Shandong Bestcomm Pharmaceutical Co., Ltd.

Ciprofol is a novel clin. anesthetic and is deemed a better alternative to propofol due to its fewer side effects.Herein, we report an atom-economical and cost-efficient manufacturing process to prepare Ciprofol, which includes regioselective para-halogenation of phenol, followed by esterification and Fries rearrangement in high yields.This strategy adopts para-halogenation to avoid the generation of para-byproducts in the Fries rearrangement.After a benign reduction of bromine and the Wittig reaction, the desired Ciprofol is achieved by ruthenium-catalyzed asym. hydrogenation.This new process has been tested on a multigram scale, with an improved overall yield of 60% and enhanced cost efficiency, while offering atom economy advantages.The low yield of the Claisen rearrangement and the use of costly and corrosive reagents in the previously reported synthesis were avoided.

In this study, we investigated the therapeutic effect and potential mechanism of Et acetate extract from hawthorn seeds (HSEAE) on DGP rats.We measured their body weight, blood sugar, gastric emptying rate, and intestinal propulsion rate, as well as the effects of HSEAE on superoxide dismutase (SOD), malondialdehyde (MDA), and glutathione peroxidase (GSH-Px) in gastric homogenate.The levels of ghrelin in rat plasma were determined by RIA, while those of motilin and gastrin were determined by ELISA.Western blot was used to detect the expression of c-kit, ghrelin, and neuronal nitric oxide synthase (nNOS) in the rats' stomachs, and immunohistochem. was used to detect changes in interstitial cells of Cajal (ICC).The results showed that different doses of HSEAE effectively promoted the gastric emptying and small intestinal propulsion (P < 0.05 or P < 0.01).In addition, HSEAE increased SOD and GSH-Px in the rats' stomachs while decreasing MDA, and increased plasma ghrelin while decreasing MTL and GAS (P < 0.05 or P < 0.01).The expression of c-kit, ghrelin, and nNOS proteins and the number of ICCs in the rats' stomachs also significantly increased (P < 0.05 or P < 0.01).Our experiments showed that HSEAE improved gastrointestinal motility in DGP rats, and its potential mechanism might be involved in the inhibition of oxidative stress injury induced by hyperglycemia, upregulating n-NOS, c-kit expression, and ICCs in their stomachs and regulating gastrointestinal hormones.