OncoWitan, Scientific Consulting Office, 59290 Lille, France.
Biomolecules. 2022 Jan 23;12(2):192. doi: 10.3390/biom12020192.
The dried flower buds of the plant Sieb. et Zucc. have been largely used in traditional Chinese medicine for the treatment of inflammatory diseases. Numerous diterpenoids have been isolated from the Genkwa Flos (yuanhua in Chinese), including a series of daphnane-type diterpene designated as yuanhuacin (YC, often improperly designated as yuanhuacine) and analogues with a patronymic name. The series includes ten daphnane-type diterpenes: yuanhuacin, yuanhuadin (YD), yuanhuafin (YF), yuanhuagin (YG), yuanhuahin (YH), yuanhuajin (YJ), yuanhualin (YL), yuanhuamin (YM), yuanhuapin (YP), and yuanhuatin (YT). They are distinct from the rare flavonoid yuanhuanin. The series comprises several anticancer agents, such as the lead compound YC, which has revealed potent activity in vitro and in vivo against models of lung and breast cancers. The main signaling pathways implicated in the antitumor effects have been delineated. Protein kinase C is a key factor of activity for YC, but in general the molecular targets at the origin of the activity of these compounds remain little defined. Promising anticancer effects have been reported with analogues YD and YT, whereas compounds YF and YP are considered more toxic. The pharmacological activity of each compound is presented, as well as the properties of Genkwa Flos extracts. The potential toxic effects associated with the use of these compounds are also underlined.
该植物的干花蕾在传统中药中被广泛用于治疗炎症性疾病。已经从芫花（yuanhua，中文名称）中分离出许多二萜类化合物，包括一系列被命名为芫花素（YC，通常错误地命名为芫花素）及其类似物。该系列包括十种达芙烷型二萜类化合物：芫花素、芫花定（YD）、芫花瑞醇（YF）、芫花苷（YG）、芫花亭（YH）、芫花京尼醇（YJ）、芫花瑞醇（YL）、芫花胺（YM）、芫花配基（YP）和芫花亭（YT）。它们与罕见的黄酮yuanhuanin 不同。该系列包括几种抗癌剂，如先导化合物 YC，它在体外和体内对肺癌和乳腺癌模型均显示出强大的活性。已经描绘了涉及抗肿瘤作用的主要信号通路。蛋白激酶 C 是 YC 活性的关键因素，但一般来说，这些化合物活性的分子靶标仍未明确。已经报道了类似物 YD 和 YT 具有有希望的抗癌作用，而化合物 YF 和 YP 则被认为毒性更大。本文介绍了每种化合物的药理活性以及芫花提取物的性质。还强调了与使用这些化合物相关的潜在毒性作用。
