Abstract
A bioactivity guided program exploring the interaction of phytochemicals in the entire plant Primula macrocalyx with the organic anion transporters (OAT1 and OAT3) and microorganisms led to the elucidation of ten known flavones (1–4, 6–10, 12) and two previously undescribed flavones (5, 11). The structures of the compounds were determined by extensive analysis of spectroscopic data, as well as by comparison with data from previous reports. Two known flavones (9, 12) are reported for the first time from the family Primulaceae. All compounds were evaluated for inhibition of OAT1 and OAT3. Six flavones (2, 3, 6–8, 12) showed potent inhibitory activity on OAT1, while seven flavones (2, 3, 6–9, 12) showed marked inhibitory activity on OAT3, with IC50 ≤ 10.0 µM. Antimicrobial activities of crude fractions against sixteen microorganisms were tested to give a target yeast strain Candida rugosa for further evaluation of MICs on the isolates. Three flavones (7, 8, 12) showed marked antifungal activity with MIC < 2.0 µM. To our knowledge, this study is the first to evaluate these flavones as inhibitors of the OAT1 and OAT3, and as antifungal agents.
Highlights
Primula macrocalyx Bunge (Primulaceae) is a perennial herbaceous plant, which has been widely used in folk medicine as an expectorant, diuretic, sedative, spasmolytic, and sudorific to treat a variety of maladies such as vitamin deficiency, colds, fever, headache, insomnia, paralysis, scurvy, tuberculosis, heart disease, rheumatism, and kidney diseases1,2
Modern pharmacologic research has shown that riccardin C is a potent inhibitor of NO synthesis10 and the related bisbibenzyl compounds having cytotoxic, antibacterial, and fungicidal activity were inhibitors of 5-lipoxygenase1
Research in mice suggests that Oat3 may mediate blood pressure regulation, so Oat3 inhibitors might be considered as potential antihypertensive agents15
Summary
Primula macrocalyx Bunge (Primulaceae) is a perennial herbaceous plant, which has been widely used in folk medicine as an expectorant, diuretic, sedative, spasmolytic, and sudorific to treat a variety of maladies such as vitamin deficiency, colds, fever, headache, insomnia, paralysis, scurvy, tuberculosis, heart disease, rheumatism, and kidney diseases. Modern pharmacologic research has shown that riccardin C is a potent inhibitor of NO synthesis and the related bisbibenzyl compounds having cytotoxic, antibacterial, and fungicidal activity were inhibitors of 5-lipoxygenase. Modern pharmacologic research has shown that riccardin C is a potent inhibitor of NO synthesis and the related bisbibenzyl compounds having cytotoxic, antibacterial, and fungicidal activity were inhibitors of 5-lipoxygenase1 These chemical compositions may contribute to the medicinal properties mentioned above. Organic anion transporter 1 (OAT1) and 3 (OAT3), which are highly expressed in the kidney, play an important part in the renal elimination of a range of substrate molecules. Organic anion transporter 1 (OAT1) and 3 (OAT3), which are highly expressed in the kidney, play an important part in the renal elimination of a range of substrate molecules12,13 Both OAT1 and OAT3 are considered to be therapeutic targets for hypertension. The dichloromethane soluble fraction of a methanol extract of entire plant of P. macrocalyx elicited marked inhibition of OAT1 and OAT3 in vitro, and potent antifungal activity against yeast strain Candida rugosa
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