Author: Yang, Wenxiang ; Ke, Xianghong ; Fan, Bolin ; Fu, Shaohua ; Xia, Ying ; Fan, Jun ; Zhang, Yinjing ; Li, Yanmei ; Qu, Jingjing ; Zeng, Yanhua ; Tian, Jie

To evaluate the safety of alpha-glycerylphosphorylcholine (α-GPC) as a novel food, the study of acute oral toxicity, subchronic toxicity, teratogenic toxicity and genotoxicity were conducted. In acute oral toxicity, no toxic effects were observed in rats of both genders administrated 10.0 g/kg BW α-GPC. In 90-day oral toxicity, female high-dose group (2,000 mg/kg) had lower body weight, body weight gain, empty stomach body weight, total protein (TP), albumin (ALB), and higher alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) in contrast to control group. In teratogenic toxicity, the body weights of pregnant rats on the 9th day (d9), the 12th day (d12), the 15th day (d15), and the 20th day (d20), body weight gains, and net body weight gains in high-dose group (2,000 mg/kg) decreased, the other parameters had no difference compared to control group. In genotoxicity tests (Mammalian erythrocyte micronucleus, Chromosome aberration and Ames test), all dose groups didn't display significant change compared with negative control group. Based on above results, α-GPC is actually low hazard novel food, has a NOAEL of 1,000 mg/kg BW for female rats and 2,000 mg/kg BW for male rats following 13-week oral exposure, has a NOAEL of 1,000 mg/kg BW for pregnant rats and 2,000 mg/kg BW for fetal rats in teratogenic toxicity, has no genotoxicity in vitro or in vivo.

31 Dec 2024·Journal of Enzyme Inhibition and Medicinal Chemistry

Discovery of natural anthraquinones as potent inhibitors against pancreatic lipase: structure-activity relationships and inhibitory mechanism

Article

Author: Qian, Xing-Kai ; He, Wen-Yao ; Chen, Zi-Qiang ; Li, Hao ; Zou, Li-Wei ; Zhou, Jing ; Ma, Hong-Hong ; Zhu, Ya-Di ; Yang, Si-Yuan

Obesity is acknowledged as a significant risk factor for various metabolic diseases, and the inhibition of human pancreatic lipase (hPL) can impede lipid digestion and absorption, thereby offering potential benefits for obesity treatment. Anthraquinones is a kind of natural and synthetic compounds with wide application. In this study, the inhibitory effects of 31 anthraquinones on hPL were evaluated. The data shows that AQ7, AQ26, and AQ27 demonstrated significant inhibitory activity against hPL, and exhibited selectivity towards other known serine hydrolases. Then the structure-activity relationship between anthraquinones and hPL was further analysed. AQ7 was found to be a mixed inhibition of hPL through inhibition kinetics, while AQ26 and AQ27 were effective non-competitive inhibition of hPL. Molecular docking data revealed that AQ7, AQ26, and AQ27 all could associate with the site of hPL. Developing hPL inhibitors for obesity prevention and treatment could be simplified with this novel and promising lead compound.

20 Dec 2024·The Journal of Organic Chemistry

Selective Hydroformylation of 1,3-Butadiene to Adipic Aldehyde Enabled by a Ligand-Relay Catalysis

Article

Author: Liu, Yifan ; Wang, Zhaozhan ; Kuang, Shaoping ; Yang, Yong

The hydroformylation of 1,3-butadiene for the selective synthesis of adipic aldehyde (AA) has been a long-standing challenge due to its intricate reaction network, resulting in low reaction efficiency and poor chemo- and regioselectivity. Herein, we propose a dual ligand-relay catalysis strategy for the selective hydroformylation of 1,3-butadiene to an AA. This strategy entails a one-pot and two-step process, commencing with a Rh-catalyzed 1,3-butadiene hydroformylation, followed by Rh-catalyzed isomerizing hydroformylation. The reaction is facilitated by using two distinct biphosphites as auxiliary ligands, each with a specific individual role in the process. Remarkably, an unprecedented chemo- and regioselectivity of up to 65.9% toward AA was achieved with complete conversion of 1,3-butadiene, marking the highest value compared to the previous state-of-the-art catalyst systems thus far. Furthermore, the process also produced a 26.5% selectivity for n-valeraldehyde as the major byproduct, a key compound of industrial importance. This study therefore represents a significant advancement in the hydroformylation of 1,3-butadiene, showcasing the potential of this ligand-relay catalysis strategy for improving selectivity in the reaction.

100 Deals associated with Dantron

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KEGG	Wiki	ATC	Drug Bank
D07107	Dantron	A06AB03	DB04816

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Indication	Country/Location	Organization	Date
Constipation	United Kingdom	-	08 Nov 1999

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