Antimicrobial activities of Asian ginseng,American ginseng,and notoginseng

Asian ginseng (Panax ginseng C.A. Meyer), American ginseng (Panax quinquefolius) and notoginseng (Panax notoginseng) are the three most commonly used ginseng botanicals in the world. With the increasing interests on antimicrobial properties of plants, the antimicrobial activities of ginseng species have been investigated by a number of researchers worldwide. This overview interprets our present knowledge of the antimicrobial activities of the three ginseng species and some of their bioactive components against pathogenic bacteria (Pseudomonas aeruginosa, Helicobacter pylori, Staphylococcus aureus, Escherichia coli, Propionibacterium acnes, et al.) and fungi (Candida albicans, Fusarium oxysporum, et al). Ginsenosides, polysaccharides, essential oil, proteins, and panaxytriol are all might responsible for the antimicrobial activities of ginseng. The antimicrobial mechanisms of ginseng components could be summarized to the following points: (a) inhibit the microbial motility and quorum‐sensing ability; (b) affect the formation of biofilms and destroy the mature biofilms, which can weaken the infection ability of the microbes; (c) perturb membrane lipid bilayers, thus causing the formation of pores, leakages of cell constituents and eventually cell death; (d) stimulate of the immune system and attenuate microbes induced apoptosis, inflammation, and DNA damages, which can protect or help the host fight against microbial infections; and (e) inhibit the efflux of antibiotics that can descend the drug resistance of the microbial. The collected information might facilitate and guide further studies needed to optimize the use of ginseng and their components to improve microbial food safety and prevent or treat animal and human infections.     

中国红参化学成分的研究

目的:研究五加科人参属常用中药红参的化学成分.方法:采用硅胶柱色谱、反相柱色谱、Sephadex LH-20柱色谱、半制备液相色谱等方法分离纯化,根据理化性质和波谱鉴定化合物的结构.结果:从红参中分离并鉴定了14个化合物,结构分别为:三七皂苷R2(1),20(S)-人参皂苷Rg3(2),20(R)-人参皂苷Rg3(3),20(S)-人参皂苷Rg2(4),20(R)-人参皂苷Rg2(5),20(S)-人参皂苷Rh1(6),20(R)-人参皂苷Rh1(7),人参皂苷Rh4(g),-R.(9),-Rb1(10),-Rg1(11),-Re(12),-Rf(13),麦芽酚(14).结论:化合物1,4,6为首次从红参中分到的人参皂苷类成分.化合物2与3,4与5,6与7分别为3对对映异构体,其中对映异构体6与7为首次分离得到的单体.     

中国红参化学成分研究

采用大孔吸附树脂、硅胶等柱色谱以及反相高效液相色谱等方法系统性分离、纯化中国红参的化学成分,根据MS、NMR等谱学数据鉴定其结构。从中国红参的水煎液中分离得到52个三萜皂苷类化合物,分别鉴定为20(S)-人参皂苷Rh1(1),20(R)-人参皂苷Rh1(2),人参皂苷Rg6(3),20(22)E-人参皂苷F4(4),人参皂苷Rk3(5),20(22)E-人参皂苷Rh4(6),人参皂苷Rg1(7),20(S)-人参皂苷Rf-1a(8),20(S)-人参皂苷Rf(9),20(R)-人参皂苷Rf(10),20(S)-三七皂苷R2(11),20(R)-三七皂苷R2(12),20(S)-人参皂苷Rg2(13),20(R)-人参皂苷Rg2(14),人参皂苷Rs2(15),人参皂苷Rs1(16),人参皂苷Rd(17),三七皂苷R1(18),人参皂苷Re2(19),人参皂苷Re(20),20-葡萄糖基人参皂苷Rf(21),西洋参皂苷R1(22),人参皂苷Ro-甲酯(23),人参皂苷Ro(24),人参皂苷Rb1(25),人参皂苷Rc(26),人参皂苷Rb2(27),人参皂苷Ra2(28),人参皂苷Ra3(29),人参皂苷Rb3(30),20(22)Z-人参皂苷Rh4(31),竹节参苷IVa丁酯(32),20(22)Z-人参皂苷Rs4(33),人参皂苷Rs5(34),20(22)E-人参皂苷Rs4(35),姜状三七苷R1-6'-丁酯(36),竹节参苷IVa甲酯(37),20(S)-人参皂苷Rs3(38),20(R)-人参皂苷Rs3(39),姜状三七苷R1-6'-甲酯(40),人参皂苷Rz1(41),人参皂苷Rk1(42),人参皂苷Rg5(43),23-O-甲基人参皂苷Rg11(44),12β,25-二羟基达玛-20(22)E-烯-3-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷(45),20(22)Z-人参皂苷F4(46),3β,12β-二羟基达玛-20(22)E,24-二烯-6-O-β-D-吡喃木糖基-(1→2)-O-β-D-吡喃葡萄糖苷(47),20(S)-人参皂苷Rg3(48),20(R)-人参皂苷Rg3(49),20(22)E-人参皂苷Rg9(50),人参皂苷Ro-6'-丁酯(51),聚乙炔基人参皂苷Ro(52)。化合物8,12,31~33,36,37,44,45,47,51为首次从人参中分离得到;化合物19,23,46为首次从红参中分离得到。     

锈腐病和受伤原料参对红参品质的影响研究

目的比较锈腐病鲜参、受伤鲜参与正常鲜参加工而成的红参品质,为人参加工利用提供依据。方法测定锈腐病鲜参、受伤鲜参和正常鲜参加工而成的红参中10种人参皂苷、总灰分、酸不溶性灰分、挥发性醚浸出物和总蛋白、糖类成分的量。结果锈腐病鲜参、受伤鲜参加工而成的红参中的总灰分、酸不溶性灰分、挥发性醚浸出物、蔗糖量都显著高于正常鲜参加工而成的红参,而10种人参皂苷量均显著低于正常鲜参加工而成的红参。结论锈腐病、受伤原料参对其加工后红参质量有显著影响。     

基于高分离度和对照图谱的红参中9种人参皂苷类成分“一测多评”质量评价研究

采用反相高效液相色谱法,Ultimate~C_(18)色谱柱,对红参中9种人参皂苷类成分进行了具有高分离度和高色谱峰纯度的同步色谱分离。采用"一测多评"中药质量评价模式,经一系列方法学考察,以人参皂苷Rb_1为内参物,建立了人参皂苷Rg_1,Re,Rf,Rb_1,Rc,Rb_2,Rb_3,Rd和20(S)-人参皂苷Rg3与人参皂苷Rb1间的相对校正因子与相对保留值,在红参对照图谱的辅助定位下,最终实现了仅采用人参皂苷Rb1一个中药对照品对红参中上述9种人参皂苷类成分的同步质量控制。     

不同规格红参中皂苷的比较分析

目的:测定几种不同规格中国红参主根及须根中人参皂苷Rg₁,Re,Rb₁,Rc,Rb₂,Rd的含量。方法:应用超声波提取法及反相高效液相色谱法分析。结果:6种皂苷的和分别为15支(每500 g)1.21%,20支1.46%,30支1.54%;红参须根8.16%。结论:人参根随着体积增大,皂苷含量减少。     

HPLC法同时测定林下参、鲜人参、生晒参和红参中14种人参皂苷

目的 建立同时测定林下参、鲜人参、生晒参和红参中14种中性和酸性皂苷量的方法.方法 采用反相高效液相色谱法,以COSMOSIL 5 C18-MS柱(250 mm× 4.6 mm,5 μm)为分析柱,乙腈-0.05 mol/L磷酸二氢钾溶液为流动相梯度洗脱,柱温25℃,体积流量为1 mL/min,检测波长203 nm.结果 人参皂苷在0.010～0.640 mg/mL内线性关系良好;加样回收率为97.4％～103.6％.结论 本法简便、准确、分离度好,可作为林下参、鲜人参、生晒参和红参的质量评价的方法,并首次发现了林下参中酸性皂苷的存在.     

基于细胞凋亡表达的生晒参、红参和西洋参四性研究展望

中药四性的研究一直是困扰中医药界的热点和难点问题,迄今未取得实质性的进展,严重影响了中医药现代化的进程.把细胞凋亡学应用于中药四性的研究,定性定量刻画中药四性的生物学效应与细胞凋亡的关系.从细胞分子水平建立一个中药四性的模式识别系统,将成为衡量中药四性的一个新突破.结合国内外大量文献研究和本课题组的研究基础,对中药四性的发展和定位提出新的观点和思路,对中药四性的研究进行评述和前瞻性分析.     

Polyprenylated benzophenones from Garcinia assigu and their potential cancer chemopreventive activities

In a further study on the chemical constituents of Garcinia assigu, two new benzophenones corresponding to the 13-O-methyl ethers (1 and 2) of the known isogarcinol and garcinol, respectively, were isolated and characterized, along with known benzophenones (3-6). Inhibitory effects of the benzophenones isolated from this plant on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells and their radical-scavenging ability against 1,1-diphenyl-2-picrylhydrazyl (DPPH) were demonstrated. The cyclized polyprenylbenzophenones (1-5) showed comparable or stronger potential cancer chemopreventive activity when compared to glycyrrhetic acid, a known anti-tumor promoter.     

不同移栽制红参品质的初步比较研究

目的:比较不同移栽制红参的品质,为人参栽培和加工利用提供依据.方法:测定不同移栽制红参中10种人参皂苷、总灰分、酸不溶性灰分、挥发油、挥发性醚浸出物和总蛋白含量.结果与结论:不同移栽制红参总灰分＜5.0％,酸不溶性灰分＜0.3％;且不同移栽制红参中人参皂苷Rg1,Re,Rb1的含量均符合《中国药典》(2010年版)规定.     

红参正果挥发油的GC MS分析

目的:研究红参正果挥发油的化学成分,为其质量评价提供科学依据.方法:采用水蒸气蒸馏法提取红参正果挥发油,毛细管GC法进行分离,归一化法测定其相对含量,MS法鉴定化学成分.结果:检出195个色谱峰,鉴定出76个化合物,占挥发油总量的78.27%.结论:红参正果挥发油的主要成分为倍半萜类,有24个单萜和倍半萜类化合物为首次从红参挥发油中分检测到.     

Korean red ginseng (Panax ginseng) improves insulin sensitivity in high fat fed Sprague-Dawley rats

Many studies have documented that ginseng has antidiabetic and antiobesity effects, but the mechanism of the effects has not been elucidated. The aim of this study was to determine the effect of Korean red ginseng (KRG, Panax ginseng) and investigate the mechanism of antidiabetic and antiobesity effects in obese insulin resistant animal models. Sprague‐Dawley (SD) rats were divided into three groups: a control group (group I) fed a normal diet, another group (group II) fed only high fat diet (HFD) and a third group (group III) fed HFD with KRG (200 mg/kg, oral) for 18 weeks. The body weight, food intake, adipose tissues, liver, kidney, pancreas, adiponectin, and leptin were measured. Blood glucose, insulin tolerance test, and hyperinsulinemic euglycemic clamp test were investigated. A significant weight reduction, especially fat mass reduction, was observed in the KRG treated group. Increased insulin sensitivity was found in the KRG treated group. We observed increased insulin signalling, increased phosphorylation of IR, IRS‐1, Akt, and membranous GLUT4 in muscle by Western blotting assay. In conclusion, KRG may have antidiabetic and antiobesity effects due to partly increased insulin sensitivity by increased adipokine and partly enhanced insulin signalling. Copyright © 2011 John Wiley & Sons, Ltd.     

Cancer chemopreventive agents (antitumor-promoters) from Ajuga decumbens.

Sixteen compounds (1-16) isolated from the flowering whole plant of Ajuga decumbens have been tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induction by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA), as a primary screening test for antitumor-promoters (potential cancer chemopreventive agents). Five compounds (6, 9, and 12-14) showed strong inhibitory effects on EBV-EA induction. Of these active compounds, two major constituents of this plant, cyasterone (6) and 8-acetylharpagide (13), showed potent antitumor-promoting activities on a mouse-skin in vivo two-stage carcinogenesis procedure, using 7, 12-dimethylbenz[a]anthracene as initiator and TPA as promoter. Further, compound 13 also exhibited potent chemopreventive activity in a mouse pulmonary tumor model.     

Cancer chemopreventive agents. New depsidones from Garcinia plants.

In a search for cancer chemopreventive agents from natural sources, chemical constituents of two kinds of Garcinia plants, Garcinia neglecta and Garcinia puat, collected in New Caledonia, were examined. Five new depsidones, garcinisidone-B (2), -C (3), -D (4), -E (5), and -F (6), were isolated, and their structures were determined by spectrometric analyses. Inhibitory effects of these depsidones on EBV-EA activation induced by TPA in Raji cells were also demonstrated.     

Effects of red ginseng extract on sleeping behaviors in human volunteers

Ethnopharmacological relevence

The ginseng root has been traditionally used as a sedative in oriental countries. However, the condition “ginseng abuse syndrome” (GAS), defined as hypertension, nervousness, sleeplessness, skin eruption, and morning diarrhea, was coined as a result of a study of people who had been using a variety of ginseng preparations. However, we reported that administration of RGE increased rapid eye movement (REM) and non rapid eye movement (NREM) sleep via GABAergic systems in animals. Therefore, this study was performed to investigate how red ginseng extract (RGE) affects sleeping behaviors in human volunteers.

Materials and methods

RGE (1500 mg) was orally administered to young male healthy volunteers (from 15 to 37 years old ages, n=15) three times a day for 7 days. Overnight polysomnographic (PSG) studies were performed two times, 1 day before and 7 days after RGE administration. We investigated differences in sleep architecture parameters such as total sleep time (TST), sleep efficacy (SE: total sleep time/time in bed), proportion of each sleep stage, and wakefulness after sleep onset (WASO) between baseline PSG and PSG after RGE administration.

Results

Total wake time (TWT) was significantly reduced (P<0.05) and SE was increased (P<0.05), although slow wave sleep stage 1 (N1) was reduced (P<0.01) and non-rapid eye movement (REM) sleep was increased (P<0.03) after administration.

Conclusion

From these results, it is presumed that RGE intake would improve the quality of sleep, thus having beneficial effects on sleep disturbed subjects.     

红参皂苷组分对大鼠血浆中神经化学物质的影响

目的考察红参皂苷组分A和B对大鼠血浆中15种神经化学物质水平的影响。方法将红参总皂苷经大孔吸附树脂分离纯化制备得到皂苷组分A和B,采用高效液相色谱-质谱法(UPLC-Q-TOF-MS/MS)测定其中皂苷成分的组成和量,并采用超高效液相色谱-三重四级杆质谱(UPLC-QQQ-MS/MS)测定大鼠血浆中多巴胺(DA)、肾上腺素(E)、去甲肾上腺素(NE)、5-羟色胺(5-HT)、5-羟吲哚乙酸(5-HIAA)、酪氨酸(Tyr)、甘氨酸(Gly)、谷氨酸(Glu)、谷氨酰胺(Gln)、天冬氨酸(Asp)、牛磺酸(Tau)、丝氨酸(Ser)、色氨酸(Try)、乙酰胆碱(Ach)、组胺(His)共15种神经化学物质的量及其变化情况。结果通过对皂苷组成和量与神经化学物质之间的内在联系分析,发现组分A和B在皂苷成分组成方面存在明显差异,极性较大皂苷类成分主要集中在组分A中,而组分B中含有的皂苷成分极性相对较小。组分A各剂量组的大鼠血浆中Ach、Tau、Glu、Gln、Asp、Tyr、E、NE、DA的量升高,组分B各剂量组的大鼠血浆中Gly、His、5-HT、Ser、5-HIAA、Try的量显著升高,并且与给药剂量呈正相关趋势,提示极性较大皂苷组分可提高兴奋性神经化学物质的量,而极性较小皂苷组分表现为提高抑制性神经化学物质的量。结论红参皂苷对中枢神经化学物质的量具有调节作用,极性较小的皂苷组分与保持大脑活动、改善记忆功能、防止脑部疲劳、维持觉醒状态和神经系统抗衰老等作用相关性较大,而极性较大的皂苷组分与调节精神节律、削弱应激反应和改善睡眠等作用相关性较大。     

Korean red ginseng stimulates insulin release from isolated rat pancreatic islets

Ethnopharmacological relevance

Korean red ginseng (KRG), one of heat-processed Korean ginseng (Panax ginseng C.A. Meyer), has a long history as herbal remedy for antidiabetic effect.

Aim of the study

The effect and mechanism of KRG on stimulation of insulin release were investigated in isolated rat pancreatic islets.

Material and methods

Pancreatic islets isolated from rats were used to evaluate the insulinotropic action of KRG. The effect of Ca on the insulinotropic action of KRG was investigated.

Results

The aqueous ethanolic extract of KRG (AEE-KRG) (0.1–1.0 mg/ml) significantly evoked a stimulation of insulin release at 3.3 mM glucose compared to the control. Experiments at different glucose concentrations (8.4 and 16.7 mM) showed that AEE-KRG significantly stimulated on its own whereas it did not potentiate insulin secretion induced by glucose. The extracellular Ca²⁺-free condition, a L-type Ca²⁺ channel blocker and an ATP-sensitive K⁺ channel opener significantly inhibited insulin secretion evoked by AEE-KRG.

Conclusion

These findings suggest that KRG displays beneficial effects in the treatment of diabetes at least in part via the stimulation of insulin release in a glucose-independent manner.     

红参对糖尿病大鼠视网膜微血管病变细胞外基质的影响

目的探讨红参对糖尿病大鼠视网膜微血管病变细胞外基质的影响.方法用链脲佐菌素(65mg/kg)一次性腹腔注射的方法建立糖尿病大鼠模型,30只SD大鼠随机分成对照组、模型组和红参干预组.红参粉末(每日1.5g/kg)灌胃给药.210天后处死动物摘除眼球,进行血管铺片形态学观察及纤连蛋白(FN)和层粘连蛋白(LN)在视网膜血管的表达,用图像分析仪测定免疫组化显色强度,进行定量分析.结果7个月糖尿病大鼠视网膜毛细血管细胞外基质增生明显,FN和LN均呈高表达(P＜0.05).红参干预后FN表达比模型组明显降低(P＜0.05),LN表达比模型组降低,但组间对比差异不显著.结论红参可抑制细胞外基质成分过度表达,从而减轻毛细血管基底膜的损伤.     

基于近红外光谱的红参提取过程动态预测模型研究

目的：利用近红外光谱技术,建立红参提取过程中关键组分的定量模型,实现快速检测功能;以近红外光谱为基础,结合动力学方程,建立提取过程动态趋势模型,实现全过程预测功能。方法：在线采集红参提取液近红外光谱,以HPLC获取关键成分数据,使用最小二乘法（PLSR）建立红参总皂苷的定量模型;通过定量模型以及近红外光谱,结合传质动力学方程,拟合建立提取过程随时间的动态关系模型,实现提取过程预测。结果：红参总皂苷定量模型的校正集相关系数r、校正均方根误差RMSEC、预测均方根误差RMSEP分别为0.996 09,0.018 9,0.016 8;以红参提取一阶动力学方程结合NIR定量模型建立提取过程趋势预测模型,模型显示趋势预测性能良好,具有较高的精度。结论：近红外法获得的定量模型拥有较好的检测精度,能实现快速在线检测功能;所建立的全过程提取动力学方程与实际提取过程趋势较为契合,满足预测需求。