38945-21-0Relevant articles and documents
Design, synthesis and evaluation of wound healing activity for β-sitosterols derivatives as potent Na+/K+-ATPase inhibitors
Cui, Shaoyu,Jiang, Hongli,Chen, Lei,Xu, Jian,Sun, Wenzhuo,Sun, Haopeng,Xie, Zijian,Xu, Yunhui,Yang, Fubai,Liu, Wenyuan,Feng, Feng,Qu, Wei
, (2020/01/31)
β-Sitosterols, is a common steroid that can be identified in a variety of plants and their efficacy in promoting wound healing has been demonstrated. Na+/K+-ATPase, more than a pump, its signal transduction function for involvement in cell growth regulation attracts widespread concern. The Na+/K+-ATPase/Src receptor complex can serve as a receptor involved in multiple signaling pathways including promoting wound healing pathways. To finding potent accelerating wound healing small molecular, we choose the high inhibitory activity of Na+/K+-ATPase and non-cardiotoxic natural compound, β-sitosterol as the substrate. A series of β-sitosterol derivatives were designed, synthesized and evaluated as potential Na+/K+-ATPase inhibitors. Among them, compounds 31, 47, 49, showed improved inhibitory activity on Na+/K+-ATPase, with IC50 value of 3.0 μM, 3.4 μM, 2.2 μM, which are more potent than β-sitosterol with IC50 7.6 μM. Especially, compound 49 can induce cell proliferation, migration and soluble collagen production in L929 fibroblasts. Compared to model, compound 49 can accelerate wound healing in SD rats. Further studies indicated that 49 can activate the sarcoma (Src), uptake the protein kinase B (Akt), extracellular signal-regulated kinase (ERK) proteins expression in a concentration dependent manner. Finally, binding mode of compound 49 with Na+/K+-ATPase was studied, which provides insights into the determinants of potency and selectivity. These results proved β-stitosterol derivative 49 can serve as an effective inhibitor of Na+/K+-ATPase and potential candidate for accelerating wound healing agents.
O - substituted hydroxylamine hydrochloride and its preparation method (by machine translation)
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Paragraph 0065; 0068; 0069, (2018/10/11)
The present invention provides a O - substituted hydroxylamine hydrochloride and its preparation, wherein the preparation method comprises the following steps: step S1, to the acetyl hydroximic acid ethyl ester in ethanol solution of adding sodium hydroxide, in addition at the same time instillment halohydrocarbon, chloride or acyl chloride substitution reaction to take place, then added to the water in order to separate out the O - substituted [...]; step S2, the said O - substituted [...] adding hydrochloric acid solution in order to produce reflux reaction O - substituted hydroxylamine hydrochloride. According to the embodiment of the invention of the O - substituted hydroxylamine hydrochloride of the preparation method, high purity of the product can be obtained, and the method is safe, easy to process, the process is simple, and is suitable for industrial production. (by machine translation)
With biological activity mixed oxygen benzene oxygen N- the oxygen radical is thick carboxylic acid amide compound and its preparation method
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Paragraph 0074; 0093; 0094; 0095, (2016/10/08)
The present invention discloses a N-oxyl fused heterocycle oxy phenoxy carboxylic acid amide compound having biological activity, and a preparation method thereof, wherein the compound is represented by a formula (I), A is selected from the following groups, R is C3-C6 alkenyl, C3-C6 alkynyl, C3-C6 halogenated alkenyl, C3-C6 halogenated alkynyl, C3-C6 cycloalkyl methyl and C3-C6 halogenated cycloalkyl alkyl methyl, R1 is H, C1-C3 alkyl, and C1-C3 halogenated alkyl, and R2 is H, halogen, C1-C3 alkyl, and C1-C3 halogenated alkyl. The compound represented by the formula (I) has broad-spectrum biological activity of weed removing or insect killing and bacterial killing, wherein some compounds have high weed removing activity and can achieve a good prevention and control effect at a use amount of 3.75-75 g effective component/hectare.