Faculty of Life Science, Kyushu Sangyo University, Fukuoka, Japan.
Eur J Pharmacol. 2017 Nov 15;815:405-415. doi: 10.1016/j.ejphar.2017.09.049. Epub 2017 Sep 29.
Terpenes are made of the isoprene unit (C), and along with their derivatives, terpenoids, they are widely distributed in plants as active ingredients involved in anti-inflammation, anti-carcinogenesis and neuroprotection. Estrogenic terpenes and terpenoids are an important category of phytoestrogens and have been used as traditional medicines. The comprehensive list of estrogenic terpenes and terpenoids includes hemi-, mono-, sesqui-, di-, tri-, tetra- and polyterpenes, their derivatives, and meroterpenes, along with the signaling pathways and cellular functions on which their estrogenicity is exerted. Signaling pathways are further classified as bidirectional or unidirectional, the latter being further divided into two types depending upon the presence of both ligands, or the absence of one or both ligands. Although estrogenic activity of terpenes and terpenoids was evaluated by ligand-binding assays, yeast two-hybrid assays, reporter-gene assays, transcription assays, protein assays, cell assays and animal testing, the mechanism of estrogenic activity is still not fully understood. Applications of estrogenic terpenes and terpenoids are categorized into cancer treatment and prevention, cardioprotection, endocrine toxicity/reproductive dysfunction, food/supplement/traditional medicine, immunology/inflammation, menopausal syndromes and neuroprotection, where their benefits are discussed based on their availability, stability and variations.
萜类化合物由异戊二烯单元 (C) 组成，与其衍生物萜类化合物一起，广泛分布于植物中，作为参与抗炎、抗癌和神经保护的活性成分。具有雌激素活性的萜类化合物和萜类化合物是植物雌激素的一个重要类别，已被用作传统药物。具有雌激素活性的萜类化合物和萜类化合物的综合清单包括半萜、单萜、倍半萜、二萜、三萜、四萜和多萜、它们的衍生物以及混合萜，以及它们发挥雌激素作用的信号通路和细胞功能。信号通路进一步分为双向或单向，后者进一步分为两种类型，取决于配体的存在或缺乏一种或两种配体。尽管通过配体结合测定、酵母双杂交测定、报告基因测定、转录测定、蛋白质测定、细胞测定和动物试验评估了萜类化合物和萜类化合物的雌激素活性，但雌激素活性的机制仍未完全阐明。雌激素活性的萜类化合物和萜类化合物的应用分为癌症治疗和预防、心脏保护、内分泌毒性/生殖功能障碍、食品/补充剂/传统医学、免疫学/炎症、更年期综合征和神经保护，根据其可用性、稳定性和变化讨论了它们的益处。
