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云连、雅连、味连|黄连与胡黄连的化学成分与药理活性及

时间:2023-08-09   浏览次数:  分享到:
俗话说:“哑巴吃黄连,有苦难言”。中药黄连味极苦,具有清热燥湿、泻火解毒等功效,在糖尿病的治疗方面也具有独特优势。黄连的来源植物相对较多,“味连”、“雅连”、“云连”均在临床上作为黄连使用。除此之外,胡黄连也有“黄连”之称,也常被当作黄连使用。事实上,胡黄连与黄连是两种不同的中药,二者的化学成分和主治功效存在较大的差异。

黄连(左)和胡黄连(右)
The proverbial expression ‘even a mute person can taste the bitterness of the coptis root and suffer in silence’ highlights the intense bitterness associated with coptis root (named Huang-Lian in Chinese), a Chinese herbal medicine renowned for its medicinal properties. This botanical remedy exhibits various therapeutic effects, including heat-clearing, dampness-drying, fire-purging, and detoxification, which render it particularly advantageous in the treatment of diabetes. Coptis root can be obtained from several plant species, such as Wei-Lian, Ya-Lian, and Yun-Lian, all of which are utilized in clinical practice as coptis. Moreover, hu coptis shares the same designation as coptis and is often used interchangeably. Nevertheless, it is important to recognize that hu coptis and coptis root are distinct traditional Chinese medicines, differing significantly in their chemical composition and primary therapeutic effects.

1. 药典收录与性味归经

黄连始载于《神农本草经》,位列上品。2015版《中国药典》规定黄连为毛茛科植物黄连 Coptis chinensis Franch.(味连)、三角叶黄连C. deltoidea C. Y. Cheng et Hsiao(雅连)或云连C. teeta Wall.(云连)的干燥根茎。黄连味苦,性寒;归心、脾、胃、肝、胆、大肠经。

胡黄连名出《新修本草》,为玄参科植物胡黄连Picrorhiza scrophulariiflora Pennell的干燥根茎,味苦,性寒;入肝、胃、大肠经
1. Pharmacopoeia Inclusion and Categorization
Huang-Lian was originally documented and classified as a top-grade herb in the Chinese ancient book Shen Nong Ben Cao Jing. According to the 2015 edition of Pharmacopoeia of the People's Republic of China, Huang-Lian specifically refers to the dried rhizome and root obtained from plants of the Ranunculaceae family, namely Coptis chinensis Franch. (Wei-Lian), Coptis deltoidea C. Y. Cheng et Hsiao (Ya-Lian), or Coptis teeta Wall. (Yun-Lian). Huang-Lian has a bitter taste and cold nature, and belongs to the meridians of the heart, spleen, stomach, liver, gallbladder and large intestine, according to traditional Chinese medicines. While Hu-Huang-Lian, first mentioned in the materia medica book Xin Xiu Ben Cao, refers to the dried rhizome and root of the plant Picrorhiza scrophulariiflora Pennell of the family Scrophulariaceae, has a bitter taste and cold nature, and belongs to the liver, stomach, and large intestine meridians.

2. 黄连饮片的炮制

黄连秋季采挖,除去须根和泥沙,干燥,撞去残留须根。
黄连味苦,临床上一般使用其炮制品。其炮制方法为:除去杂质,润透后切薄片,晾干,用黄酒、姜汁、醋、吴茱萸或猪胆汁炮制,分别得到酒黄连、姜黄连、醋黄连、萸黄连等。临床上以酒黄连、姜黄连、萸黄连较为常用。
胡黄连的炮制以生切为主。
2. Processing of Huang-Lian Slices
Huang-Lian is harvested during the autumn season. After the removal of adventitious roots and debris, it undergoes a drying process, during which any remaining adventitious roots are knocked off. Huang-Lian possesses a bitter taste, thus its processed products are frequently utilized in clinical applications. The processing procedure involves the elimination of impurities, followed by thin slicing of the herb after moistening and subsequent drying. Then it is subjected to processing with yellow wine, ginger juice, vinegar, Evodia rutaecarpa, or pig bile, resulting in various processed forms such as Jiu- Huang-Lian (wine-processed), Jiang-Huang-Lian (ginger-processed), Cu-Huang-Lian (vinegar-processed), and others. Among these, Jiu-Huang-Lian, Jiang-Huang-Lian and Cu-Huang-Lian are commonly employed in clinical practice. In contrast, Hu-Huang-Lian is primarily used in its raw form.

3. 黄连的化学成分

黄连的化学成分包括生物碱类、木脂素类、黄酮类、有机酸等。生物碱类化合物为黄连的主要药效成分,2015版《中国药典》规定以小檗碱、表小檗碱、黄连碱、巴马汀作为黄连的指标成分进行质量检测。其中,小檗碱(黄连素)含量最高,可高达10%。“味连”、“雅连”、“云连”中小檗碱的含量略有差异,其中“云连”中小檗碱含量最高。相比于“雅连”和“云连”“味连”中巴马汀、黄连碱、表小檗碱、非洲防己碱含量较高,药根碱含量较低。
现已从黄连中鉴定到的木脂素主要包括(±)-5′-甲氧基松脂素、(±)-松脂醇、 (±)-落叶松树脂醇、(±)-5′-甲氧基落叶松树脂醇、(±)-异落叶松树脂醇、(+) -异落叶松脂素、黄连木脂素A、黄连木脂素B等;黄连中的黄酮类化合物主要包括鼠李素、汉黄芩素3,5,7-三羟基-6,8-二甲基黄酮、2′,4,4′-三羟基-6′-甲氧基二氢查尔酮、7,4′-二羟基-5-甲氧基黄烷酮、6,8-二甲基-3,5,7-三羟基菲酮等;黄连中的有机酸类化合物主要有东莨菪素、原儿茶酸、阿魏酸、绿原酸、邻二苯酚、乳酸、香草酸、龙胆酸等。
胡黄连的化学成分主要包括胡黄连苦苷等环烯醚萜类、葫芦素类和酚苷类化合物,与黄连中的化学成分差异显著。
黄连中的生物碱类化合物骨架
3. Chemical Composition of Huang-Lian
The chemical constituents of Huang-Lian encompass alkaloids, lignans, flavonoids, and organic acids. Alkaloids serve as the primary bioactive constituents of Huang-Lian, and the 2015 edition of Pharmacopoeia of the People's Republic of China designates berberine, epiberberine, coptisine and palmatine as the reference compounds for evaluating the quality of Huang-Lian. Notably, berberine, also known as coptisine, displays the highest concentration, reaching up to 10%. Slight variations in berberine content exist among Wei-Lian, Ya-Lian and Yun-Lian, with Yun-Lian exhibiting the highest content. In comparison to Ya-Lian and Yun-Lian, Wei-Lian demonstrates elevated levels of palmatine, coptisine, epiberberine, and columbamine, while its jatrorrhizine content is relatively lower.
The lignans identified from Huang-Lian include (±)-5'-methoxypinosylvin, (±)-pinosylvinol, (±)-larch resinol, (±)-5'-methoxyresinol of larch, (±)-isoresinol of larch, (+)-isolariciresinol, coptis lignan A, and coptis lignan B. The flavonoids present in Huang-Lian mainly contain taxifolin, 3,5,7-trihydroxy-6,8-dimethylflavone, 2',4,4'-trihydroxy-6'-methoxydihydrochalcone, 7,4'-dihydroxy-5- methoxyflavanone, and 6,8-dimethyl-3,5,7-trihydroxyphenanthrene-1,4-dione. The organic acids identified from Huang-Lian primarily include catechic acid, ferulic acid, chlorogenic acid, resorcinol, lactic acid, vanillic acid, and gentiopicroside.
The chemical constituents of Hu-Huang-Lian primarily include sesquiterpene lactones such as hu coptis glucoside, cucurbitacins, and phenolic glycosides. These compounds exhibit significant differences compared to the chemical constituents found from Huang-Lian.

4. 黄连的药理活性

黄连具有清热燥湿,泻火解毒的传统功效,临床用于主治湿热痞满、呕吐吞酸、泻痢、黄疸、高热神昏、心火亢盛、心烦不寐、心悸不宁、血热吐魈、目赤、牙痛、痈肿 疔疮等症,外用可治湿疹、湿疮、耳道流脓。现代药理学研究表明黄连具有抗菌、消炎、抗肿瘤、抗氧化、调血脂、降血糖、抗心律失常等药理活性。尤为值得注意的是,作为黄连指标成分的小檗碱,同时也是黄连的主要抗菌活性成分,季铵类生物碱的结构特点使其主要以盐酸盐(即盐酸小檗碱,或盐酸黄连素)的形式生产、使用,具有清热燥湿、行气止痛、止痢止泻的药效,抗菌谱广,临床主要用于治疗痢疾、肠炎、眼结膜炎、化脓性中耳炎等,还因其具有阻断α-受体的功能而用于治疗心律失常。
胡黄连具有保肝、利胆、抗炎、保护神经细胞、调节血糖、降血脂等作用,此外对心肌细胞的凋亡具有保护作用。

盐酸小檗碱的化学结构
4. Pharmacological Activities of Huang-Lian
Traditionally, Huang-Lian possesses therapeutic effects of clearing heat, drying dampness, purging fire, and detoxification, and it is used to treat conditions such as damp-heat obstructing the middle burner, vomiting with acid regurgitation, diarrhea, jaundice, high fever with delirium, excessive heart fire, restlessness and insomnia, palpitations and uneasiness, vomiting blood due to heat, red eyes, toothache, abscesses, and boils in clinical practice. Topically, it can be used to treat eczema, moist sores, and purulent discharge from the ear canal. It has been revealed by modern pharmacological studies that Huang-Lian possesses pharmacological activities such as hypoglycemic, antimicrobial, antioxidant, anti-inflammatory, anticancer, regulation of blood lipids, and antiarrhythmic effects.
It is worthy to note that berberine, as an indicator component of Huang-Lian, is also the main antibacterial active ingredient of the title plant. The structural characteristics of quaternary alkaloids make it mainly produced and used in the form of hydrochloride (berberine hydrochloride), which has a wide antimicrobial spectrum, and is mainly used for the treatment of dysentery, enteritis, ocular and conjunctival inflammation, purulent otitis media and so on. It is also used in the treatment of cardiac arrhythmia due to its role in blocking α-receptors.
The activities of Hu-Huang-Lian revealed by modern pharmacology include hepatoprotective, choleretic, anti-inflammatory, neuroprotective, blood sugar-regulating and lipid-lowering. Furthermore, it was discovered that Hu-Huang-Lian exhibit a protective effect against apoptosis in myocardial cells.
总之,黄连与胡黄连在化学成分及药理活性方面均存在明显差异,用途迥异。黄连作为一种重要的中药材,具有清热解毒、抗菌消炎和调节胃肠功能等临床药效,对感染性疾病、消化系统疾病、呼吸系统疾病和肝胆疾病均具显著疗效,应用范围非常广泛,市售以黄连为主要药效成分的中成药有双黄连口服液、黄连双清丸、牛黄上清丸、清胃黄连丸、黄连上清丸、黄连胶囊等。
In conclusion, Huang-Lian and Hu-Huang-Lian differ significantly in their chemical composition and pharmacological activities, resulting in distinct applications. Huang-Lian, as a significant traditional Chinese medicine, exhibits clinical effects including heat-clearing, detoxification, antimicrobial, anti-inflammatory, and regulation of gastrointestinal function. It demonstrates obviously therapeutic efficacy in infectious diseases, digestive disorders, respiratory conditions, and liver and gallbladder ailments. To date, Huang-Lian is widely utilized and can be found in various commercially available Chinese patent medicines, such as Shuang-Huang-Lian oral solution, Huang-Lian-Shuang-Qing pills, Niu-Huang-Shang-Qing pills, Qing-Wei-Huang-Lian pills, Huang-Lian-Shang-Qing pills, and Huang-Lian capsules.


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