三七根、叶、花皂甙对麻醉犬血流动力学的影响

本文研究了三七根、叶、花总甙及三七皂甙C_1和E_1对麻醉犬血流动力学的作用。结果表明:根总甙明显降低动脉血压和总外周阻力,增加心输出量和减慢心率,降低心肌耗氧指数。根总甙中含量最多的单体皂甙C_1(即人参皂甙Rg_1)可使血压短时下降,但LV dp/dt_(max)和心输出量显著增加,伴总外周阻力明显下降。叶总甙及其含量较多的皂甙E_1(即人参皂甙Rb_1)对上述指标均无明显影响。花总甙的作用温和短暂。 这些结果提示三七根皂甙是心血管药理作用的活性成分,地上部分皂甙无明显心血管作用,且毒性较大。     

羽叶三七叶中甙类成分的研究

从羽叶三七叶中分离到十三种甙类成分,经FAB-MS,¹³CNMR谱,双照射¹HN-MR谱,¹H-¹H COSY谱及与标准品直接对照,证明十一种为已知化合物,分别为人参皂甙F₁(Ⅰ),F₂(Ⅱ),F₃(Ⅲ),R_g2(Ⅳ),R_a(Ⅴ),R_d(Ⅵ),R_b1(Ⅷ),R_b3(Ⅷ),24(S)-假人参甙F₁₁(Ⅸ),人参黄酮(Ⅹ)和珠子参甙F₁(Ⅺ);另外两种为新的达玛烷型皂甙,命名为羽叶三七甙F₁(Ⅻ)和F₂(ⅫⅠ),并确定其化学结构。同时修正珠子参甙F₃的结构。进一步阐明人参黄酮甙结构中的两个糖的连接方式。     

中国辽宁栽培西洋参化学成分的研究

中国辽宁栽培西洋参(Panax quinquefolius Linn)的总皂甙用低压硅胶柱和反相Rp18Labar柱层析分离得到18种化合物,用IR,MS(FD-MS,FAB-MS),¹³C-NMR及化学方法鉴定了16种化合物的化学结构;分别为棕榈酸(1),齐墩果酸(2),胡萝卜甙(daucosterin 3),人参皂甙-Rh₁(4),—Rg₃(5),—Rg₂(6),—Rg₁(7),—Rf(8),—Re(9),—Rd(10),—Rb₂(11),—Rb₁(12)、—R₀(13),蔗糖(14),人参三糖(15)及一种新皂甙(16),结构为:20(s)原人参二醇-3-[-O-β-D-吡喃糖基(1→2)β-D-葡萄吡喃糖基(1→2)β-D-葡萄吡喃糖基],20-[-O-β-D-葡萄吡喃糖基(1→6)β-D-葡萄吡喃糖甙,命名为人参皂甙-RAO(ginsenoside-RA₀)。化合物(4)和(5)系首次从西洋参中分离出的已知皂甙。     

HPLC法测定人参三七颗粒中人参皂苷Rg1、Re、Rb1和三七皂苷R1的含量

摘 要 目的: 建立同时测定人参三七颗粒中人参皂苷Rg₁、Re、Rb₁和三七皂苷R₁含量的方法。方法: 采用HPLC法,色谱柱为Sunfire C₁₈（150 mm×4.6 mm,5 μm）分析柱,流动相以乙腈-水梯度洗脱;检测波长为203 nm;柱温30℃;流速1.0 ml·min^-1。结果:人参皂苷Rg₁,Re,Rb₁和三七皂苷R₁之间有较好的分离度,4种成分在线性范围内与峰面积之间线性关系良好,人参皂苷Rg₁、Re、Rb₁和三七皂苷R₁加样回收率分别为99.83%,97.84%,98.43%,97.34%,RSD分别为2.08%,1.66%,1.73%和1.42%（n=5）。结论:本方法可同时测定人参三七颗粒中的人参皂苷Rg₁,Re,Rb₁和三七皂苷R₁含量。     

喙果绞股蓝中皂甙成分的研究

首次从喙果绞股蓝(Gymostemma yixingense CY Wu et SK Chen)中分得四个皂甙成分(Ⅰ～Ⅳ),经理化常数测定、光谱解析和化学方法确定了它们的结构。其中Ⅰ为新化合物,命名为喙果皂甙A(yixinosideA),Ⅱ,Ⅲ和Ⅳ分别鉴定为绞股蓝皂甙XLIVXLII(gypensideXLIV,XLII)和具明显调脂作用的人参皂甙Rb₁(ginsenosideRb₁)。此外,Ⅰ经酸水解得到一新皂甙元1β-羟基人参二醇(1β-hydroxylpanaxadiol)(Ⅴ)和一新次级甙,命名为喙果皂甙B(yixinosideB,VI)。     

三七绒根中皂甙B1及B2的分离和鉴定

从三七Panax notoginseng(Burk.)F.H.Chen绒根中分得二种微量皂甙,三七皂甙B₁和B₂三七皂甙B₁为一种新皂甙,证明其结构为达玛20(22)-烯3β,12β,25三醇6-O-β-D-葡萄吡喃糖甙(Ⅰ),其皂甙元亦为一种新皂甙元,其结构为达玛20(22)-烯-3β,12β,6 C,25四醇。三七皂甙B₂经鉴定为已知皂甙人参皂甙(ginsenoside—Rh₁,Ⅱ)。     

人参皂甙Rb1对应激性性行为缺损的保护作用及机制

用悬吊应激模型,小鼠连续应激小鼠10d,每天应激一次,并循序增加应激强度,每次应激前30min,ip人参皂甙Rb₁,观察人参皂甙Rb₁对应激性性行为低下的保护作用。结果表明,应激模型组小鼠性行为明显减少,甚至达到缺损的程度,同时血浆睾酮水平明显降低,而Rb₁各剂量组(2.5,5,10mg·kg^-1)对应激引起的性行为低下及血浆睾酮水平下降均有明显的对抗作用。提示人参皂甙Rb1对应激性性行为低下有保护作用,其机制可能与Rb₁抑制应激动物血浆皮质酮升高和提高睾酮水平有关。     

HPLC-MS/MS测定同济2号颗粒剂中黄芪甲苷、绿原酸、人参皂苷Rg1、人参皂苷Rb1和三七皂苷R1

目的 建立HPLC-MS/MS同时测定同济2号颗粒中5个主要活性成分黄芪甲苷、绿原酸、人参皂苷Rg₁、人参皂苷Rb₁及三七皂苷R₁的方法。方法 以水(0.1%甲酸)-乙腈(0.1%甲酸)为流动相,梯度洗脱,体积流量为0.4 mL/min。YMC-Pack Pro C₈色谱柱分离,采用电喷雾离子源(ESI源),负离子模式,以选择性离子监测模式(SIM)进行测定。监测离子分别是m/z 829(黄芪甲苷)、m/z 353(绿原酸)、m/z 845(人参皂苷Rg₁)、m/z 1 108(人参皂苷Rb₁)、m/z 932(三七皂苷R₁)。结果 黄芪甲苷、绿原酸、人参皂苷Rg₁、人参皂苷Rb₁和三七皂苷R₁分别在0.075～2.4、0.95～30.3、1.71～54.72、1.12～35.92、0.45～14.28 μg/mL与峰面积呈良好线性关系。结论 该方法专属性好,灵敏度高,准确快捷,适用于同济2号颗粒的快速检测,为该药的质量标准提供依据。     

用核磁共振新技术测定日本续断皂甙E1的结构

从日本续断Dipsocus japunicus Miq.根的乙醇提到物中得到一个新三萜皂甙(5糖甙)，命名为日本续断皂甙E₁(japondipsaponin E₁)。用化学方法及¹HNMR,¹³CNMR,¹H-¹H COSY，一维多重接力COSY，选择性远程DEPT和三重共振NOE差谱等方法，鉴定其结构为3-O-α-L-吡喃鼠李糖(1-3)-β-D-吡喃葡萄糖（1→3）-α-L-吡喃鼠李糖（1→2）-α-L-吡喃阿拉伯糖常春藤皂甙元28-O-β-D-吡喃葡萄糖甙。     

HPLC-ELSD同时测定跌打丸中三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1的含量

目的 建立同时测定跌打丸中三七皂苷R₁、人参皂苷Rg₁和人参皂苷Rb1含量的HPLC-ELSD检测方法。方法 采用Phenomenex Kinetex C₁₈色谱柱(100 mm×4.6 mm,2.6 μm),柱温30 ℃,流速0.5 mL·min^-1,流动相为乙腈-水,梯度洗脱,ELSD检测器,漂移管温度110 ℃,载气(空气)体积流量3.0 L·min^-1。结果 三七皂苷R₁、人参皂苷Rg₁、人参皂苷Rb1分别在0.158~3.16 μg(r=0.999 8),0.407~8.14 μg(r=0.999 5),0.446~8.92 μg(r=0.999 9)内呈良好的线性关系,平均加样回收率分别为97.55%(RSD=1.04%),98.09%(RSD=1.03%),97.34%(RSD=0.81%)。结论 该方法简便、快速、准确,可用于跌打丸的质量控制。     

三七的化学研究——Ⅰ.三七绒根的成份研究

三七(panax notoginseng (Burk.) F. H. Chen)为云南特产药材,我国常用中药。其功能为滋补强壮,止血化瘀,消肿止痛,治气血虚弱,跌打损伤,产后瘀阻,崩漏,经闭,内出血,胃和十二指肠溃疡,咳血,吐血,便血,尿血,鼻衄等。近年来国内一些医院将三七用于治疗冠心病,获得较好疗效,故我们对三七化学成份进行研究,其研究结果如下:     

三七总皂甙及三七皂甙C1对实验动物血糖的影响

General saponin is the major effective substance in the fibrous root of Panax notoginseng (Burk) F. H. Chen, and sanchinoside C₁ is the main constitueet of this general saponin. Their effects on blood sugar were Studied on experimental animals. It was found that oral administration of sanehinoside C₁ in mice, was followed, by a slight rise in fasting blood sugar and a fall to normal level in hyperglycemia. But sanchinoside C₁ showed no influence on hyperglycemia induced by adrenalin.General saponin of Panax notoginseng can also raise the fasting blood sugar level in mice and decreases the hyperglycemia in mice and rabbits, but it did not influence on the ability of insulin in reducing blood sugarln rabbits. The effect of this general saporiin differs from sanchinoside C₁ in that the latter increases hyperglycemia induced by adrenalin in mice and rabbits.     

Effects of ginseng saponins isolated from red ginseng on ultraviolet B-induced skin aging in hairless mice

It is well-known that chronic ultraviolet B (UVB) exposure at low-dose causes skin photoaging including increases in skin thickness and wrinkle formation and reduction in skin elasticity. This study examined the effects of total saponins and ginsenoside Rb₁ isolated from Red Ginseng roots on skin thickness, elasticity, and wrinkle formation caused by long-term, low-dose UVB irradiation in hairless mice. The topical application of total ginseng saponins (10 pg or 100 ng/mouse) and ginsenoside Rb₁ (100 fg, 10 pg, or 1 ng/mouse) significantly inhibited increases in skin thickness and wrinkle formation and the reduction in skin elasticity induced by long-term UVB irradiation. Furthermore, we examined the histological effects of total saponins and ginsenoside Rb₁ in the skin of UVB-irradiated hairless mice. The increases in apoptotic, Ki-67-, and 8-hydroxy-2′-deoxyguanosine-positive cells induced by UVB exposure were prevented by the topical application of total saponins and ginsenoside Rb₁. Furthermore, total saponins and ginsenoside Rb₁ prevented the disruption of collagen fibers induced by the long-term UVB irradiation. Ginsenoside Rb₁ (100 fg, 10 pg, and 1 ng/ml) increased the Bcl-2 expression level in UVB-treated human keratinocytes. The protective effect of ginsenoside Rb₁ on UVB-mediated apoptosis may be due to the up-regulation of Bcl-2 expression. These results suggest that the protective effect of ginsenoside Rb₁ on skin photoaging induced by chronic UVB exposure may be due to the increase in collagen synthesis and/or the inhibition of matrix metalloproteinase expression in dermal fibroblasts.     

Two new dammarane-type triterpene saponins from red American ginseng

Two new dammarane-type triterpene saponins were isolated from the red American ginseng. The new saponins were named as pseudoginsenoside G₁ (1) and pseudoginsenoside G₂ (2). Their structures were elucidated by the combined analysis of NMR and mass spectrometry as 3-O-[β-d-glucopyranosyl-(1 → 2)-β-d-glucopyranosyl]-dammar-12-one-20S,24R-epoxy-3β,25-diol (pseudoginsenoside G₁) (1) and 3-O-[β-d-glucopyranosyl-(1 → 2)-β-d-glucopyranosyl]-dammar-12-one-20S,24S-epoxy-3β,25-diol (pseudoginsenoside G₂) (2).     

富集纯化前上样液参数影响三七皂苷类成分的研究

目的 考察富集纯化前上样液参数pH值、氯化钠浓度、时间等对三七皂苷类成分的影响.方法 用UV、TLSC分别测定3种不同上样液在不同时间段的三七总皂苷、人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1的含量.结果 3种上样液放置72 h后,人参皂苷Rg1含量均增加(P＜0.01);三七皂苷R1含量均减少(P＜0.05);人参皂苷Rb含量变化无差异;pH5.5上样液和pH 7.0上样液中的总皂苷含量均增加(P＜0.05),pH5.5且含4％氯化钠的上样液中总皂苷含量无明显变化.结论 在富集纯化过程中,上样液的pH值、无机盐浓度和时间对皂苷类成分含量变化有影响.     

巴曲酶对急性心肌缺血犬冠脉节段阻力和流量的影响

犬冠状动脉定量狭窄造成急性心肌缺血,观察巴曲酶(batroxobin)对冠脉循环及血流动力学的影响。结果显示,batroxobin可剂量依赖性地增加缺血心脏冠脉血流量,2BU·kg^-1(0.1BU·kg^-1·min^-1)iv后40min,缺血犬冠脉流量比盐水对照组增加12%,此时小冠脉阻力由4.1±0.5降至3.2±0.5mmHg·min·ml^-1,而大冠脉阻力无明显变化;给药后120min,上述作用仍然持续,且冠脉总阻力降低13%,左室压上升及下降最大速率与盐水对照组相比分别增大14%和16%。结果表明,batroXobin在冠脉低灌流状态下仍可降低小冠脉阻力,增加冠脉流量,这可能是其改善缺血犬冠状循环及心脏功能的机理之一。     

人参皂苷Rb1磷脂复合物的制备及其理化性质研究

目的:制备人参皂苷Rb1磷脂复合物,并研究其理化性质。方法:以人参皂苷Rb1与磷脂的复合率为评价指标,对制备工艺进行单因素考察,并采用正交实验设计对处方进行优化。利用紫外光谱法、差示扫描量热法等对所得的磷脂复合物进行鉴定。测定磷脂复合物中Rb1的含量,并考察磷脂复合物在不同体系中的表观油水分配系数。结果:人参皂苷Rb1与磷脂形成了分子型复合物。最佳制备方法的复合率为99.92%±0.14%,其中Rb1的含量在99.00%以上。磷脂复合物在不同体系中的表观油水分配系数与原药相比均显著增加。结论:确定了人参皂苷Rb1磷脂复合物的最佳制备工艺,并且其磷脂复合物明显的提高了原药的脂溶性。     

Formulation optimization of prostaglandin E1-loaded lipid emulsion: Enhanced stability and reduced biodegradation

The purpose of this study is to develop a new formulation for prostaglandin E₁ (PGE₁)-loaded lipid emulsion (Lipo-PGE₁) with improved stability and reduced biodegradation. High-pressure homogenization was used to prepare the Lipo-PGE₁, and high-performance liquid chromatography and accelerated test were used to evaluate its physicochemical stability. A tissue homogenate incubation test was firstly established and validated to assess its biodegradation. The factors influencing the stability of Lipo-PGE₁, including oil phase, emulsifier, pH value, and drug concentration were systematically investigated. The optimized formulation consisting of poloxamer188 1.5% (w/v), egg lecithin 0.5% (w/v), soybean oil 10.0% (w/v), oleic acid 0.24% (w/v), and glycerol 2.2% (w/v), with the pH value at 4.0, was defined and characterized. When compared with the currently available commercial product of Lipo-PGE₁, the degradation percentage of this optimized Lipo-PGE₁ reduced by 47.1% after sterilization, the drug remaining percentage increased by 13.9% after storage at 4°C over 6 months. Also, a significant reduction in biodegradation of the optimized Lipo-PGE₁ in comparison with the commercial Lipo-PGE₁ was observed by a tissue homogenate incubation test. Overall, we provided a novel formulation for Lipo-PGE₁ with a better physicochemical stability and a less biodegradation than the currently available commercial product of Lipo-PGE₁, indicating its potential superiority in clinical application.     

Inhibition of intestinal motility by the putative BK<Subscript>Ca</Subscript> channel opener LDD175

LDD175 (4-chloro-7-trifluoromethyl-10H-benzo[4,5]furo[3,2-b]indole-1-carboxylic acid) is a benzofuroindole compound characterized previously as a potent opener of the large conductance calcium activated (BK_Ca) channels. Activators of the BK_Ca channels are potential therapies for smooth muscle hyperactivity disorders. The present study investigates the influence of LDD175 on the mechanical activity of the ileum smooth muscle. LDD175 inhibited spontaneous contractions of the ileum in a concentration-dependent manner (pEC₅₀=5.9 ± 0.1) (E _max=96 ± 1.0% at 100 μM, n=3). It also remarkably inhibited contractions due to acetylcholine (ACh) (pEC₅₀=5.3 ± 0.1)(E _max=97.7 ± 2.3%, n=6) and electrical field stimulation (EFS) (pEC₅₀=5.5 ± 0.1) (E _max=83.3 ± 6.0%, n=6). In strips precontracted by 20 mM KCl, LDD175 significantly reduced the contractions yielding a pEC₅₀ of 6.1 ± 0.1 and E _max of 96.6 ± 0.9%, (n=6). In 60 mM KCl, a concentration-dependent inhibition was observed with respective pEC₅₀ and E _max values of 4.1 ± 0.1 and 50.8 ± 5.0% (n=3). BK_Ca channel blockers iberiotoxin (IbTX) and tetraethylammonium chloride (TEA, 1 mM) attenuated the relaxative effect of LDD175 but not barium chloride (BaCl₂), and glibenclamide (K_IR and K_ATP channel blockers, respectively). These data demonstrate the antispasmodic activity of LDD175 attributable to the potentiation of the BK_Ca channels.