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    云連、雅連、味連|黃連與胡黃連的化學成分與藥理活性及

    時間:2023-08-09   瀏覽次數:  分享到:
    俗話說:“啞巴吃黃連,有苦難言”。中藥黃連味極苦,具有清熱燥濕、瀉火解毒等功效,在糖尿病的治療方面也具有獨特優勢。黃連的來源植物相對較多,“味連”、“雅連”、“云連”均在臨床上作為黃連使用。除此之外,胡黃連也有“黃連”之稱,也常被當作黃連使用。事實上,胡黃連與黃連是兩種不同的中藥,二者的化學成分和主治功效存在較大的差異。

    黃連(左)和胡黃連(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. 藥典收錄與性味歸經

    黃連始載于《神農本草經》,位列上品。2015版《中國藥典》規定黃連為毛茛科植物黃連 Coptis chinensis Franch.(味連)、三角葉黃連C. deltoidea C. Y. Cheng et Hsiao(雅連)或云連C. teeta Wall.(云連)的干燥根莖。黃連味苦,性寒;歸心、脾、胃、肝、膽、大腸經。

    胡黃連名出《新修本草》,為玄參科植物胡黃連Picrorhiza scrophulariiflora Pennell的干燥根莖,味苦,性寒;入肝、胃、大腸經。
    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. 黃連飲片的炮制

    黃連秋季采挖,除去須根和泥沙,干燥,撞去殘留須根。
    黃連味苦,臨床上一般使用其炮制品。其炮制方法為:除去雜質,潤透后切薄片,晾干,用黃酒、姜汁、醋、吳茱萸或豬膽汁炮制,分別得到酒黃連、姜黃連、醋黃連、萸黃連等。臨床上以酒黃連、姜黃連、萸黃連較為常用。
    胡黃連的炮制以生切為主。
    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. 黃連的化學成分

    黃連的化學成分包括生物堿類、木脂素類、黃酮類、有機酸等。生物堿類化合物為黃連的主要藥效成分,2015版《中國藥典》規定以小檗堿、表小檗堿、黃連堿、巴馬汀作為黃連的指標成分進行質量檢測。其中,小檗堿(黃連素)含量最高,可高達10%。“味連”、“雅連”、“云連”中小檗堿的含量略有差異,其中“云連”中小檗堿含量最高。相比于“雅連”和“云連”,“味連”中巴馬汀、黃連堿、表小檗堿、非洲防己堿含量較高,藥根堿含量較低。
    現已從黃連中鑒定到的木脂素主要包括(±)-5′-甲氧基松脂素、(±)-松脂醇、 (±)-落葉松樹脂醇、(±)-5′-甲氧基落葉松樹脂醇、(±)-異落葉松樹脂醇、(+) -異落葉松脂素、黃連木脂素A、黃連木脂素B等;黃連中的黃酮類化合物主要包括鼠李素、漢黃芩素3,5,7-三羥基-6,8-二甲基黃酮、2′,4,4′-三羥基-6′-甲氧基二氫查爾酮、7,4′-二羥基-5-甲氧基黃烷酮、6,8-二甲基-3,5,7-三羥基菲酮等;黃連中的有機酸類化合物主要有東莨菪素、原兒茶酸、阿魏酸、綠原酸、鄰二苯酚、乳酸、香草酸、龍膽酸等。
    胡黃連的化學成分主要包括胡黃連苦苷等環烯醚萜類、葫蘆素類和酚苷類化合物,與黃連中的化學成分差異顯著。
    黃連中的生物堿類化合物骨架
    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. 黃連的藥理活性

    黃連具有清熱燥濕,瀉火解毒的傳統功效,臨床用于主治濕熱痞滿、嘔吐吞酸、瀉痢、黃疸、高熱神昏、心火亢盛、心煩不寐、心悸不寧、血熱吐魈、目赤、牙痛、癰腫 疔瘡等癥,外用可治濕疹、濕瘡、耳道流膿?,F代藥理學研究表明黃連具有抗菌、消炎、抗腫瘤、抗氧化、調血脂、降血糖、抗心律失常等藥理活性。尤為值得注意的是,作為黃連指標成分的小檗堿,同時也是黃連的主要抗菌活性成分,季銨類生物堿的結構特點使其主要以鹽酸鹽(即鹽酸小檗堿,或鹽酸黃連素)的形式生產、使用,具有清熱燥濕、行氣止痛、止痢止瀉的藥效,抗菌譜廣,臨床主要用于治療痢疾、腸炎、眼結膜炎、化膿性中耳炎等,還因其具有阻斷α-受體的功能而用于治療心律失常。
    胡黃連具有保肝、利膽、抗炎、保護神經細胞、調節血糖、降血脂等作用,此外對心肌細胞的凋亡具有保護作用。

    鹽酸小檗堿的化學結構
    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.
    總之,黃連與胡黃連在化學成分及藥理活性方面均存在明顯差異,用途迥異。黃連作為一種重要的中藥材,具有清熱解毒、抗菌消炎和調節胃腸功能等臨床藥效,對感染性疾病、消化系統疾病、呼吸系統疾病和肝膽疾病均具顯著療效,應用范圍非常廣泛,市售以黃連為主要藥效成分的中成藥有雙黃連口服液、黃連雙清丸、牛黃上清丸、清胃黃連丸、黃連上清丸、黃連膠囊等。
    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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