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Cytotoxic Xanthones from Hypericum stellatum, an Ethnomedicine in Southwest China.

ABSTRACT: Hypericum stellatum, a species endemic to China, is used to treat hepatitis by several ethnic groups in Guizhou Province. This research was inspired by the traditional medicinal usage of H. stellatum, and aims to explore the phytochemistry and bioactivity of H. stellatum to explain why local people in Guizhou widely apply H. stellatum for liver protection. In this study, two new prenylated xanthones, hypxanthones A (8) and B (9), together with seven known compounds, were isolated from the aerial parts of the plant. Spectroscopic data as well as experimental and calculated ECD spectra were used to establish the structures of these compounds. Six xanthones isolated in this study, together with four xanthones previously isolated from H. stellatum, were evaluated for their growth-inhibitory activities against five human liver carcinoma cell lines to analyze the bioactivity and structure-activity relationship of xanthones from H. stellatum. Isojacareubin (6) showed significant cytotoxicity against five human liver carcinoma cell lines, with an IC50 value ranging from 1.41 to 11.83 ?M, which was stronger than the positive control cisplatin (IC50 = 4.47-20.62 ?M). Hypxanthone B (9) showed moderate cytotoxicity to three of the five cell lines. Finally, structure-activity analysis revealed that the prenyl and pyrano substituent groups of these xanthones contributed to their cytotoxicity.

SUBMITTER: Ji Y

PROVIDER: S-EPMC6804229 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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Cytotoxic Xanthones from Hypericum stellatum, an Ethnomedicine in Southwest China.

Ji Yuanyuan Y Zhang Ruifei R Zhang Chen C Li Xingyu X Negrin Adam A Yuan Chaonan C Kennelly Edward J EJ Long Chunlin C

Molecules (Basel, Switzerland) 20191002 19

Hypericum stellatum, a species endemic to China, is used to treat hepatitis by several ethnic groups in Guizhou Province. This research was inspired by the traditional medicinal usage of H. stellatum, and aims to explore the phytochemistry and bioactivity of H. stellatum to explain why local people in Guizhou widely apply H. stellatum for liver protection. In this study, two new prenylated xanthones, hypxanthones A (8) and B (9), together with seven know ...[more]

PMID: 31581734

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Project description:BACKGROUND:The Wuliang Mountains of the Jingdong region is a settlement area of the Yi community located in south-western Yunnan Province in China. Due to its unique geographical location, this area harbours abundant medicinal plant resources. The medicinal plants used by the local people have a long history and play an important role in their daily life. During the long-term mixed lifestyle, the knowledge of traditional medicinal plants in different communities has been assimilated to some extent. Therefore, this paper is based on ethnobotanical investigations to document traditional medicinal plants used by local people and discuss the differences between the Yi and Han communities in the study area. METHODS:Data on traditional medicinal plants were collected from September 2016 to August 2017 in the Yi autonomous county of Jingdong. Seven townships and 16 villages were selected for the field investigations. Information was obtained through key informant interviews. A total of 44 key informants were interviewed, and all of them were herbalists or herbal sellers. RESULTS:In this study, a total of 302 traditional medicinal plant species belonging to 117 families and 252 genera were investigated and documented, most of which were obtained from herbalists. Although family Asteraceae was the most prevalent, with 27 species, the most commonly utilized species were members of family Papaveraceae, Dactylicapnos scandens (D. Don) Hutch., which is used as an antipyretic drug. Herbs comprised half of the total number of species, and the whole plant is the most frequently utilized plant part. The plants were used to treat more than 93 human diseases, with antipyretic drugs being the most common form of herbal medicine. The traditional medicinal plants used in the study area possess a high ratio of being documented in the literature. According to the analysis, the Chinese Pharmacopoeia recorded 76 species and the Resources of Traditional Chinese Medicine recorded 233 species of traditional medicinal plants. By evaluating the endangered status of the traditional medicinal plants in the study area, we found good conservation status of the cited medicinal plants. Regarding the similarity between the communities, there were significant differences between the Yi and Han communities, as indicated by the Jaccard similarity index (0.232). CONCLUSIONS:Medicinal plants are the embodiment of wisdom from our ancestors and play a significant role in treating various human disorders. As one of the birthplaces of Yi medicine, the study area possesses a high species diversity of traditional medicinal plants used by local people. With the rapid development of modern medicine, however, the inheritance of this valuable culture is facing enormous threats even though its potential value has not yet been fully explored. Therefore, some effective protection measures should be taken, and some modern techniques should be implemented to prove the safety and improve the scientific acceptance of the traditional medicinal plants.

Project description:The global cancer burden remains a serious concern with the alarming incidence of one in eight men and one in eleven women dying in developing countries. This situation is aggravated by the multidrug resistance (MDR) of cancer cells that hampers chemotherapy. In this study, the cytotoxicity of the methanol extract (HRB), fractions (HRBa, HRBb, and HRBa1-5), and compounds from the bark of Hypericum roeperianum (HRB) was evaluated towards a panel of 9 cancer cell lines. The mode of action of the HRB and trichadonic acid (1) was also studied. Column chromatography was applied to isolate the constituents of HRB. The cytotoxicity of botanicals and phytochemicals was evaluated by the resazurin reduction assay (RRA). Caspase-Glo assay was used to evaluate the activity of caspases, and reactive oxygen species (ROS) (H2DCFH-DA) were assessed by flow cytometry. Phytochemicals isolated from HRB were trichadonic acid (1), fridelan-3-one (2), 2-hydroxy-5-methoxyxanthone (3), norathyriol (4), 1,3,5,6-tetrahydroxyxanthone (5), betulinic acid (6), 3'-hydroxymethyl-2'-(4″-hydroxy-3″,5″-dimethoxyphenyl)-5',6':5,6-(6,8-dihydroxyxanthone)-1',4'-dioxane (7), and 3'-hydroxymethyl-2'-(4″-hydroxy-3″,5″-dimethoxyphenyl)-5',6':5,6-(xanthone)-1',4'-dioxane (8). Botanicals HRB, HRBa, HRBa2-4, HRBb, and doxorubicin displayed cytotoxic effects towards the 9 tested cancer cell lines. The recorded IC50 values ranged from 11.43 µg/mL (against the P-glycoprotein (gp)-overexpressing CEM/ADR5000 leukemia cells) to 26.75 µg/mL (against HCT116 (p53+/+) colon adenocarcinoma cells) for the crude extract HRB. Compounds 1, 5, and doxorubicin displayed cytotoxic effects towards the 9 tested cancer cell lines with IC50 values varying from 14.44 µM (against CCRF-CEM leukemia cells) to 44.20 µM (against the resistant HCT116 (p53-/-) cells) for 1 and from 38.46 µM (against CEM/ADR5000 cells) to 112.27 µM (against the resistant HCT116 (p53-/-) cells) for 5. HRB and compound 1 induced apoptosis in CCRF-CEM cells. The apoptotic process was mediated by enhanced ROS production for HRB or via caspases activation and enhanced ROS production for compound 1. This study demonstrated that Hypericum roeperianum is a potential source of cytotoxic phytochemicals such as trichadonic acid and could be further exploited in cancer chemotherapy.

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Cytotoxic Xanthones from Hypericum stellatum, an Ethnomedicine in Southwest China.

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Cytotoxic Xanthones from <i>Hypericum stellatum</i>, an Ethnomedicine in Southwest China.

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