三七花蕾皂甙成分的研究

从云南名贵药材三七(Panax notoginseng(Burk)F.H.Chen)的花蕾中分得10种化合物,经化学和光谱方法确定为:β-谷甾醇(β-Si-tosterol),胡萝卜甙(daucosterol),三七皂甙-Fe(notoginsenoside-Fe),绞股蓝皂甙-Ⅸ(gypenoside-Ⅸ),人参皂甙-Rc 和人参皂甙-Rb_3(ginsenosides-Rc和 ginsenosides-Rb_3)。其余4个微量化合物尚待进一步鉴定。     

用HPLC法研究不同提取方法对人参单体皂甙的提取效果

本文采用MPG-ODS色谱柱,以醋酸铵作HPLC流动相的改性荆在15 min以内较好地分离出单体皂甙Rg_2、Rb_1、Rc、Rd、Rg_1、Re等,首次比较了化学上醇提取方法和食用时水提取方法对单体皂甙及总皂甙提取效果的不同,结果表明,食用水对Rg组类皂甙的提取量高于Rb组,这将为人参的药理学研究及临床食用提供科学依据。     

三七中达马烷型皂甙的热不稳定性及酸水解产物

前人已证明人参和三七中富含的达马烷型人参皂甙在通常酸性水解下甙元即发生变化,而在弱酸(如50％醋酸,0.1N盐酸)条件下则形成次级皂甙。本文报道人参甙(ginseno-sides)和三七甙(notoginsenosides)的水溶液在水浴上加热亦分别形成相应的C-20位去糖基的次级皂甙。联系到人参和三七均有在蒸煮加工后C-20位去糖基皂甙收率增大的趋势,似可认为人参和三七中的这类皂甙有相当一部分是在生药的加工泡制以及提取过程中形成的次级皂甙,而不一定是植物体的原生成分。将人参甙Rb_1单体以酸水解,不仅得到主产物人参二醇(3),还分离到异去氢原人参二醇(5)、达马烷-20(22)-烯-3β,12β,26-三醇(6)、20(R)-达马烷-3β,12β,20,25-四醇(7)以及20(S)-和20(R)-原人参二醇(1、2)的混合物,从而认为这些微量成分与人参二醇一样均为达马烷型人参皂甙在酸性水解条件下C-20位糖基断裂后由真甙元的侧链转化形成的工作产物。     

羽叶三七根茎的三萜皂甙成分及其化学分类学意义

羽叶三七(Panax japonicus C. A. Meyer var. bipinnalifidus (Scem.) Wu et Feng)又称疙瘩七,产我国西北部至西南部山区,是人参届植物中分布海拔和纬度均较高的一个种类。在陕西省秦岭地区主要产于南北坡海拔2100—2900米的针叶林下阴湿处。民间以其根茎入药,具有清热解毒、顺气健胃、活血祛瘀、滋补强壮之效。作为国产人参属植物皂甙成分系统研究的一个部分,本文报告秦岭产羽叶三七根茎的皂甙成分,并讨论其化学分类学意义。     

不同产地西洋参皂甙成分的HPLC分析

以西洋参的主要皂甙成分人参皂甙Re和Rb1为标准对照品 ,建立西洋参药材的HPLC定量分析技术 ,并参考人参皂甙Rc,Rd及Rg2 的相对峰面积进行主成分分析。色谱条件为 :C18柱 (5 μm ,3.9× 15 0mm) ,乙腈 :水流动相 ,二元梯度洗脱 ,检测波长 2 0 3nm。结果表明 ,就皂甙成分的组成与含量而言通过人参皂甙Re和Rb1的含量测定和皂甙的主成分分析 ,不同产地的西洋参药材皂甙成分存在一定的差别。吉林省靖宇县产的西洋参与进口品最为接近。     

云南栽培西洋参皂甙的高压液相色谱定量分析

采用N-18ODS柱,以CH_3CN:H_2O(31:69 v/v)中加入50mM KH_2PO_4和CH_3CN:H_2O:H_3PO_4(20:80:0.5 v/v)为流动相,在202 nm紫外吸收波长检测下,测定了云南丽江引种栽培的西洋参中丙二酸人参皂甙(malonyl ginsenoside)Rb_1、Rb_2、Rc、人参皂甙(ginsenosidc)Rb_1、Rb_2、Rc、Rd、Ro和Rc、Rgl等10种主要皂甙的含量,讨论了不同的栽培年代、采收季节、地下部位以及商品等级中皂甙含量的变化,对该地区西洋参的生产提出了建议。     

西洋参与人参中人参皂甙含量的比较

采用ＴＬＣ和ＨＰＬＣ方法分析比较西洋参（Ｐａｎａｘ ｑｕｉｎｑｕｅｆｏｌｉｕｍ Ｌ．）、人参（Ｐ．ｇｉｎｓｅｎｇ Ｃ．Ａ．Ｍｅｙ．）及其加工品红参（ｒｅｄ ｇｉｎｓｅｎｇ）,以及不同规格的西洋参中人参皂甙的含量。结果表明,西洋参中人参皂甙总量及人参二醇型皂甙的含量明显高于人参及红参,且含有１种人参及红参中未发现的未知人参皂甙Ｒｘ,但不含人参及红参中含有的Ｒｆ;人参中人参二醇型皂甙的含量高于人参三醇     

土生曲霉转化三七中药材的研究

从土壤真菌中筛选出直接转化中药材三七化学成分的菌株YM31966,经鉴定该菌株为土生曲霉(Aspergillus terreus).以固态转化方式,结合化学提取分离方法,通过高效液相色谱、核磁共振及质谱等波谱检测,该菌株转化三七产物由三七皂苷nR2 、RX1和人参皂苷Rg1、Rd、Rh1、Rh4构成主体成分,而原三七成分Rb1、Rc、Re和R1、R3,R6等物质被分解.结果表明,土生曲霉是一株能转化中药材三七的微生物,它具有改变原三七化学成分,形成新化合物,以及提高某些原化合物成分含量的作用.     

复合酶解法提取三七皂苷的实验研究

以三七提取液中总皂苷的含量和提取物得率为指标,考察了乙醇回流法、渗漉法、纤维素酶解法、果胶酶解法、复合酶解法的优劣,并采用单因素法和四因素（纤维素酶用量、果胶酶用量、酶解温度、乙醇浓度）三水平正交设计法对复合酶解法提取工艺条件进行优选,得到如下较理想的提取工艺条件：纤维素酶用量为15U／g（生药）、果胶酶用量为140U／g（生药）,酶解pH值为4．5,酶解温度为50℃,乙醇浓度为80％,提取时间为2．5h。所得三七提取液中总皂苷的含量为12．01％,提取物得率为35．82％。     

三七总皂苷原粉和超微粉的理化性质比较研究

通过对药用植物三七总皂苷原粉和超微粉的粉体粒度、电位、显微结构、红外光谱、溶解速度这几项理化性质的研究,判定两种粉体的优劣,为三七总皂苷超微粉的市场推广提供依据。实验结果表明,三七总皂苷原粉经纳米化处理后成为三七总皂苷超微粉,其化学结构没有发生变化,但显微结构从条状的晶体变为由纳米球紧密排列的不规则形态,其粉体平均粒径也从1 122.4 nm缩小到153.4 nm,完成了从微米到纳米的转变,其水溶液也变为稳定的胶体溶液。运用高效液相色谱法,在模拟人体环境的条件下,发现三七总皂苷超微粉比三七总皂苷原粉早1 min完全溶解。说明三七总皂苷超微粉比三七总皂苷原粉颗粒更小,更易溶于水,更易与人体吸收。     

三七总皂苷对脑缺血再灌注大鼠神经血管单元超微结构的影响

为了观察脑缺血再灌注(cerebral ischemia reperfusion, CIR)大鼠缺血灶周边脑组织不同时间点神经血管单元(neurovascular unit, NVU)超微结构变化,研究三七总皂苷(Panax notoginseng saponins, PNS)对脑缺血再灌注大鼠脑组织NVU超微结构的影响,本研究采用改良Zea Longa法制作局灶性大脑中动脉闭塞(MCAO)模型,缺血2 h后再灌注;采用Longa法评分标准检测各组大鼠术后4 h神经功能评分,随之各组进行干预,分别在缺血再灌注后24 h、72 h、7 d、3周进行神经功能评分和透射电镜下观察各组大鼠缺血灶周边脑组织的NVU超微结构变化。研究结果表明,干预前即术后4 h治疗组和对照组神经功能评分比较无明显差异;PNS干预后治疗组大鼠神经功能评分逐渐改善,缺血再灌注后24 h与对照组比较,差异无统计学意义(p>0.05),再灌注72 h、7 d、3周的大鼠神经缺损评分与同时间点对照组相比差异具有统计学意义(p<0.05)。电镜观察发现再灌注24 h、72 h、7 d、3周治疗组大鼠脑组织NVU超微结构的病理形态损伤均较同时间点对照组明显减轻。本研究结论认为,PNS通过整合促进脑缺血后NVU的神经元、胶质细胞和微血管的修复,改善神经功能缺损症状,对脑缺血具有保护作用。     

Biotransformation of Saponins by Endophytes Isolated from Panax notoginseng

The biotransformation of the major saponins in Panax notoginseng, including the ginsenosides Rg1, Rh1, Rb1, and Re, by endophytes isolated from P. notoginseng was studied. One hundred and thirty‐six endophytes were isolated and screened for their biotransformational abilities. The results showed that five of the tested endophytes were able to transform these saponins. These five strains were identified based on their ITS or 16S rDNA sequences, which revealed that they belonged to the genera Fusarium, Nodulisporium, Brevundimonas, and Bacillus genera. Ten transformed products were isolated and identified, including a new compound 6‐O‐[α‐L ‐rhamnopyranosyl‐(1→2)‐β‐D ‐glucopyranosyl]‐20‐O‐β‐D ‐glucopyranosyldammarane‐3,6,12,20,24,25‐hexaol ( 3 ), and nine known compounds, compound K ( 1 ), ginsenoside F2 ( 2 ), vinaginsenoside R13 ( 4 ), vinaginsenoside R22 ( 5 ), pseudo‐ginsenoside RT4 ( 6 ), (20S)‐protopanaxatriol ( 7 ), ginsenoside Rg1 ( 8 ), vinaginsenoside R15 ( 9 ), and (20S)‐3‐O‐β‐D ‐glucopyranosyl‐6‐O‐β‐D ‐glucopyranosylprotopanaxatriol ( 10 ). This is the first study on the biotransformation of chemical components in P. notoginseng by endophytes isolated from the same plant.     

Ginsenoside Rd from Panax notoginseng is cytotoxic towards HeLa cancer cells and induces apoptosis

The saponin ginsenoside Rd (1), isolated from Panax notoginseng, is used for the treatment of cardiovascular diseases, inflammation, different body pains, trauma, and internal and external bleeding due to injury. In this study, we report that 1 inhibits the cell growth of human cervical cancer (HeLa) cells in a concentration- and time-dependent manner, with an IC(50) value of 150.5+/-0.8 mcirog/ml after 48 h of incubation. The drug-treated cells displayed features of apoptosis, including typical morphological characteristics and formation of DNA ladders, as evident from agarose-gel electrophoresis. Flow-cytometric analysis showed that the cell-cycle distribution of HeLa cells exposed to 1 is characterized by a decrease of the G(0)/G(1)-phase and an increase of the S-phase cells, respectively, in a dose-dependent manner. The apoptotic rate of HeLa cells treated for 48 h with 210 microg/ml of 1 was 35.8%. Further, 1 was found to increase the expression of Bax and to decrease the expression of Bcl-2 proteins, respectively, and to lower the mitochondrial transmembrane potential of HeLa cells. The caspase-3 inhibitor DEVD-CHO (at 2 microM) increased the viability of HeLa cells treated with 1. Taken together, our study suggests that ginsenoside Rd (1) significantly inhibits HeLa cell proliferation, and induces cell apoptosis through down-regulating Bcl-2 expression, up-regulating Bax expression, lowering the mitochondrial transmembrane potential, and activating the caspase-3 pathway. Thus, 1 could serve as a lead to develop novel chemotherapeutic or chemopreventive agents against human cervical cancer.     

Studies on Fermentation Culture of Cells of Panax notoginseng

The saponin content of Panax notoginseng cell cultures-was 11.14% of dry weight, the saponin yield was 1513.3mg· L-1, and yield of cell cultures was 13.58g dry wt · L-1 per month in fermentation culture, which were all better than those obtained from in suspension culture. Increasing inoculum quantity could obviously increase growth rate, saponin content and yield of cell cultures. An aeration rate of 0.8vvm was optimal for fermentation culture of the cells. The pH value of the culture broth went down from 5.80 to 3.92 gradually and never returned in fermentation culture of P. notoginseng cells.     

三七总皂苷抗肝纤维化作用机制的研究进展

肝纤维化是各种慢性肝病共同的病理基础,是慢性肝病发展到肝硬化、肝癌的必经途径。寻找有效的抗肝纤维化药物是近年研究的热点,其中对三七的研究也取得了很大进展。现综述近几年三七皂苷在保护肝细胞、抑制肝星形细胞活化、促进肝星形细胞凋亡、抑制细胞外基质的合成及促使其降解等方面的作用及可能机制,同时也阐述了三七总皂苷在抗肝纤维化中的重要意义及应用前景。     

三七(Panax notoginseng)根残体化感自毒效应研究

为研究三七(Panax notoginseng(Burk)F.H.Chen)采收过程中残留须根的化感自毒效应,采用土培和水培2种方法,按不同比例添加三七须根粉碎物,检测根残体作用下土培三七土壤中皂苷的动态变化及水培三七根部形态结构变化。结果显示,土培条件下,随着须根粉碎物处理时间的延长,土壤中皂苷成分种类增加、总皂苷含量减少。水培条件下,随着处理时间的延长,添加须根粉碎物处理后的三七根尖细胞壁增厚,细胞中出现菌丝体;随着处理时间及处理浓度的增加,细胞开始皱缩甚至破碎,细胞中无完整细胞器结构,三七根部细胞结构差异明显。研究表明三七采收过程中残留在土壤中的须根腐解释放的化学物质可能是导致三七自毒效应的因素之一。     

Effects of oligosaccharins on callus growth and saponin content of Panax notoginseng

This work provides some evidences for the saponinproduction of Panax notoginseng callus by using biologi-cally active,wall-related oligosaccharins.In anappropriate concentration,three kinds of oligosaccharinsstimulated saponin formation or callus growth.Theconcentration of DO,GO and CO for saponin productionof Panax notoginseng callus culture were 15ppm,15ppmaud 20ppm respectively by comparing saponin yield.Itwas very obvious for DO to increase saponin contentwhen the concentration was 10ppm,and for GO tostimulate callus growth when the concentration was20ppm.It would be a good way to produce saponin byusing oligosaccharins in large scale culture in thefuture.