Advances in the Study of Biotransformation of Ginsenoside by Microorganisms

研究表明人参稀有皂苷具有很强的生物活性,为获得稀有人参皂苷的各种研究越来越多,而生物转化法制备稀有人参皂苷已成为一条重要途径.本文对产稀有人参皂苷微生物转化的方法最新研究进展进行了简要的综述,并简要展望了人参皂苷生物转化研究的前景.     

人参皂苷生物转化的研究进展

目的综述人参皂苷在体内及体外的生物转化研究概况。方法查阅国内外相关文献,以其中的26篇文献为依据对人参皂苷在体内的转化途径及产物加以介绍,也对体外转化中使用的酶法和微生物法加以详细阐述。结果人参皂苷在体内被代谢成为多种稀有人参皂苷,它们是人参在体内发挥药理活性作用的物质。体外生物转化人参皂苷的方法较多,并取得了许多有意义的成果。结论为人参皂苷的代谢研究及稀有人参皂苷的体外生物转化制备提供了参考。     

真菌EST-Ⅰ及EST-Ⅱ对人参皂苷Rg_1定向转化为人参皂苷F_1的研究

目的筛选能将人参皂苷Rg1定向转化为稀有人参皂苷F1的真菌。方法通过硅胶柱色谱从三七总皂苷中分离纯化出人参单体皂苷Rg1;采用固体与液体发酵培养法,从325株真菌中筛选到能对单体人参皂苷Rg1进行生物转化的菌株。采用1H-NMR1、3C-NMR波谱手段及理化性质鉴定人参皂苷Rg1及其转化产物。结果发现真菌菌株EST-Ⅰ与EST-Ⅱ将人参皂苷Rg1定向转化为人参皂苷F1,说明两种菌株能产生特异性水解C-6位葡萄糖的β-葡萄糖苷酶。结论该方法是一种制备稀有人参皂苷F1的新方法。     

黑曲霉Aspergillus niger对人参皂苷Re的微生物转化

目的：筛选长白山人参土壤中的活性微生物,转化单体人参皂苷产生稀有人参皂苷成份。方法：从长白山人参根际土壤中分离各类菌株,对单体人参皂苷Re进行微生物转化,通过硅胶柱层析等方法对转化产物进行分离纯化,采用波谱解析及理化常数对其进行结构鉴定。结果：从长白山人参根际土壤中分离各类真菌菌株68株,3株真菌对三醇组人参皂苷Re具有转化作用,其中黑曲霉Aspergillusniger的转化活性较强,转化产物为人参皂苷Rg1、Rg2和Rh1。结论：首次报道黑曲霉能将人参皂苷Re转化为人参皂苷Rg1、Rg2和Rh1这一转化过程。     

人参叶中Ocotillone-型人参皂苷的分离

从人参叶中分离得到一个Ocotillone 型人参皂苷和两个已知人参皂苷 ,通过化学和理化性质鉴定方法 ,此Ocotil lone 型人参皂苷被鉴定为假人参皂苷 RT5,它是迄今为止在人参中发现的第一个Ocotillone 型人参皂苷 ,同时也讨论了其可能的生物转化途径     

稀有人参皂苷糖苷化合成方法的研究进展

稀有人参皂苷是人参皂苷中一类重要的活性成分,该类化合物具有极强的抗肿瘤活性。其主要通过糖苷化的方法来实现,现有的糖苷化方法主要包括化学合成法、酶解法和微生物转化法。研究表明糖苷化能改变化合物的生物活性、稳定性、水溶性、以及与受体分子的相互识别和结合特性,另外还能降低或除去内源和外源有毒物质的毒性。综述了3类糖苷化方法,并对比总结各个方法的优劣之处,有利于选择出最佳的合成稀有人参皂苷的糖苷化方法,以满足临床和科研等方面的需求。对人参皂苷的糖苷化最新研究进展进行综述,并对糖苷化人参皂苷的发展趋势作了简要的讨论。     

真菌EST-I及EST-II对人参皂苷Rg1定向转化为 人参皂苷F1的研究

目的 筛选能将人参皂苷Rg1定向转化为稀有人参皂苷F1的真菌。方法 通过硅胶柱色谱从三七总皂苷中分离纯化出人参单体皂苷Rg1;采用固体与液体发酵培养法,从325株真菌中筛选到能对单体人参皂苷Rg1进行生物转化的菌株。采用1H-NMR、13C-NMR波谱手段及理化性质鉴定人参皂苷Rg1及其转化产物。结果 发现真菌菌株EST-Ⅰ与EST-II将人参皂苷Rg1定向转化为人参皂苷F1,说明两种菌株能产生特异性水解C-6位葡萄糖的β-葡萄糖苷酶。结论 该方法是一种制备稀有人参皂苷F1的新方法。     

三七皂苷药物动力学及体内代谢研究进展

三七Panax notoginseng(Burk.)F.H. CHEN与人参同为名贵的古老中药,对心血管、血液、免疫系统及代谢均有一定药理作用.三七总皂苷[1](total saponins of Pnanx notoginseng,PNS)为三七根茎的有效部位,主要是达玛烷型20(S)-原人参二醇型(ppd)和20(S)-原人参三醇型(ppt)四环三萜皂苷,不含齐墩果酸型皂苷,单体的含量和比例与人参亦不同.本文对三七皂苷的药物动力学、体内代谢及其代谢产物活性的研究进展进行了简要综述.     

人参皂苷生物合成相关糖基转移酶研究基本策略及进展

人参、西洋参和三七等传统中药材因其广泛且良好的药理活性一直倍受关注,而人参皂苷是其主要活性成分。糖基转移酶是催化人参皂苷生物合成最后一步的关键酶。人参皂苷苷元经过糖基转移酶的修饰,产生了复杂多样的人参皂苷,从而具有广泛的药理活性。目前人们已通过合成生物学技术实现了人参皂苷苷元和稀有人参皂苷compound K的合成。人参皂苷苷元的糖基化作为人参皂苷生物合成途径的最后一步,是整个合成途径中最重要的环节之一,近年来也取得了一些研究进展。本文介绍了人参皂苷生物合成途径中相关糖基转移酶研究的基本策略,并对相关进展进行了综述,为人参皂苷生物合成途径的深入解析及通过合成生物学途径获得人参皂苷提供理论参考。     

红参中原人参萜三醇人参皂苷对P-糖蛋白介导的多药耐药性的逆转作用

作者研究了韩国产红参中人参皂苷是否可逆转 P-糖蛋白(Pgp)介导的多药耐药性(MDR)细胞对抗肿瘤药的 MDR。被检测的人参皂苷包括人参总皂苷、原人参萜三醇人参皂苷(PTG)、原人参萜二醇人参皂苷(PDG)、人参皂苷 Rb_1、Rb_2、Rc、Rg_1和 Re 等成分。选用的 MDR 细胞为耐柔红霉素的 AML-2/D100和耐多柔比星的 AML-     

Protective effects of ginsenosides against Bisphenol A-induced cytotoxicity in 15P-1 Sertoli cells via extracellular signal-regulated kinase 1/2 signalling and antioxidant mechanisms

Numerous studies have demonstrated that Bisphenol A (BPA) can cause reproductive toxicity. Ginseng has wide range of pharmacological actions and, more importantly, has proven its worth with respect to reproductive function in several reports. We have suggested that ginsenosides, the main active components of ginseng, may protect against BPA-induced cell damage. Therefore, an in vitro culture model of 15P-1 Sertoli cells was employed to investigate whether ginsenosides have protective effects on BPA-stimulated 15P-1 Sertoli cells. The results revealed that ginsenosides (75 μg/ml) significantly inhibited BPA-induced decreases in cell viability and increases in apoptosis. Immunofluorescence staining showed that BPA exposure-induced collapse of vimentin intermediate filaments was prevented by the application of ginsenosides. Ginsenosides also inhibited extracellular signal-regulated kinase (ERK1/2) phosphorylation and BPA-induced alterations of Bcl-2 and Bax protein expression in 15P-1 Sertoli cells. Furthermore, the alterations of T-AOC, superoxide dismutase, glutathione peroxidase, glutathione reductase, glutathione and malondialdehyde levels in BPA-stimulated cells were partially prevented with pre-treatment with ginsenosides. Taken together, these results suggest that ginsenosides have protective effects against BPA-induced cell damage and that these effects are mediated by preventing ERK1/2 phosphorylation and through the enhancement of cellular antioxidant capacity. Ginsenosides may therefore be beneficial in the prevention of environmental BPA-induced, reproduction-related toxicity.     

The protective effects of ginsenosides on human erythrocytes against hemin-induced hemolysis.

Panax ginseng has been used in traditional Chinese medicine to enhance stamina and capacity to deal with fatigue and physical stress. Many reports have been devoted to the effects of ginsenosides on many in vitro or in vivo experimental systems. The major aim of this work is to investigate the protective effects of 12 individual ginsenosides including Rb1, Rb3, Rc, Rd, Re, Rg1, Rg2, Rg3, Rh1, Rh2, R1 and pseudoginsenoside F11, together with the central structures of aforementioned ginsenosides, 20(S)-protopanaxadiol (PD) and 20(S)-protopanaxatriol (PT), on hemin-induced hemolysis of human erythrocytes. This is because hemin can induce hemolysis by accelerating the potassium leakage, dissociating skeletal proteins and prohibiting some enzymes in the membrane of erythrocyte. Thus, the structure-activity-relationship (SAR) between ginsenosides and protective effects has been screened in this in vitro experimental system. It is found that Rh2 and Rg3 intensify hemolysis in the presence of hemin, and initiate hemolysis even in the absence of hemin. All the other ginsenosides protect human erythrocytes against hemin-induced hemolysis more or less. The overall sequence is Rc>Rd>Re approximately Rb1>Rg1 approximately Rh1>Rb3 approximately Rg2 approximately R1 approximately F11 approximately PT. In addition, the protective effects of PD and PT have been detected, and found that PD promotes hemolysis appreciably, whereas PT protects erythrocytes efficiently. Moreover, the protective effects of PT ginsenosides are similar to PT itself, and the protective effects of PD ginsenosides vary remarkably, demonstrating that the positions of the sugar moieties make the protective activities of ginsenosides complicated. Especially, sugar moiety at 20-position is critical for PD ginsenosides to inhibit hemolysis, whereas hydroxyl group at 3-position is important for PT ginsenosides. The present result may be useful for understanding the SAR of ginsenosides.     

人参皂苷用于肝脏疾病的研究进展

人参皂苷是五加科人参属人参的主要有效成分,目前发现其单体多达150余种,且不同人参皂苷单体的药理作用也各有差异。人参皂苷主要有抗肿瘤、抗老年痴呆等作用。近年来的研究表明,人参皂苷在肝脏疾病如肝癌、肝纤维化、肝损伤和肝炎等,以及肝移植与肝脏切除中已经显现出一定的治疗作用。人参皂苷在肝脏疾病中的作用机制较为复杂,主要是通过抗氧化、抗炎等作用来保护肝细胞和调节肝功能。本文在查阅国内外文献的基础上,综述了人参皂苷在肝脏疾病治疗中的研究进展,同时就其作用机制进行了阐述,以期为该成分在肝脏疾病中的进一步研究提供参考。     

人参皂苷抗肿瘤作用机制的研究进展

人参皂苷是人参中最主要的活性成分,大量的研究证明其具有抑制肿瘤细胞增殖、促进肿瘤细胞凋亡、抑制肿瘤细胞侵袭和迁移等作用。本文通过查阅近年来的文献,针对人参皂苷抗肿瘤的作用机制进行综述,为临床人参皂苷在肿瘤治疗中的应用提供一定的指导。     

人参皂苷药理研究进展

人参皂苷是人参的主要有效物质，其药理作用表现多样。目前，对于单个人参皂苷的药理作用研究已非常深入，尤其在代谢调控方面的研究已成为一个焦点。本文就人参皂苷对神经系统、小肠传送功能、内分泌系统、免疫系统、信号传导、抗衰老、溶血、烧伤创面愈合、抗肿瘤增效、人的精子活力、药物代谢酶、降血糖方面的影响，综述了国际上近几年来所取得的研究新进展，并对原人参二醇类皂苷与原人参三醇类皂苷的药效作用进行了简要的比较。     

In vitro candidacidal action of Korean red ginseng saponins against Candida albicans

Korean red ginseng saponins (ginsenosides) have been reported as having various biological properties, but the antifungal effects and the mode of action of ginsenosides remain mostly unknown. In this study, saponins were isolated from Korean red ginseng, and the antifungal effects of ginsenosides were investigated. Ginsenosides showed fungicidal effects toward pathogenic fungi tested. To elucidate the antifungal mode of action of ginsenosides, flow cytometry analysis and the change in membrane dynamics using 1,6-diphenyl-1,3,5-hexatriene (DPH), as a plasma membrane probe, were performed with Candida albicans. The results suggest that ginsenosides may exert antifungal activity by disrupting the structure of cell membrane. The present study indicates that ginsenosides have considerable antifungal activity, deserving further investigation for clinical applications.     

Effects of ginsenosides on the glutamate release and intracellular calcium levels in cultured rat cerebellar neuronal cells

These studies were designed to examine the effects of ginsenosides on glutamate neurotransmission. In primary cultures of rat cerebellar granule cells, ginsenosides (Rb1, Rc and Rg1, 500 μg/ml) increased glutamate release which was measured by HPLC, but Re did not show an elevation of glutamate release. However, all of these ginsenosides down-regulated N-methyl-D-aspartate (NMDA)-induced glutamate release. Rc strongly increased glutamate release and elevated intracellular calcium concentrations (Ca²⁺ _i) which was measured by ratio fluorometry with FURA-2 AM. These, results indicate that ginsenosides have a homeostatic effect on glutamate neurotransmission, and there is a structure-function relationship among the ginsenosides tested.