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1、摘要 人参皂苷主要有原人参二醇(Protopanaxadiol, PPD) 型、原人参三醇( Protopanaxatriol, PPT) 型、齐墩果酸(Oleanic Acid, OA)型三种类型，其具有广泛的生物学活性，包括免疫调节、抗肿瘤、提高学习记忆、抗衰老、抗炎、抗痴呆、抗疲劳和促进造血等。但是人参皂苷本身不易被吸收，生物利用度较低。大量研究表明,人参皂苷在胃肠道去糖代谢后形成苷元或次苷，这些成分更容易被胃肠道吸收，且活性较皂苷增强。人参皂苷元混合物DS-1226系采用专有技术从人参茎叶中提取、水解、精制而成的一种类似人参皂苷肠代谢组合物的新型中药有效组份,该产品及技术已获得中国、美
2、国、加拿大、欧盟、台湾等8个国家或地区的授权专利,其主要成分为PPT(33 %)和PPD (16 %)。行为学实验表明DS-1226对睡眠干扰所致的学习记忆障碍具有改善作用，此外其还对化疗所致的骨髓抑制有保护作用。人参是五加科(Araliaceae) 人参属植物人参Panax ginseng C.A.Meyer的干燥根，是珍贵的中药材，始载于神农本草经，在我国药用历史悠久。人参主产于我国吉林的长白山等地区，具有大补元气、补脾益肺、生津、安神益智等功效-4。人参中含有多种类型的化学成分，如皂苷类、挥发油类、多糖类、氨基酸和多肽类、微量元素等，其中人参皂苷是主要的活性成分15。人参皂苷属于三萜类皂
3、苷，目前可分为三类6:-类为原人参二醇( Protopanaxadiol, PPD) 型，主要有人参皂苷Rb1、Rb2、 Rb3、 Rc、Rd、Rh2等;另一类为原人参三醇( Protopanaxatriol, PPT) 型，有人参皂苷Re、Rf、Rg1、Rg2、Rh1等;还有一类为齐墩果酸(Oleanic Acid, 0A)型，有人参皂苷Ro、Rh3、Ri、F4等。近年来，对于人参皂苷以及其代谢产物的药理作用、药动学特性的研究成为热点，并且发现人参皂苷的代谢产物，即次苷及其苷元，相对于天然皂苷更容易吸收入血，且具有更好的药理活性。因此，本文对人参皂苷及其苷元的药理活性、药动学研究进展进行综述
4、。关键词：人参皂苷，活性成分，药用研究Abstract：Ginsenosides mainly include Protopanaxadiol (PPD), Protopanaxatriol (PPT) and Oleanic Acid (OA), which have a wide range of biological activities, including Immune regulation, anti-tumor, improve learning and memory, anti-aging, anti-inflammatory, anti-dementia, anti-fati
5、gue and promote hematopoiesis. However, ginsenoside itself is not easily absorbed and its bioavailability is low. Numerous studies have shown that ginsenosides form aglycon or glucosides after glucosaccharide metabolism in the gastrointestinal tract. These components are more easily absorbed by the
6、gastrointestinal tract and are more active than saponins. The ginsenoside mixture DS-1226 is a novel traditional Chinese medicine active ingredient similar to the ginsenoside intestinal metabolite composition extracted, hydrolyzed and refined from the ginseng stems and leaves by proprietary technolo
7、gy. The product and technology have been obtained in China and the United States. Authorized patents in 8 countries and regions such as Canada, the European Union, and Taiwan, whose main components are PPT (33%) and PPD (16%). Behavioral experiments have shown that DS-1226 has an improved effect on
8、learning and memory impairment caused by sleep disturbance, and it also has a protective effect on myelosuppression induced by chemotherapy.Ginseng is the dry root of Panax ginseng C.A. Meyer, a ginseng plant of the Araliaceae family. It is a precious Chinese herbal medicine. It is contained in the
9、Shennong Bencao Classic and has a long history of medicinal use in China. Ginseng is mainly produced in Changbai Mountain and other areas in Jilin, China. It has the functions of replenishing vital energy, replenishing spleen and tonifying the lungs, producing fluid, and soothing the nerves. Ginseng
10、 contains many types of chemical components, such as saponins, volatile oils, polysaccharides, amino acids and peptides, trace elements, etc., of which ginsenoside is the main active ingredient 15. Ginsenoside belongs to triterpenoid saponins and can be divided into three types: 6:-type is Protosanx
11、adiol (PPD) type, mainly ginsenoside Rb1, Rb2, Rb3, Rc, Rd, Rh2, etc.; It is a protopanaxatriol (PPT) type, ginsenoside Re, Rf, Rg1, Rg2, Rh1, etc.; and one type is Oleanic Acid (0A) type, ginsenoside Ro, Rh3, Ri , F4, etc. In recent years, studies on the pharmacological effects and pharmacokinetic
12、properties of ginsenosides and their metabolites have become hot spots, and it has been found that the metabolites of ginsenosides, namely glucosides and their aglycones, are more easily absorbed into the blood than natural saponins, and Has better pharmacological activity. Therefore, this paper rev
13、iews the pharmacological activities and pharmacokinetics of ginsenosides and their aglycones.Key words: ginsenoside, active ingredient, medicinal research人参皂苷药理活性研究概况一、 抗肿瘤作用目前已发现人参皂苷Rg3、Rg1、Rhl、Rh2、Rb1等多种皂苷以及苷元PPD、PPT具有抗肿瘤活性11;14。这些成分在促进肿瘤细胞凋亡、抑制肿瘤细胞增殖、抑制肿瘤血管生成、逆转肿瘤多药耐药、抑制肿瘤细胞侵袭转移、影响肿瘤信号转导相关基因的表达、增
14、强肿瘤化放疗患者免疫力等方面均表现出一定的临床应用潜力,特别是在降低肿瘤患者放化疗副作用及增强肿瘤细胞对治疗药物敏感性方面尤为突出。金岩等人“探讨了人参皂苷Rb1、Rgl与5-氟脲嘧啶对地塞米松诱导S 180荷瘤小鼠脾淋巴细胞凋亡的影响。结果发现，人参皂苷Rb!与Rgl均能够抑制地塞米松对脾淋巴细胞诱导的凋亡，同时5- 氟尿嘧啶与人参皂苷Rb1无拮抗作用，而与人参皂苷Rg1有拮抗作用。原人参二醇型、原人参三醇型和齐墩果酸型人参皂苷的化学结构二、 抗痴呆近年来，人参皂苷治疗阿尔茨海默病(AD)正.F益受到重视，其机制主要与促进淀粉样蛋白(AB)形成的B-分泌酶和y-分泌酶、蛋白磷酶2A活性，抗氧
15、化及消除自由基有关。赵莹等研究了人参皂苷Re对自然衰老大鼠学习记忆功能的影响，并初步探讨其作用机制。结果发现，人参皂苷Re可显著对抗自然衰老引起的记忆获得障碍,对麻醉大鼠海马齿状回基础突触传递有增强作用，且能形成突触长时程增强形象。该作用可能与其增强基础突触传递、促进LTP形成有关。陈新梅等考察了人参皂苷Rg1脂质体(Rg1-L)对东莨菪碱诱导大鼠学习记忆障碍的改善作用，并对其相关机制探讨。结果表明，Rg1-L可以显著改善模型大鼠学习记忆功能，同时可抑制大脑皮质中乙酰胆碱酯酶活性。庄莹等探讨了人参皂苷Rg2对AB25-35诱导的阿尔茨海默病(AD)大鼠模型的学习记忆能力及老年斑(SP)形成的影
16、响。结果发现，模型组和空白组大鼠学习记忆能力较正常对照组有明显下降，人参皂苷Rg2各剂量预防给药组大鼠的学习记忆能力较模型组有所增强,模型组、空白组和低剂量组大鼠大脑皮质中有SP形成，呈均匀致密的嗜银团，其余各组均未观察到SP。三、 抗抑郁抑郁是由各种原因引起的以抑郁为主要症状的心境障碍或情感性障碍,包括注意缺失、睡眠障碍等，是-种高发病、高复发的疾病。目前研究发现人参皂苷对可通过调控中枢神经系统达到抗抑郁的药理活性。党海霞经研究发现，Rg1(50、100mg/kg)可明显对抗慢性应激引起的糖水偏爱指数下降、新奇环境下首次摄食时间延长，显示出一定的抗抑郁效应。在穿梭箱测试中，Rg1(50mg/kg)可对慢性应激刺激可引起大鼠穿梭箱测试中主动回避次数、反应速度和运动路程的下降以及被动回避次数、反应速度和运动路程的增加,体现出对抑郁症所致认知功能障碍的改善作用。通过HPLC-ECD、ELISA法和免疫组织化学法等实验，表明Rg1各剂量组可不同程度的拮抗慢性应激模型引起的大鼠海马和前额叶皮层N
