Delving into the Latest Updates on Anhui China Resources Jinchan Pharmaceutical Co., Ltd. with Synapse

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Arenobufagin (ArBu) is a natural anticancer drug with good anti-tumor effects, but its clinical applications and drug development potential are limited due to its toxicity. The purpose of this study is to reduce the toxic side effects of ArBu and improve the efficacy of tumor treatment by incorporating it into poly(ethylene glycol)-b-poly (lactide) co-polymer (PEG-PLA). ArBu@PEG-PLA micelles were prepared by a thin film hydration method. The optimized micelles were characterized by size, stability, drug loading, encapsulation rate, and drug release. The tumor-inhibition efficacy of the micelles was evaluated on A549 cells and tumor-bearing mice. The ArBu@PEG-PLA micelles have good drug-loading capacity, release performance, and stability. They can accumulate at the tumor site through the EPR effect. The micelles induce apoptosis through a mitochondrial apoptosis pathway. Compared with the free ArBu, the ArBu@PEG-PLA micelles had lower toxicity and higher safety in the acute toxicity evaluation experiment. The in vivo anti-tumor experiment with tumor-bearing mice showed that the tumor-inhibition rate of ArBu@PEG-PLA micelles was 72.9%, which was 1.28-fold higher than that of free ArBu (57.1%), thus showing a good tumor treatment effect. This study indicates that ArBu@PEG-PLA polymeric micelles can significantly improve the toxicity and therapeutic efficacy of ArBu. These can lead to a new therapeutic strategy to reduce the toxicity of ArBu and enhance tumor treatment.

01 Feb 2021·SteroidsQ4 · MEDICINE

Discovery of 3-peptide substituted arenobufagin derivatives as potent antitumor agents with low cardiotoxicity

Q4 · MEDICINE

Article

Author: Wang, Yuan ; Wang, Chuanhao ; Zhu, Yazhao ; Yao, Jianzhong ; Wu, Yuelin ; Zhang, Hui ; Miao, Zhenyuan ; Ma, Haijun ; Ma, Jianjiang ; Luo, Chuan ; Chen, Baobao

Active natural productscan be valuable lead compounds and numerous drugs derived from natural products have successfully entered the clinic. Arenobufagin, one of the important active components of toad venom, indicates significant antitumor activities with limited preclinical development for its strong cardiotoxicity. Ten 3-monopeptide substituted arenobufagin derivatives have been designed and synthesized. Antitumor activity and cardiotoxicity assays lead to the discovery of compound ZM226 as a potent antitumor agent with low cardiotoxicity. These findings suggest optimization of arenobufagin on position 3 maybe an efficacious strategy for the development of antitumor drug candidates derived from arenobufagin.

15 Mar 2016·China Journal of Chinese Materia Medica

Effects of different stocking density and diet on development of Bufo gargarizans tadpoles

Article

Author: Yang, Yan ; Gao, Bo ; Huang, Lu-Qi ; Kang, Yan ; Li, Jun-de ; Li, Deng-Lin ; Zhao, Qun

The effects of four different stocking densities and five different diets on the growth of Bufo gargarizans tadpoles were studied to determine the optimum stocking density and diet. For stocking density experiment, the tadpoles were fed respectively at different density of 200, 500, 1 000 and 2 000 tadpoles per square meter. For diet experiment, the tadpoles were divided into five groups fed respectively with five different diets. The body weight, snout-vent length and tail length were measured every seven days, and mortality was recorded. The results showed that: the survival rates of tadpole before metamorphosis and after metamorphosis were from 68.7% to 96.3% and from 5.7% to 36.0%, respectively; the optimum stocking density is 1 000 tadpoles per square meter for the stocking density had no effect on the survival rate of tadpole before metamorphosis, and the tadpoles had the relative large body weight and survival numbers in 1000 tadpoles per square meter; the diet Ⅱ(37.9% crude protein and 5.7% crude fat), Ⅳ (25.1% crude protein and 4.0% crude fat), and Ⅴ (egg yolk) were all the optimum diets for the diet had no effect on the survival rate of tadpole before metamorphosis and the tadpoles fed with three kinds of diet above had relatively large body weight, and one of these three diets based on their availability and cost should be adopted during breeding period.

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Pipeline

Pipeline Snapshot as of 08 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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