Diterpenes and their derivatives as promising agents against dengue virus and dengue vectors: A literature‐based review

Dengue, a mosquito‐borne viral disease, causes about 100 million cases of infection annually. It is a major public concern, and if left untreated or improperly diagnosed, may cause serious health problems or even death. Historically, dengue has not considered priorities for pharmaceutical companies made the available treatment options. Therefore, medicinal scientists are revealing new insights and enabling novel interventions and approaches to dengue prevention and control. Diterpenes, a class of terpenes have gained much attention due to their diverse biological effects. This review aimed at summarizing available evidences of diterpenes and their derivatives acting against dengue virus and their vectors. For this, an updated search was made in the databases: PubMed and ScienceDirect by using specific keywords. Among the 117 published reports, a total of 30 articles was included in this review. Findings suggest that a number of diterpenes and/or their derivatives act against dengue virus and their two potential vectors namely Aedes aegypti and Ae. albopictus. In conclusion, diterpenes and their derivatives may have the potential alternative therapeutic tools for the management of dengue virus and some associated diseases transmitted by Aedes mosquito.     

中药豨莶草的化学成分及其药理作用研究进展

目的探讨菊科植物豨莶草化学成分及其近年来药理作用研究进展。方法检索、整理、归纳国内外有关豨莶草化学成分及其药理作用研究文献。结果与结论豨莶草主要含有二萜类、倍半萜类、黄酮类等化学成分,豨莶草提取物及化学成分具有抗炎镇痛、抗过敏、心血管保护等生物活性。     

Novel Taxane Diterpenoids from Taiwanese Yew Trees

Recent discovery of new and bioactive taxane diterpenoids from the roots, barks, seeds, leaves and the stems of Taxus mairei and T. sumatrana, Taiwanese yew trees are described. More than thirty new compounds including taxumatrols A and B (36, 37) have been isolated and their structures determined by spectroscopic analysis and chemical derivatization and correlation. Some of the isolated taxoids exhibited potent cytotoxicity against human tumor cells.     

Daphne-type diterpenes from genus Daphne and their anti-tumor activity

Daphne-type diterpenenoids is the major biologically active constituents in the genus Daphne. We find that there are about 101 Daphne-type diterpenes in this genus, most of these compounds show different degrees of inhibitory effect on various cancer cell. Some of them have been studied in depth and the potent molecular mechanisms might be associated with modulation of different cell-signaling pathways. In addition, some compounds of this type also can inhibit the synthesis of protein and DNA. Absolutely, the anti-tumor activity of Daphne-type diterpenes is worthy of attention. Unfortunately, most of the current research on the activity of these compounds is focused on simple drug efficacy, and its in-depth mechanism research is far from enough. On the other point of view, there still exists wide growing space on the depth of these compounds.     

剑叶凤尾蕨化学成分及其细胞毒活性研究

采用95%乙醇提取药材,提取液回收至无醇味后依次过聚酰胺树脂、MCI树脂、中压制备液相色谱和制备型高效液相色谱,从剑叶凤尾蕨全草中分离得到8个二萜类化合物和2个倍半萜类化合物。质谱(ESI-MS)数据和核磁共振(NMR)数据与文献数据对比鉴定分离得到的化合物分别为ent-3β-hydroxy-kaur-16-en-19-al(1),4-epi-kaurenic acid(2),mitrekaurenone(3),7β,16α,17-trihydroxy-ent-kauran-19-oic acid(4),crotonkinin E(5),crotonkinin F(6),pterisolic acid A(7),pterisolic acid C(8),(2R)-pterosin P(9)和dehydropterosin B(10)。化合物1~6首次从凤尾蕨属中分离得到,化合物7~10首次从剑叶凤尾蕨中获得。细胞毒活性测试表明化合物5~8具有一定的抑制人结肠癌细胞HCT-116、肝癌细胞Hep G2和人胃癌细胞BGC-823的活性。     

Diterpenes and Their Derivatives as Potential Anticancer Agents

As therapeutic tools, diterpenes and their derivatives have gained much attention of the medicinal scientists nowadays. It is due to their pledging and important biological activities. This review congregates the anticancer diterpenes. For this, a search was made with selected keywords in PubMed, Science Direct, Web of Science, Scopus, The American Chemical Society and miscellaneous databases from January 2012 to January 2017 for the published articles. A total 28, 789 published articles were seen. Among them, 240 were included in this study. More than 250 important anticancer diterpenes and their derivatives were seen in the databases, acting in the different pathways. Some of them are already under clinical trials, while others are in the nonclinical and/or pre‐clinical trials. In conclusion, diterpenes may be one of the lead molecules in the treatment of cancer. Copyright © 2017 John Wiley & Sons, Ltd.     

中国红树科植物角果木中Dolabrane型二萜的抗肿瘤作用

目的 探讨中国红树植物角果木中Dolabrane型二萜Tagalsins A的抗肿瘤作用及其初步作用机制.方法 建立小鼠H22肝癌实体瘤及H22肝癌腹水瘤模型,随机分为Tagalsins A高、中、低剂量组(20、10、5 mg·kg-1)、生理盐水组(空白对照)、环磷酰胺组(CTX 10 mg·kg-1),每组小鼠各10只.建模24 h后开始给药,Tagalsins A各剂量组给予Tagalsins A连续灌胃7 d,对照组灌胃给予同体积生理盐水,CTX组连续腹腔给予CTX 7 d.末次给药24 h后处死动物,计算抑瘤率、生命延长率、脏器指数;流式细胞术测细胞凋亡率.结果 Tagalsins A各剂量组小鼠H22实体瘤生长较空白对照组明显减慢(F=8.90,q=3.31～6.52,P＜0.01).Tagalsins A低、中、高剂量组的抑瘤率分别为24.49%、35.37%、48.30%,其中Tagalsins A中、高剂量组抑瘤作用与CTX组比较差异无显著性(q=2.85、1.01,P＞0.05).Tagalsins A明显延长H22腹水瘤小鼠生存时间(F=17.06,q=5.45～11.26,P＜0.01);降低小鼠的胸腺指数(F=21.82,P＜0.01),而升高肝脏指数(F=121.84,P＜0.01).Tagalsins A各组肿瘤细胞的凋亡率较空白对照组明显升高(F=127 7.68,q=51.11～82.02,P＜0.01).结论 Dolabrane型二萜Tagalsins A对小鼠H22移植瘤的生长具有明显的抑制作用,其机制可能与诱导细胞凋亡有关.     

光叶巴豆根的化学成分研究

目的 研究光叶巴豆根的化学成分.方法 利用溶剂法及多种色谱技术进行化学成分的分离纯化,并运用现代波谱技术及理化性质鉴定化合物结构.结果 从光叶巴豆根部的95％乙醇提取物中分离得到7个化合物,分别鉴定为levatin(Ⅰ),croverin(Ⅱ),crovatin(Ⅲ),sonderianial(Ⅳ),棕榈酸(palmitic acid,Ⅴ),反式肉桂酸(cinnamic acid,Ⅵ),苯甲酸(benzoic acid,Ⅶ).结论以上化合物均是首次从该植物中分离得到.     

迷迭香总二萜酚的体内抗氧化作用研究

目的：探讨迷迭香提取物的体内抗氧化作用及其物质基础。方法：通过建立小鼠运动性氧化损伤模型，测定并比较给药组（迷迭香总二萜酚组）与对照组的血清、心、肝、脑及股四头肌等组织内的丙二醛（MDA）含量和超氧化物歧化酶（SOD）、谷胱甘肽过氧化物酶（GSH-Px）的活性。结果：给予迷迭香总二萜酚提取物的中、高剂量（分别为250和500mg/kg体重）组的小鼠除脑外其他各组织内的MDA含量都有明显降低，SOD和GSH-Px活性都有明显升高。结论：迷迭香提取物具有较好的体内抗氧化作用，其中的二萜酚类化合物可能是其抗氧化作用的物质基础。     

雷公藤研究进展及其质量标志物的预测分析

雷公藤是一味传统中药,所含化学成分丰富,具有多方面的药理活性。在刘昌孝院士提出中药质量标志物(Q-marker)新概念的基础上,系统综述了雷公藤化学成分及药理活性,并根据质量标志物的定义结合雷公藤的传统药效、传统药性、临床用药新用途、可测成分、入血成分和配伍研究进行分析,对雷公藤质量标志物进行预测,以期为雷公藤药材质量的深入研究提供参考。