西洋参冠瘿组织培养及其人参皂苷Re和人参皂苷Rg1的产生

考察了培养基组成、培养时间、接种量、pH值、肌醇浓度等对冠瘿组织生长及其人参皂苷含量的影响 ;用HPLC检测了冠瘿组织中人参皂苷Re和人参皂苷Rg1 的含量。高压纸层析电泳证实 ,根癌农杆菌Ti质粒上的T DNA片段已整合进入植物细胞核基因组中。在考察的 6种培养基中 ,White培养基最适合人参皂苷Rg1 的累积(0 0 95 % ) ,MS培养基最适合人参皂苷Re的累积 (0 194 % )。以MS为基本培养基培养 36d、32d时人参皂苷Re和人参皂苷Rg1 累积含量最高 (分别为 0 14 7%和 0 0 6 1% ) ;接种量为 4g、2g (FW flask) ,有利于人参皂苷Re和人参皂苷Rg1的累积 ;培养基pH 5 8时人参皂苷Re含量最高 (0 184 % ) ,培养基pH 5 6时人参皂苷Rg1 累积量最高 (0 0 5 4 % ) ;肌醇浓度为 0 0 5g L时 ,能促进人参皂苷Re合成 (0 182 % ) ,浓度为 0 30g L时 ,有利于人参皂苷Rg1 累积 (0 0 5 5 % )。     

西洋参总皂苷酶水解产物成分研究

西洋参总皂苷经β-糖苷酶催化水解,采用HPLC检测分析确定西洋参总皂苷中的主要原人参二醇型皂苷Rb1、Rd、Rc和Rb2已经完全被水解。水解产物通过反复硅胶柱层析和反向硅胶柱层析分离纯化得到7个皂苷,通过NMR谱图分析分别鉴定为人参皂苷compound K(1)、人参皂苷Mc(2)、人参皂苷Rg1(3)、人参皂苷Rg2(4)、人参皂苷Re(5)、人参皂苷F1(6)和拟人参皂苷F11(7)。β-糖苷酶催化西洋参总皂苷水解实验表明,西洋参中原人参二醇型皂苷的水解产物是人参皂苷compound K和人参皂苷Mc。     

西洋参冠瘿组织悬浮培养及其人参皂苷类成分的分离

对西洋参冠瘿组织悬浮培养生长特征进行了考察,并对其悬浮培养物中的人参皂苷类成分进行了提取、分离和鉴定。研究得到了培养物最大生物量收获时间［18.62 g/L(dry weight)］及其中最高人参皂苷累积时间（620.4 mg/L on the 27thday）。培养基中碳源、磷、氨基氮、硝基氮的利用率分别为91.8%, 100%, 81% 和97%。利用现代分离纯化方法从培养物中分离得到了4种人参皂苷类成分,利用理化及谱学技术分别鉴定为假人参皂苷F11（pseudoginsenoside F₁₁,Ⅰ）, 人参皂苷Rd（ginsenoside Rd,Ⅱ）, 人参皂苷Rb1（ginsenoside Rb1 ,Ⅲ）和人参皂苷Rb3（ginsenoside Rb3,Ⅳ）。     

人参皂苷降脂作用的研究

为了测定西洋参总皂苷及单体皂苷是否有降脂活性,通过体外实验分别测定脂肪分解活性、小肠刷状缘膜小囊吸收脂肪酸、三油酸甘油酯油酸的释放率。结果表明,西洋参茎叶总皂苷在0．5g／L浓度时,对胰脂肪酶活性的抑制率为90％;人参皂苷Rc,Rb1,Rb2对胰脂肪酶活性均显示很强的抑制作用,在0．5g／L浓度时抑制率分别为100％,96％,97％。西洋参总皂苷和人参皂苷Rc,Rh,Rb2可以通过抑制胰脂肪酶活性起到降脂作用。     

黑根霉对人参皂苷Re的生物转化

利用菌种黑根霉Rhizopus sp.对人参皂苷Re进行生物转化,并对人参皂苷Re及其发酵产物进行HPLC系统分析比较,经液相色谱-质谱分析得出人参皂苷Re转化率为92.16%,并制备出人参皂苷Re发酵产物中峰值升高的成分,转化后的人参皂苷发酵产物中化合物1确定为人参皂苷Rg2,化合物2为Rg2的同分异构体,得率为10.13%;化合物3和化合物4确定为人参皂苷Rg5/Rk1,得率为29.23%。从结果初步推测得出人参皂苷Re被黑根霉转化为人参皂苷Rg2的机理,人参皂苷Re转化成人参皂苷Rg5/Rk1的机理还有待于进一步研究。     

三七叶、人参叶和西洋参叶皂苷类成分的研究(英文)

三七叶、人参叶和西洋参叶其皂苷类成分相近,但专属性成分各异,皂苷类成分的分布比例也各不相同。本文建立了HPLC-UV法测定上述皂苷成分的方法,经过方法学考察,各种皂苷成分精密度好、加样回收率高,方法可靠。11种皂苷成分总含量顺序为:西洋参叶>人参叶>三七叶;二醇组皂苷成分含量:西洋参叶>三七叶>人参叶;三醇组皂苷成分含量:人参叶>西洋参叶>三七叶。西洋参叶中二醇组皂苷和人参叶中三醇组皂苷含量明显高于其他。西洋参叶中人参皂苷Rb3和Rd的含量之和占11种皂苷成分的60%以上。鉴于其中人参皂苷的高含量,三七叶、人参叶和西洋参叶应该作为皂苷来源得到充分利用;不同的皂苷成分有不同的药理活性,应基于它们的皂苷组成和比例选择性进行研究和开发。     

人参生殖器官皂苷含量动态变化

为了明确从现蕾、开花到结实过程中的人参生殖器官中各单体皂苷含量的动态变化,应用HPLC法测定了人工栽培的五年生人参不同时期生殖器官中的人参单体皂苷Rb1、Rb2、Rb3、Rc、Rd、Re、Rg1和Rg3的含量。结果显示:从现蕾到果实成熟的过程中,人参单体皂苷Rb1、Rb2、Rb3、Rc、Rd、Re、Rg1和Rg3的含量的平均值分别为0.643%,0.189%,1.026%,1.014%,1.941%,8.381%,0.724%和0.041mg.g-1。从现蕾到果实成熟的过程中,人参单体皂苷Rb1含量的最高值在7月16日,单体皂苷Rb3、Rc、Rd和Rg1含量的最高值在7月11日,单体皂苷Rb2和Rg2含量的最高值在8月7日。     

小型生物反应器内人参不定根的人参皂苷累积

对小型生物反应器(3~10 L)培养人参不定根的生长和人参皂苷(Rg1、Re、Rb1)的累积规律,以及蔗糖浓度、初始接种量对其生长和人参皂苷累积的影响进行研究。结果表明:小型生物反应器内人参不定根的最佳收获周期为7周。初始接种量和蔗糖浓度影响生物反应器内人参不定根的生长和人参皂苷的累积,20或40 g/L蔗糖对人参不定根的生长和人参皂苷的累积优于60 g/L蔗糖;5和10 L生物反应器内最佳初始接种量分别为15和30g,其不定根的生长量分别为9.29和19.17 g,人参皂苷含量分别为5.16和4.58 mg/g。生物反应器内培养7周的人参与栽培4年的人参相比,人参皂苷Rg1和Re含量相差不大,但栽培人参中Rb1的含量远高于生物反应器中所培养的人参不定根。     

人参皂苷与生态因子的相关性

环境条件影响中药材活性成分的形成和积累.利用各种数学统计分析方法探讨影响人参皂苷积累的生态因子,提高人参品质.人参样品采自人参道地产区(主产区)吉林、辽宁、黑龙江三省5年生栽培人参,同时采集采样点处的土壤样品.超高效液相(UPLC)色谱法分析了不同产区9种人参皂苷(Rg1、Re、Rf、Rg2、Rb1、Rc、Rb2、Rb3、Rd)的含量;利用“中药材产地适宜性分析地理信息系统”的生态因子空间数据库,获得采样区包括温度、水分、光照等10个生态因子数据;按土壤理化性质常规方法测定土壤样品中的有效硼、有效铁等微量元素和速效氮、速效钾等有效养分.对人参有效成分含量与土壤养分进行典型相关性分析发现,土壤中的有效硼、有效铁、速效氮与人参皂苷含量呈显著正相关,即适当提高土壤中有效硼、有效铁和速效氮的含量可以促进人参皂苷成分的积累,土壤水分与所测人参皂苷含量(Rb3除外)呈显著正相关,速效磷(P)、pH、速效锌(Zn)与各人参皂苷含量呈弱相关;人参皂苷与气候因子相关分析表明,温度(年活动积温、年平均气温、7月最高气温、7月平均气温、1月最低气温、1月平均气温)与人参皂苷含量呈显著负相关,其中与药典中人参含量测定项下的人参皂苷Rg1、Re、Rb1负相关尤为显著(r＞0.6),说明在一定温度范围内,人参皂苷是随着温度的降低而升高的,即适当低温有利于人参皂苷有效成分的积累;海拔与人参皂苷Rc、Rb2、Rb3含量呈显著正相关(r＞0.6),即相对较高的海拔可以促进这3种成分的积累;而年均降水量、年相对湿度和年均日照时数与人参皂苷相关不显著.通过主成分分析(PCA)、典型相关分析、排序等统计方法,考察不同产地样品中人参皂苷含量与生态因子间的相关性,研究结果揭示了温度在人参的主要活性成分-皂苷类形成中起决定性作用,在一定的温度范围内,温度越低越有利于人参皂苷的积累;阐明了土壤中的有效硼、有效铁、速效氮与人参皂苷含量成正相关.研究结果提示在人参实践生产中可以通过适当低温处理,增施硼、铁、氮肥等农艺措施来调控人参皂苷含量.     

人参皂苷Rb3对胰脂肪酶的抑制作用

采用硅胶柱层析、JTY树脂分离制备人参皂苷Rb3,薄层板(TLC)跟踪,高效液相色谱法(HPLC)检测。目的是研究西洋参叶中不同浓度的人参皂苷Rb3对胰脂肪酶的抑制作用影响,从而表明人参皂苷Rb3在抗肥胖中的作用。用制得的人参皂苷Rb3,在卵磷脂所乳化的甘油三酯的检测系统中进行体外胰脂肪酶抑制实验。结果表明:制得的人参皂苷Rb3经过三种不同展开剂,薄层板展开,均为一个点,进一步经HPLC检测其纯度为93.2%。胰脂肪酶抑制试验结果表明人参皂苷Rb3在浓度为0～1 mg/mL时,其抑制率达到85.11±0.409%,而且远远高于西洋参叶提取物。本文通过胰脂肪酶抑制试验表明Rb3具有抗肥胖作用,其抑制机制有待进一步研究。     

Conversion of Major Ginsenoside Rb1 to Ginsenoside F2 by Caulobacter leidyia

Ginsenoside Rb₁ is the most predominant ginsenoside in Panax species (ginseng) and the hydrolysis of this ginsenoside produces pharmaceutically active compounds. Caulobacter leidyia GP45, one of the isolates having strong β-glucosidase-producing activity, converted ginsenoside Rb₁ to the active metabolites by 91%. The structures of the resultant metabolites were identified by NMR. Ginsenoside Rb₁ had been consecutively converted to ginsenoside Rd (1), F₂ (2) and compound K (3) via the hydrolyses of 20-C β-(1→6)-glucoside, 3-C β-(1→2)-glucoside, and 3-C β-glucose of ginsenoside Rb₁.     

人参皂苷CK的研究进展

人参皂苷coumpound K(CK)是人参中原人参二醇型皂苷在人体肠道内的主要代谢产物,属于稀有人参皂苷。人参皂苷CK独特的生物活性已经引起了人们广泛关注,针对它的科学研究也日益增多。因此,有必要介绍近年来人参皂苷CK药理活性和制备方法方面的研究进展。     

Ginsenoside RG1 and corticosteroid receptors in rat brain

Old (28 months) male Wistar rats were treated chronically for two weeks with ginsenoside Rg1 or with vehicle delivered via sc implanted Alzet mini-pumps (rate of ginsenoside release 2.4 micrograms/0.5 microliter/h). The number of Type 1 corticosterone-preferring receptor sites (CR) and Type 2 glucocorticoid receptors (GR) was measured in the cytosol of hippocampus tissue of rat brain with an in vitro binding assay. In old rats the Bmax of Type 1 CR and Type 2 GR was reduced by 51.5% and 28.3% respectively. Following the two week treatment with Rg1 the Bmax of Type 1 CR increased by 60% and a receptor concentration was reached which was 21% lower than that observed in the young control animals. Minor differences in affinity of steroid binding to both receptor systems were observed in the groups of rats. The possible binding of ginsenosides to brain corticosteroid receptors in vitro was investigated as well. The inclusion of a 500 fold molar excess of Rg1 in hippocampus cytosol did not displace 3H-corticosterone from its soluble receptor sites. The affinity of Rg1 with these sites in vitro is therefore negligible. In conclusion, the binding capacity of Type 1 CR and Type 2 GR is reduced in the hippocampal brain region of aged rats. Upon chronic infusion of ginsenoside Rg1, only Type 1 CR capacity is restored towards the level observed in young control animals. This finding suggests that in old rats the ginsenoside enhances the CORT signal via Type 1 CR on the function of the hippocampus, which is a limbic brain structure involved in cognition, mood and affect.     

人参皂苷Rg3药代动力学及抗肿瘤作用的研究进展

人参皂苷Rg3是存在于天然药物人参中的一种四环三萜皂苷,研究表明人参皂苷Rg3具有确切的抗肿瘤活性,在诱导肿瘤细胞凋亡、抑制肿瘤细胞增殖、增强免疫功能等方面具有显著作用。本文通过查阅近年来相关文献,概括人参皂苷Rg3药效学及药代动力学研究进展,探讨人参皂苷Rg3抗肿瘤的作用机理以及体内吸收、分布、代谢、排泄规律,并在此基础上结合现代中药理论对今后人参皂苷Rg3的研究方向进行了展望。     

人参皂苷化合物生物合成进展

人参皂苷是我国许多传统名贵药用植物的主要活性物质,在医药、保健品、营养品和化妆品开发领域有广阔的应用前景,特别是稀有人参皂苷具有显著的抗肿瘤、保护神经系统、保肝护肝等药理活性.但其在植物中含量低且不稳定,严重影响了人参皂苷类物质的开发利用.自20世纪末以来,随着生物技术的不断发展和多种生物基因组的测序和解析,使得人参皂...     

人参皂苷抗衰老机制的研究进展

人参皂苷的抗衰老作用被认为是人参皂苷的重要作用之一。人参皂苷主要通过四种途径实现其抗衰老功能:通过提高机体内SOD、CAT、GSH2Px活性,诱导SOD、CAT基因表达,减少LPO、MDA含量等实现其抗衰老作用;通过促进神经递质释放、增加神经递质传递者(Ach)含量、促进NBM神经元TrkB mRNA表达、阻止神经原产生过量硝酸盐等实现其抗衰老功能;通过免疫系统在细胞和分子水平上的适度调节延缓衰老;人参皂苷亦能通过影响细胞周期调控因子、衰老基因表达,延长端粒长度、增强端粒酶活性等来实现其抗衰老功能。人参皂苷抗衰老的更完善和更深入的分子作用机制研究将成为未来研究的重点之一。     

Ginsenoside Re suppresses electromechanical alternans in cat and human cardiomyocytes

Ginseng botanicals are increasingly used as complementary or alternative medicines for a variety of cardiovascular diseases, yet little is known about their cellular actions in cardiac muscle. Electromechanical alternans (EMA) is a proarrhythmic cardiac abnormality that results from disturbances of intracellular Ca(2+) homeostasis. This study sought to determine whether a purified ginsenoside extract of ginseng, Re, exerts effects to suppress EMA and to gain insight into its mechanism of action. Alternans was induced by electrically pacing cardiomyocytes at room temperature. Re (> or = 10 nM) reversibly suppressed EMA recorded from cat ventricular and atrial myocytes and Langendorff-perfused cat hearts. In cat ventricular myocytes, Re reversibly suppressed intracellular Ca(2+) concentration ([Ca(2+)](i)) transient alternans. Re exerted no significant effects on baseline action potential configuration or sarcolemmal L-type Ca(2+) current (I(Ca,L)), Na(+) current, or total K(+) conductance. In human atrial myocytes, Re suppressed mechanical alternans and exerted no effect on I(Ca,L). In cat ventricular myocytes, Re increased [Ca(2+)](i) transient amplitude and decreased sarcoplasmic reticulum (SR) Ca(2+) content, resulting in an increase in fractional SR Ca(2+) release. In SR microsomes isolated from cat ventricles, Re had no effect on SR Ca(2+) uptake. Re increased the open probability of ryanodine receptors (RyRs), i.e., SR Ca(2+)-release channels, isolated from cat ventricles and incorporated into planar lipid bilayers. We concluded that ginsenoside Re suppresses EMA in cat atrial and ventricular myocytes, cat ventricular muscle, and human atrial myocytes. The effects of Re are not mediated via actions on sarcolemmal ion channels or action potential configuration. Re acts via a subcellular mechanism to enhance the opening of RyRs and thereby overcome the impaired SR Ca(2+) release underlying EMA.     

Evaluation of chemopreventive action of Ginsenoside Rp1

We evaluated the chemopreventive properties of Ginsenoside Rp1 on 7,12-Dimethyl benz (a) anthracene (DMBA) skin papillomagenesis in Swiss albino mice. A significant reduction in values of tumor incidence, tumor burden, and cumulative number of papilloma was observed in mice treated orally with Ginsenoside Rp1 continuously at pre-, peri- and post-initiational stages of papillomagenesis as compared to the control group. Chemopreventive potential of Ginsenoside Rp1 was also observed on the skin metabolizing enzymes in Swiss albino mice. Ginsenoside Rp1 produced a significant elevation in the skin microsomal cytochrome p-450 and cytochrome b5, glutathione S-transferase (GST), reduced glutathione (GSH), glutathione peroxidase (GPX), glutathione reductase (GR), DT-diaphorase, superoxide dismutase (SOD) and catalase levels in the group of mice treated with Ginsenoside Rp1 for seven consecutive days. However, there was significant decrease in lipid peroxidation (LPO) level in Ginsenoside Rp1 treated group.