Department of Chemistry, Faculty of Science and Mathematics, University of Niš, Višegradska 33, 18000 Niš, Serbia.
Curr Med Chem. 2013;20(18):2273-95. doi: 10.2174/0929867311320180001.
Among 484 Hypericum L. (Guttiferae/Hypericaceae) species, widespread in warm temperate areas throughout the world, only H. perforatum is widely used in official medicine. Hypericum perforatum has been reported as an antidepressant, antiviral, antimicrobial, anti-inflammatory, and a healing agent. The main constituents of the Hypericum species are naphthodianthrones, primarily represented by hypericin and pseudohypericin, phloroglucinol derivatives, especially hyperforin, and flavonoids, such as quercetin, quercitrin, hyperoside and rutin. Hypericin and pseudohypericin have been found to possess antiretroviral activity. Hyperforin may also have an important contribution to the antidepressant activity of Hypericum extracts. The content of the above active constituents in some Hypericum species is higher than in H. perforatum. Also, a number of studies of the biological activities of Hypericum species have shown that the most recognized species of this genus, H. perforatum, was not the most active. Comprehensive analysis of the published research on the chemical composition and biological activity, showed that H. richeri has a similar pharmacological potential as St. Jon's wort. The species, with high content of naphtodianthrones,which might be used against viruses and retroviruses, are: H. androseamum,H. annulatum, H. barbatum, H. boissieri, H. elegans, H. hirsutum, H. hyssopifolium, H. humifusum, H. montanum. H. montbretii, H. triquetrifolium, H. richeri, H. rochelii, H. rumeliacum, H. thasium, andH. patulum. Very few species (e.g. H. inodorum and H. moseranum) contained the similar amounts of hyperforine as H. perforatum. Since hyperforin was recognized as one of the most crucial components for the antidepressive activity, it seems that H. perforatum barely has an alternative for this purpose. Plant species containing considerable amounts of other acylphloroglucinol derivatives have the potential to demonstrate antibacterial and cytotoxic activity. Some of these species are: H. sampsonii, H. ascyron, H. foliosum, H. geminiflorum and H. scabrum. However, only a few studies concerning the activity of extracts and isolated compounds were done in vivo. Also, data on the safe usage of Hypericum constituents as phytotherapeutics are scarce. Since some of Hypericum species are scarcely distributed or endemic as well as some of the secondary metabolites are presented in very small amounts, bio-production, especially endophytes, could represent an abundant and reliable source of pharmacologically active metabolites of Hypericum species for exploitation in pharmaceutical industry.
在 484 种贯叶金丝桃属（藤黄科/金丝桃科）植物中，只有贯叶连翘在世界范围内广泛应用于官方药物。贯叶连翘已被报道具有抗抑郁、抗病毒、抗菌、抗炎和愈合作用。金丝桃属植物的主要成分是萘并二蒽酮，主要由金丝桃素和伪金丝桃素、间苯三酚衍生物组成，特别是金丝桃素，以及类黄酮，如槲皮素、槲皮苷、圣约翰草苷和芦丁。已发现金丝桃素和伪金丝桃素有抗逆转录病毒活性。金丝桃素可能对贯叶连翘提取物的抗抑郁活性也有重要贡献。一些金丝桃属植物中上述活性成分的含量高于贯叶连翘。此外，对金丝桃属植物生物活性的大量研究表明，该属最具代表性的物种贯叶连翘并非最活跃。对已发表的化学成分和生物活性研究进行综合分析表明，里舍尔金丝桃具有与圣约翰草类似的药理学潜力。该物种含有高含量的萘并二蒽酮，可能用于对抗病毒和逆转录病毒，包括：贯叶金丝桃、倒卵叶金丝桃、贯叶连翘、绒毛贯叶连翘、秀丽金丝桃、绒毛金丝桃、腺梗金丝桃、密花金丝桃、高山金丝桃、蒙氏金丝桃、三叶金丝桃、里舍尔金丝桃、罗氏金丝桃、罗马尼亚金丝桃、披针叶金丝桃、平卧金丝桃。只有少数物种（例如，绒毛贯叶连翘和柔毛金丝桃）与贯叶连翘含有相似数量的金丝桃素。由于金丝桃素被认为是抗抑郁活性的最关键成分之一，因此似乎贯叶连翘在这方面几乎没有替代品。含有相当数量其他酰基间苯三酚衍生物的植物物种具有展示抗菌和细胞毒性活性的潜力。这些物种包括：长柱金丝桃、长梗金丝桃、多花金丝桃、全缘金丝桃和绒毛金丝桃。然而，仅进行了少数关于提取物和分离化合物的体内活性研究。此外，关于贯叶金丝桃属成分作为植物疗法的安全使用的数据也很少。由于一些金丝桃属物种分布稀少或特有，以及一些次生代谢产物的含量非常低，因此生物生产，特别是内生菌，可能代表贯叶金丝桃属植物中具有药理活性代谢物的丰富可靠来源，可用于制药工业。
