抗辐射的天然药物研究进展

近年来,国际核危机形势严峻以及日常生活中人们长期遭受周围环境中低剂量辐射,使辐射防护药物的研究显得至关重要。而天然药物以及民族药物由于其资源丰富、疗效确切、副作用小等优点,越来越受到研究者的重视。本文就常见的具有抗辐射作用的天然药物及其活性成分,以及疗效确切的抗辐射民族药物研究进展作一综述。     

Antifibrinolytic and antimycotic properties of 2-thiontetrahydro-1,3,5-thiadiazine]

A series of tetrahydro-1,3,5-thiadiazine-2-thiones have been tested for their fungistatic and antifibrinolytic effects. The fungistatic activity depends upon the substitution of nitrogen in positions 3 and 5 of the ring system. But it is, however, only the derivatives that are able to split off the antifibrinolytically active w-amino acids by solvolysis which produces antifibrinolytic effect in vivo.     

Screening for natural medicines effective for the treatment of osteoporosis

Journal of Natural Medicines - Bone-forming osteoblasts are differentiated from mesenchymal stem cells and dysregulation of this differentiation can lead to osteoporosis. Meanwhile, bone-resorbing...     

Bilogical and toxicological properties of econazole, a broad-spectrum antimycotic.

The spectrum of activity of 1-(2,4-dichloro-beta-[(p-chlorobenzoyl)oxy]phenethyl)imidazole-nitrate (econazole, R 14827) was tested in vitro on various pathogenic fungi and bacteria, and also in vivo in guinea-pigs and rats experimentally infected with dermatophytes and C. albicans. The in vitro activity spectrum is very broad: the dermatophytes, the yeasts, the dimorphic fungi, the aspergilli, the mycetoma causing agents and the Gram-positive bacteria being most sensitive. Guinea-pigs infected with T. mentagrophytes, M. canis or C. albicans and treated topically or orally with econazole, were cured. In each of these tests the activity of econazole was compared with that of different reference drugs. Vaginal candidiasis in rats was cured after oral administration of econazole. Toxicity and teratogenicity studies in different laboratory animals indicate that econazole is well tolerated.     

液相色谱——质谱联用技术及其在天然药物分析中的应用

目的　介绍近年来液相色谱—质谱联用技术的研究进展及其在天然药物分析中的应用。方法　主要介绍液相色谱—质谱(LC -MS)接口技术中API技术的研究进展及液相色谱 -电喷雾离子化质谱(LC -ESI -MS)。液相色谱 -大气压化学离子化质谱(LC -APCI -MS)等技术在天然药物分析中的应用。结果及结论　液相色谱 -质谱在接口技术方面取得了很大进展,且随着该技术的不断完善液质联用技术在天然药物分析中占据越来越重要的地位     

Metabolic pathways and pharmacokinetics of natural medicines with low permeability

Drug metabolism plays an important role in the drug disposal process. Differences in pharmacokinetics among individuals are the basis for personalized medicine. Natural medicines, formed by long-term evolution of nature, prioritize the action of a target protein with a drug. Natural medicines are valued for structural diversity, low toxicity, low cost, and definite biological activities. Metabolic pathway and pharmacokinetic research of natural medicines is highly beneficial for clinical dose adjustment and the development of personalized medicine. This review was performed using a systematic search of all available literature. It provides an overview and discussion of metabolic pathways and the pharmacokinetics of natural medicines with low permeability. The related enzymes and factors affecting them are analyzed. The series of metabolic reactions, including phase I reactions(oxidation hydrolysis, and reduction reactions) and phase II reactions (binding reactions), catalyzed by intracellular metabolic enzymes (such as CYP450, esterase, SULT, and UGT enzymes) in tissues (such as liver and gastro-intestinal tract) or in the body fluid environment were examined. The administration route, drug dose, and delivery system had a large influence on absorption, metabolism, and pharmacokinetics. Natural medicines with low permeability had distinctive metabolisms and pharmacokinetics. The metabolic and in vivo kinetic properties were favorably modified by choosing suitable drug delivery systems, administration routes and drug doses, among other variables. This study provides valuable information for clinicians and pharmacists to guide patients safe, effective, and rational drug use. The research of metabolism and pharmacokinetics is significant in guiding personalized clinical medicine.     

中国海洋中药材品种调查

目的 掌握流通领域中海洋中药材的商品状况,为海洋中药材的开发利用和质量管理对策提供基础信息。方法 以国家级中药材市场(安国、亳州、清平、玉林)为主要基地,通过药市直接调查、走访药商、考察药材加工厂、文献与网络信息调研等途径,调查海洋中药材市场状况。结果 海洋中药材在中药材市场流通的品种有78种,其中常见品种50种,大宗品种18种;市场流通混乱,大多海洋中药材基原生物不清,销量和资源量也不清;替代品、混淆品、伪品以及掺假等普遍存在。结论 在中药材市场上,海洋中药材品种少,质量参差不齐,市场管理体系不健全,急需开发新药材品种,提升质量标准,建立规范的市场管理与运营机制。     

我国中药来源的抗HIV天然化合物研究进展

由于迄今仍无艾滋病 (acquired immunodeficiency syndrome, AIDS) 疫苗问世, 抗人类免疫缺陷病毒 (human immunodeficiency virus, HIV) 药物仍然是艾滋病治疗的主要手段。传统中药和药用植物来源的天然化合物具有结构多样性、毒性较低、来源广泛等特点, 因而在防治艾滋病方面有着独特的优势和巨大的潜力。研究者已经对天然化合物抗HIV作用进行了大量研究, 并取得了可喜的成绩, 发现了一些生物碱、香豆素、木脂素、黄酮类、萜类、鞣质类、多糖类、蛋白质和多肽类等天然化合物具有抗HIV的活性。然而, 多数研究都是在体外试验完成的, 大多数天然化合物体外抗HIV活性偏低, 而且抗HIV的靶点仍不十分清楚。本文结合笔者实验室研究工作, 重点介绍近年来我国传统中药来源的抗HIV活性较强的天然化合物研究进展。     

代谢组学在天然药物肝肾毒性评测中的应用

代谢组学是20世纪90年代中后期继基因组学、转录组学和蛋白质组学之后发展起来的一种新技术,它通过考察生物系统中所有代谢产物的动态变化,来研究生物系统的代谢途径,阐明代谢物与机体病理生理刺激及遗传因素改变的相互关系。本文在查阅文献的基础上,对近年来代谢组学在诸如雄黄、朱砂、关木通、广防己、附子、稀土元素等中药及天然药物对肝肾毒性评测中的应用进行了综述。     

抗心衰天然药物及活性化合物研究进展

心力衰竭(heart failure, HF)是世界性公众健康问题,全球心衰患者高达数千万人。其发病率每年递增,死亡率近年急剧上升,且有年轻化趋势,尽管近年来医学发展迅猛,但心衰的不良预后至今未得到有效改善。天然药物及其活性化合物具有温和低毒、多靶点综合疗效等特点,在恢复心脏功能、减轻能量障碍和提高生活质量等方面均具有明显优势。近年来在临床抗心衰应用中日益广泛,对天然药物及其活性化合物抗心衰机制进行深入研究,将为抗心力衰竭的临床治疗提供新的研究靶点和治疗方法。     

Simple tests demonstrating the antimycotic effect of chitosan

We show that under the conditions of a fungal growth test, 66% deacetylated krill chitosan did not affect pathogenic fungi which cause human mycosis. However, as demonstrated by our fungal cell adherence test, chitosan not only inhibited the adhesion of Candida albicans cells to human vaginal epithelial cells or to HeLa cells, but also acted non-specifically on fungal and epithelial cells. This explained our earlier observations of the enhancement of therapetic efficacy of anti-fungal formulations, to which chitosan had been added. We recommend the joint use of fungal growth and fungal cell adherence tests as a generally useful, economical and readily available method for assessing the activity of anti-fungal preparations.     

用固定化酶筛选模型从天然产物中筛选α-葡萄糖苷酶抑制剂

目的:用固定化酶筛选模型从天然产物中筛选α-葡萄糖苷酶抑制剂.方法:把α-葡萄糖苷酶固定化,模拟其在体内小肠壁上的情况,建立固定化酶筛选模型,先用α-葡萄糖苷酶抑制剂阿卡波糖对该模型进行验证,然后用该筛选模型对2种天然产物-虎杖水溶性部位和广西血竭甲醇溶液进行筛选.结果:阿卡波糖对固定化α-葡萄糖苷酶和游离α-葡萄糖苷酶的IC50分别为0.413 mg·mL-1和0.126 mg·mL,虽然固定化酶被阿卡波糖抑制的IC50值是游离酶的3.3倍,但固定化酶筛选模型更准确地反映阿卡波糖的体内作用.虎杖水溶性部位和广西血竭的甲醇溶液对固定化α-葡萄糖苷酶的IC50分别为0.224 mg·mL-1和5.5 μg·mL-1.结论:该筛选模型能很好的进行体外α-葡萄糖苷酶抑制剂的筛选,其筛选结果和文献报道相符.     

Drug metabolism and pharmacokinetics of nanodrugs from Chinese medicines and natural products

Over the past few years, nanoscale Chinese medicine has become one of focuses in modern Chinese medicine research. There is an increasing need for a more systematic study on the basic issues involved in traditional Chinese medicine and a more active participation of researchers in the application area of nanoscale traditional Chinese drugs. In this review, author analyzed the current applications of nanotechnology in research and development of drugs from natural products and herbal medicines involving traditional Chinese medicines, and also discussed the bio-medicinal evaluation issues on ADME including bio-distribution and metabolism of nanodrugs. Author noted that great challenges faced in nanodrugs from herb drugs and natural products are the follows: (1) the first challenge is to prepare nanodrug delivery system and quantitatively evaluate the therapeutic effects and safety; (2) the second challenge is to clarify the concrete metabolism course; and (3) the third challenge is to study the pharmacokinetics of nanodrugs.