Search

Plants in the genus Hypericum (Hypericaceae), include more than 500 species worldwide, and many are valued for their medicinal properties, and are used as traditional herbal medicines. However, only H. perforatum is officially recognized as herbal drug in several pharmacopoeias, and used as an antidepressant clinically. Hypericum perforatum had been used as an herbal medicine since the Han Dynasty (206 B.C. -220 A.D.) in China. It taxonomically belongs to the section Hypericum in the genus Hypericum. There are about 42 species in the section Hypericum , with six species occurring in China. All six are recorded as traditional herbal medicines for treating aliments, including hepatitis, malaria, traumatic hemorrhage, irregular menstruation, wounds, and bruises. The study aimed to characterize the chemical profiles of five phylogenetically related Hypericum species, and compare their metabolites with three H. perforatum products. Informed by ethnobotanical use, the extracts prepared from the five species were further investigated into anticancer, anti-inflammatory and antiplasmodial activity. This study tested the hypothesis that systematic metabolomic and bioactivity characterization of species in section Hypericum will help to validate their phytotherapeutic use and reveal potential drug lead compounds. Targeted and non-targeted metabolic analyses coupled with chemometrics were conducted on H. perforatum and four medicinal species, H. attenuatum , H. enshiense , H. erectum , and H. faberi , native to China from section Hypericum. UPLC-QTOF-MS/MS and UPLC-TQD-MS/MS were used for non-targeted and targeted metabolic analyses, respectively. Cytotoxicity bioassays on four cancer cell lines, anti-inflammation tests and anti-plasmodial activity on Plasmodium falciparum 3D7, selected based on traditional medicinal use, were evaluated on extracts from Hypericum species. Progenesis QI and EZinfo were used for chemometrics analysis to link the chemical profile and bioassay activity to aid in the identification of bioactive compounds. In total, 58 compounds were identified from the five species, including compounds with well-characterized bioactivity. Hypericum attenuatum , H. erectum , and H. perforatum , displayed the highest cytotoxicity, and contain the cytotoxic compounds petiolin A, prolificin A, and hypercohin G, respectively. Hypericum faberi and H. perforatum showed the highest anti-inflammatory activity, with pseudohypericin, quercetin and chlorogenic acid being observed at higher concentrations. Hypericum perforatum and H. erectum showed anti-plasmodial activity, with higher hyperforin and xanthones in these species that may account for the anti-plasmodial activity. This study characterized the chemical differences among five Hypericum species using metabolomics. These ethnomedically important species were tested for their biological activities in three distinct in vitro assays. The ethnobotanical data were useful for identifying bioactive Hypericum species. Hypericum attenuatum , H. erectum and H. faberi are promising phytotherapeutic species, although they are much less studied than H. perforatum , St. John's wort. Combining ethnobotanical surveys with chemometric analyses and bioactivity screening can greatly enhance the discovery of promising active constituents. [Display omitted] • Profiled five Hypericum species with non-targeted and targeted chemometrics. • Identified 58 representative compounds from five species that drive chemotaxonomy. • Described Hypericum cytotoxicity, anti-inflammatory, and anti-plasmodial activity. • Employed chemometrics to aid in the identification of bioactive compounds. [ABSTRACT FROM AUTHOR]

Hypericum species have been used traditionally as astringent, antipyretic, diuretic, antiphlogistic, analgesic, and antidepressant in Europe, America, Africa, and Asia. One of the most extensively investigated medicinal herbs, H. perforatum L. (St. John's wort), is widely used in many countries to treat mild to moderate mental depression. Hypericum species are abundant throughout China, including 30 used as ethnomedicines. There are limited publications describing the ethnobotanical uses and biological activities associated with Hypericum species in China. Some reported activities include the treatment of wounds and bruises, irregular menstruation, dysentery, hepatitis, mastitis, jaundice, hemoptysis, and epistaxis. This review aims to critically examine how Hypericum species are used ethnomedicinally in China, to see if the ethnobotanical data may be useful to help prioritize Hypericum species and certain phytochemical constituents that may be new drug leads, and consider the focus and lack of the phytopharmacological study on Hypericum species in China. Classic medicinal books and ethnomedicinal publications were reviewed for the genus Hypericum (called jin si tao in Chinese). In addition, relevant information about ethnobotany, phytochemistry, and pharmacology were from online databases including SciFinder, Science Direct, PubMed, Google Scholar, and China National Knowledge Infrastructure (CNKI). " Hypericum ", "金丝桃", "ethnobotany", "traditional use", "ethnomedicine", "phytochemistry", "pharmacology" and "bioactivity" were used as keywords when searching the databases. Thus, available articles from 1959 to 2019 were collected and analyzed. Among 64 Hypericum species recorded in China, 30 have been used as ethnomedicines by 15 linguistic groups such as Dai, Dong, Han, Miao, and Mongolian people. Hypericum species in China possess traditional uses which are also mirrored in Europe, America, Africa, and other countries in Asia. However, there are some unique ethnomedicinal uses in China. For example, several Hypericum species are used as a local remedy in southwest China, and H. attenuatum Fisch. ex Choisy is used to treat cardiac disorders in northeast China. Antitumor, anti-inflammatory, antimicrobial, neuroprotective, antidepressant, hepatoprotective, cardioprotective, and antiviral activities have been reported in numerous biological studies. The main phytochemical constituents in Hypericum consist of phloroglucinols, naphthodianthrones, xanthones, flavonoids, and terpenoids. There is a rich traditional knowledge regarding the ethnomedicinal uses of Hypericum species in China. Through phytochemical and pharmacological studies, several medicinal Hypericum from China have yielded many bioactive phytochemicals, possessing antitumor, anti-inflammatory, antimicrobial, and neuroprotective properties. Hypericum species from China are potential sources of drugs to fight cancer and other chronic diseases. Remarkably, nearly half of Hypericum species in China have rarely been studied, and their ethnomedicinal potential have not been scientifically evaluated. Thus, in vitro mechanistic studies, in vivo pharmacology, and clinical efficacy are all needed, prioritizing those studies that relate most closely with their traditional uses. In addition, a comprehensive plant-resource evaluation, quality control, and toxicology studies are needed. Image 1 [ABSTRACT FROM AUTHOR]