醇(7)、胡萝卜苷(8)、单棕榈酸甘油酯(9).结论:化合物5,6,8,9为首次从该植物中分离得到.     

附子的化学成分研究

目的研究毛茛科植物乌头的子根附子的化学成分,为附子的进一步研究提供物质基础。方法以90%乙醇回流提取,采用硅胶、凝胶柱色谱等多种柱色谱技术以及重结晶等方法进行分离,并根据理化性质和波谱数据进行结构鉴定。结果共分离鉴定了6个二萜类生物碱,分别为乌头碱(1),新乌头碱(2),尼奥林(3),附子宁(4),宋果灵(5)和欧乌头碱(6)。结论化合物6为首次从附子中分得。     

HPLC法测定附子与其炮制品中双酯型生物碱

目的 通过测定附子及熟附片(干片蒸制)、黑顺片、熟附片(鲜片蒸制)、盐附子、炮附片中次乌头碱、乌头碱、新乌头碱的量,揭示炮制减毒的科学内涵.方法 样品采用10％氨水浸润,乙醚超声提取的方法;色谱柱为Agilent Zorbax SB-C18柱(4.6 mm× 150 mm,5μm);流动相为乙腈-0.2％冰醋酸(浓氨水调节pH为7.29)(28∶72);检测波长235 nm;结果与生附子相比,次乌头碱、乌头碱、新乌头碱在清水黑顺片、盐附子等炮制品中的量大大降低;结论本实验从化学的角度阐释了附子炮制减毒的科学依据.     

Combined analysis of transcriptomics and metabolomics revealed complex metabolic genes for diterpenoids biosynthesis in different organs of Anoectochilus roxburghiiOA

Objective: Diterpenoids with a wide variety of biological activities from Anoectochilus roxburghii, a precious medicinal plant, are important active components. However, due to the lack of genetic information on the metabolic process of diterpenoids in A. roxburghii, the genes involved in the molecular regulation mechanism of diterpenoid metabolism are still unclear. This study revealed the complex metabolic genes for diterpenoids biosynthesis in different organs of A. roxburghii by combining an...     

附子C_(19)二萜生物碱结构及活性研究进展

附子为常用中药,具有回阳救逆、散寒止痛、温阳化气的功效。C_(19)二萜生物碱是其主要生物碱类成分,可分为双酯型、单酯型和胺醇型,其在发挥抗炎、镇痛、抗肿瘤等药效同时,也可导致心脏毒性和神经毒性。对附子C_(19)二萜生物碱化学结构、药理及毒理作用进行系统梳理,以期为临床更安全、有效地使用附子提供理论依据。     

Cytotoxic,apoptotic, and sensitization properties of ent‐kaurane‐type diterpenoids from Croton tonkinensis Gagnep on human liver cancer HepG2 and Hep3b cell lines

Human hepatocellular carcinoma (HCC) is the most common type of liver cancer, the second most common cause of death from cancer worldwide. A very poor prognosis and a lack of effective treatments make liver cancer a major public health problem, notably in less developed regions, particularly in eastern Asia. This fully justifies the search of new molecules and therapeutic strategies against HCC. Ent‐kaurane diterpenoids are natural compounds displaying a broad spectrum of potential therapeutic effects including anticancer activity. In this study, we analyzed the pharmacological properties of a family of ent‐kaurane diterpenoids from Croton tonkinensis Gagnep in human HepG2 and Hep3b cell lines, used as cellular reference models for in vitro evaluation of new molecules active on HCC. A structure‐related cytotoxicity was observed against both HCC cell lines, enlighting the role of the 16‐en‐15‐one skeleton of ent‐kaurane diterpenoids. Cytotoxicity was closely correlated to apoptosis, evidenced by concentration‐dependent subG1 cell accumulation, and increased annexin V expression. In addition, subtoxic concentration of ent‐kaurane diterpenoid dramatically enhanced the sensitivity of HCC cells to doxorubicin. All together, our data bring strong support to the potential interest of ent‐kaurane diterpenoids, alone or in combination with a cytotoxic agent, in cancer and more precisely against HCC.     

雷公藤二萜成分研究

自福建产雷公藤的根皮部分离获得六个二萜成分(D_1～D_6)。又自湖北产雷公藤的根部得三个二萜成分(D_3、D_5和D_6)。根据其波谱数据和其他理化性质证明:D_1为雷公藤内酯酮,D_2为雷公藤内酯醇,D_3为雷酚内酯,D_4为雷酚酮内酯。D_5和D_6为两个新成分,其结构分别定为:-14-羟基-松香-8,11,13-三烯-3-酮和11-羟基,14-甲氧基-松香-8,11,13-三烯-3-酮。免疫学实验表明,以上二萜成分中D_1和D_2对由ConA引起的淋巴细胞增生有显著的抑制作用。     

鄂贝缩醛A的结构解析与合成

目的：研究民间药鄂北贝母Fritillaria ebeiensis G.D.Yu et G.Q.Ji鳞茎的非生物碱成分。方法：用MeOH提取,反复硅胶柱色谱分离与纯化,经理化常数测定、波谱解析、化学合成及降解反应,确定其结构。结果：从乙酸乙酯萃取物中分离鉴定了1个二萜,其结构为ent-kauran-16β,17-acetal ent-16β-kauran-17(S)-aldehyde (1)。结论：化合物1为新的对映-贝壳杉烷型缩醛聚合二萜,命名为鄂贝缩醛A(fritillebinide A)。