Abstract

As a TCM, Hedyotis diffusa Willd. has been using to treat malignant tumors, and many studies also showed that the extracts from Hedyotis diffusa Willd. possessed evident antitumor activities. Therefore, we carried out chemical study on Hedyotis diffusa Willd. and investigated the cytotoxicity of the obtained compounds on a panel of eight tumor cell lines. As a result, four new compounds were isolated from Hedyotis diffusa Willd., including three iridoid glycosides of Shecaoiridoidside A–C (1–3) and a cerebroside of shecaocerenoside A (4). Also, six known iridoid compounds (5–10) were also obtained. The cytotoxicity of all compounds against human tumor cell lines of HL-60, HeLa, HCT15, A459, HepG2, PC-3, CNE-2, and BCG-823 were also evaluated in vitro. New compound 3 exhibited evident cytotoxicity to all tumor cell lines except the Hela, and the IC50 values are from 9.6 µM to 62.2 µM, while new compound 4 showed moderate cytotoxicity to all the cell lines, and the IC50 values are from 33.6 µM to 89.3 µM. By contrast, new compound 1 and known compound 9 showed moderate cytotoxicity to HCT15, A459, and HepG2 selectively. Known compound 7 also exhibited moderate cytotoxicity to HCT15 and A459 selectively.

Highlights

  • As an annual herb, Genus of Hedyotis has been widely distributed in subtropical area of the world [1].62 species of Hedyotis are distributed in China, among which more than 20 species are used as medicines, ingcluding Hedyotis diffusa Willd. (H. diffusa Willd.)

  • The components of iridoids, triterpenes, flavonoids, lignans, anthraquinones, alkaloids, cerebrosides, coumarins, and sterols were discovered during the chemical studies of H. diffusa Willd. [2,6,7,8]

  • New compound 3 exhibited evident cytotoxicity to all tumor cell lines except the Hela, and the IC50 values are from 9.6 μM to 62.2 μM, while new compound 4 showed moderate cytotoxicity to all the cell lines and the IC50 values are from 33.6 μM to 89.3 μM

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Summary

Introduction

Genus of Hedyotis has been widely distributed in subtropical area of the world [1].62 species of Hedyotis are distributed in China, among which more than 20 species are used as medicines, ingcluding Hedyotis diffusa Willd. (H. diffusa Willd.). Genus of Hedyotis has been widely distributed in subtropical area of the world [1]. 62 species of Hedyotis are distributed in China, among which more than 20 species are used as medicines, ingcluding Hedyotis diffusa Willd. Has been recorded in Chinese pharmacopoeia (2015 edt) and possesses the efficacies of diuresis to reduce edema, clearing away the heat evil and detoxifying, and promoting blood circulation to arrest pain [2]. The components of iridoids, triterpenes, flavonoids, lignans, anthraquinones, alkaloids, cerebrosides, coumarins, and sterols were discovered during the chemical studies of H. diffusa Willd. There are some differences of the chemical constituents if the H. diffusa Willd. The contents of anthraquinones and iridoids in H. diffusa Willd. From Guangdong province were higher than the H. diffusa The contents of anthraquinones and iridoids in H. diffusa Willd. from Guangdong province were higher than the H. diffusa

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