Abstract
Six new coumarin glycosides, genglycoside A–F (1–6), were isolated from the aerial parts of Gendarussa vulgaris, along with ten known analogues (7–16). Their structures were unambiguously established on the basis of extensive spectroscopic data and HPLC analysis. The cytotoxic activities of all isolated compounds were evaluated by MTT assay. Compound 12 showed the most potent cytotoxicity in Eca-109, MCF-7, and HepG2 cell lines. By the preliminary structure–activity relationships, it was firstly discovered that the glycosylation or esterification at 7,8-dihydroxy or 7-hydroxy drastically reduced the cytotoxic activity of the parent coumarin.
Highlights
Gendarussa vulgaris Nees, which belongs to the family of Acanthaceae, is an evergreen dwarf shrub mainly distributed in China, India, Sri Lanka, and the Malay Peninsula [1]
Results and Discussion comparison of its NMR data with those reported in the literature [17]
Natural products have played an important role in new drug discovery
Summary
Gendarussa vulgaris Nees, which belongs to the family of Acanthaceae, is an evergreen dwarf shrub mainly distributed in China, India, Sri Lanka, and the Malay Peninsula [1]. Occurring coumarins have exhibited a broad spectrum of pharmacological actions, including as an anticoagulant [3], CNS stimulant [4], antioxidant [5], antiviral [6], hepatoprotective [7], anti-inflammatory [8], anticancer [9], and cyclooxygenase, lipooxygenase, cholinesterase (ChE), and monoamine oxidase (MAO) inhibitory activities [9,10], antimutagenic [10], etc. As potential therapeutic drugs against cancer, coumarins have exhibited obvious anti-proliferative activity in malignant melanoma, prostate cancer, and renal cell carcinoma in some clinical trials [11], and very rare cardiotoxicity, nephrotoxicity, dermal toxicity, and other MDR (multi-drug resistance) side effects [9]. In our search for cytotoxic natural products from the aerial parts of G. vulgaris, six new coumarin glucosides (1–6) were obtained together with ten known analogues (7–16). Structure elucidation, and cytotoxicity of all isolated compounds against Eca-109, MCF-7, and HepG2 cell lines are described here (Figure 1)
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