Yamasaki H
Acta Med Okayama. 1976 Feb;30(1):1-20.
The root and stem decoctions of Sinomenium acutum Rehd. et Wils. (formerly Sinomenium diversifolius Diels, one type of Fang-chi (Chinese)) have been used as a folk remedy for neuralgia and rheumatoid arthritis in many areas of the Far East. In Japan and China various viny plants have been identified as Fang-chi (Boi in Japanese) since antiquity. This uncertain nomenclature has made it difficult to evaluate the efficacy of the Fang-chi described in the classic literature. Among traditional Fang-chi plants only Sinomeniumacutum has been demonstrated to contain the alkaloid sinomenine, which is now known to be effective in neuralgia and rheumatic diseases. Sinomenine is a unique plant alkaloid, as it potently releases histamine in association with degranulation of tissue mast cells in mammalian tissues. This action occurs preferentially in the skin and joint capsules. The released histamine is responsible for the dominant pharmacological actions of sinomenine, such as vasodilatation, increased vascular permeability, acceleration of the thoracic and peripheral lymph flow, contraction of plain muscles, increased peristalsis of the intestines, and stimulation of gastric acid secretion. At toxic doses of sinomenine, convulsive central excitation was observed in most laboratory animals. Clinical side effects encountered with high doses of injected sinomenine or of decocted Sinomenium acutum were: injection site flare, pruritus in the head and upper part of the body, edema around the lips and eyelids, and temporary cephalalgia. Most of these side effects were reduced by classical antihistamines (H1-receptor antagonists). Daily subcutaneous injections of sinomenine for more than one week produced an analgesic effect in mice. Granulation tissue growth and adjuvant arthritis induced in rats were both inhibited by daily injections of a small dose of sinomenine hydrochloride or histamine dihydrochloride. These inhibitory effects were mediated through histamine H2-receptors probably on fibroblasts (for granulation tissue growth) and on T-cells (for adjuvant arthritis), since these effects were clearly inhibited by the H2-antagonist burimamide but not by the H1-antagonist mepyramine. The anti-rheumatic effect on Sinomenium acutum are probably genuine and can probably be attributed to the histamine-releasing properties of sinomenine.
青风藤（原称毛青藤，防己的一种）的根和茎煎剂在远东许多地区一直被用作治疗神经痛和类风湿性关节炎的民间药物。在日本和中国，自古以来各种藤本植物就被认定为防己（日语称“Boi”）。这种不确定的命名使得难以评估古典文献中所描述的防己的功效。在传统的防己植物中，只有青风藤被证明含有青藤碱，现已知道其对神经痛和风湿性疾病有效。青藤碱是一种独特的植物生物碱，因为它能在哺乳动物组织中与组织肥大细胞脱颗粒相关联地强力释放组胺。这种作用优先发生在皮肤和关节囊中。释放出的组胺是青藤碱主要药理作用的原因，如血管舒张、血管通透性增加、胸段和外周淋巴液流动加速、平滑肌收缩、肠道蠕动增加以及胃酸分泌受刺激。在大多数实验动物中，青藤碱达到中毒剂量时会观察到惊厥性中枢兴奋。高剂量注射青藤碱或青风藤煎剂时出现的临床副作用有：注射部位发红、头和身体上部瘙痒、嘴唇和眼睑周围水肿以及暂时性头痛。大多数这些副作用可通过经典的抗组胺药（H1受体拮抗剂）减轻。连续一周以上每日皮下注射青藤碱对小鼠产生了镇痛作用。每日注射小剂量盐酸青藤碱或二盐酸组胺可抑制大鼠肉芽组织生长和佐剂性关节炎。这些抑制作用可能是通过组胺H2受体介导的，可能作用于成纤维细胞（对肉芽组织生长而言）和T细胞（对佐剂性关节炎而言），因为这些作用明显被H2拮抗剂布立马胺抑制，而不被H1拮抗剂美吡拉敏抑制。青风藤的抗风湿作用可能是真实的，可能归因于青藤碱的组胺释放特性。
