In traditional medicine, Bauhinia glauca subsp. hupehana has long been used as an analgesic agent in China. The aim of this study was to evaluate the antinociceptive activity of the ethanol extract of the aerial parts of B. glauca subsp. hupehana (BHE) in rats and its chemical fingerprint. The antinociceptive activity of BHE was assessed in mice using chemically and heat–induced pain models, such as the acetic acid–induced writhing, hot plate, tail–flick and glutamate tests. Naltrexone hydrochloride, a non–selective opioid receptor antagonist, was utilized to determine the involvement of the opioid system. In addition to this, the involvements of the cGMP and ATP–sensitive K+ channel pathways were also detected using methylene blue and glibenclamide. The oral administration of BHE (at doses of 50, 100 and 200 mg/kg) produced significant and dose–related inhibitions in both the chemically and heat–induced pain models. Interestingly, in the abdominal constriction test, when the dose of BHE was increased to 800 mg/kg (p.o., n = 10), the inhibition rate was 100%. The antinociceptive mechanism may involve the cGMP pathway and ATP sensitive K+ channel pathway. The central antinociceptive effect was not antagonized by naltrexone. One phenolic acid, one lignin and five flavonoids were isolated from BHE. The antinociceptive activity of BHE was most likely due to the presence of the flavonoids. The acute toxicity results showed that BHE was safe at a high dose (2 g/kg, p.o.). The current investigation demonstrates that B. glauca subsp. hupehana is a potential candidate for the development of novel, non–opioid, analgesic phytomedicines.
A novel analgesic pyrazine derivative, named crotonine, was isolated from the leaves of Croton tiglium L. The structure was elucidated as 2-(furan-2-yl)-5-(2,3,4-trihydroxy-butyl)-1,4-diazine by spectroscopic analysis. Crotonine inhibited remarkably the acetic acid-induced writhing in mice.
Abstract:Four new pregnane glycosides 1-4 were isolated from the ethanol extract of the stem of Gymnema sylvestre and named gymsylvestrosides A-D. Hydrolysis of compound 1 under the catalysis of Aspergilus niger β-glucosidase afforded compound 5 (gymsylvestroside E). Their structures were determined by spectroscopic methods such as HRESIMS, 1D and 2D NMR, as well as HMQC-TOCSY experiment. Compounds 1-4 were screened for Saccharomyces cerevisiae α-glucosidase inhibitory activity.
A new acylated C-glycosylflavone (1) was isolated from Trollius ledebouri Reichb together with two known C-glycosyflavones (2, 3). The structures were elucidated by spectroscopic methods, including HRMS, IR, 1H and 13C NMR and 2D experiments (COSY, HMQC and HMBC). The anti-inflammatory activities of 1-3 were tested on TPA-induced mice ear edema (in vivo).
A new cytotoxic macrocyclic trichothecene calcarisporin B1 (1), and two known compounds roridin H (2) and roridin J (3) were isolated from the cultured mycelia of Calcarisporium arbuscula Preuss. The structure of 1 was determined to be 8alpha-acetoxy roridin H on the basis of spectral data. The cytotoxic activities of 1-3 were evaluated in vitro.
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