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At present, there are about 120 million diabetic patients in China, and traditional diabetes drugs are not effective in reducing fasting blood sugar
.
The abnormal activity of hepatic gluconeogenesis is one of the main reasons for the persistently high blood sugar level in diabetic patients, and it is also the main culprit of fasting hyperglycemia in patients
.
Hepatic gluconeogenesis mediated by the key CREB/CRTC2 transcriptional complex in the liver is one of the main pathways of the body's blood glucose elevation
.
CREB/CRTC2 protein-protein interaction inhibitors can regulate the expression of downstream gluconeogenesis-related genes and reduce fasting blood glucose by inhibiting gluconeogenesis
.
Propolis is a viscous solid gelatinous substance formed by mixing plant resin collected by bees with secretions such as mandibular glands and wax glands
.
Propolis has been used for centuries as a traditional folk medicine to treat a variety of ailments, and it has been found to improve diabetes complications by lowering glucose and blood lipid levels
.
Although some of the characteristic compounds in propolis, such as polyphenols, flavonoids, and caffeic acid, have been reported to improve metabolic syndrome, identifying novel targets of active compounds from propolis and exploring their underlying mechanisms remains a serious challenge
.
On January 11, 2022, the team of Prof.
Liu Yu from Fudan University, Prof.
Liu Hong from Shanghai Institute of Materia Medica, Chinese Academy of Sciences, and Prof.
Hu Lihong from Nanjing University of Traditional Chinese Medicine published a paper entitled: A propolis-derived small molecule ameliorates metabolic rate in the journal Nature Communications.
Research paper on syndrome in obese mice by targeting the CREB/CRTC2 transcriptional complex
.
This study has made important progress in the research of CREB/CRTC2 protein-protein interaction inhibitor, a new target of diabetes
.
For the first time, it was verified that the main component of Brazilian propolis, artepillin C (artepillin C), can inhibit the CREB/CRTC2 protein-protein interaction, and it was verified that the natural product apidilin C binds to CREB and blocks CREB/CRTC2 protein- Protein interaction, regulating the expression of gluconeogenesis-related genes, and then exerting the therapeutic effect of reducing fasting blood sugar
.
In this study, the researchers verified for the first time that the main component of Brazilian propolis, artepillin C (artepillin C), can inhibit the CREB/CRTC2 protein-protein interaction, and at the same time reduce fasting blood glucose and increase insulin in db/db mice Sensitivity, lowers blood lipid levels in the body
.
Through in vitro and in vivo experiments, it was verified that the natural product Apidiline C binds to CREB, blocks the CREB/CRTC2 protein-protein interaction, regulates the expression of gluconeogenesis-related genes, and then exerts the therapeutic effect of reducing fasting blood sugar
.
In order to improve the inhibitory effect and druggability of the natural product Apideline C on the CREB/CRTC2 protein-protein interaction, the researchers comprehensively used a variety of structural optimization and design strategies in medicinal chemistry to conduct the CREB/CRTC2 protein-protein interaction inhibitor.
Structure-activity relationship study and pharmacological activity evaluation
.
Through multiple rounds of structural optimization, it was found that the lead compound A57 targeting the CREB/CRTC2 protein-protein interaction inhibitor has a strong inhibitory effect on the CREB/CRTC2 protein-protein interaction with IC50 reaching 0.
74 μM, which is a natural product of apidiline 30 times the inhibitory activity of C; Compound A57 significantly inhibited the transcription levels of gluconeogenesis rate-limiting enzyme genes Pck1 and G6pc; oral administration significantly reduced fasting blood glucose and blood lipid levels in db/db mice, but not in CRTC2 KO mice The glucose activity further verified the hypoglycemic mechanism of the lead compound A57
.
The research work provides a new target and a new treatment strategy for diabetic patients with poor fasting blood glucose treatment effect.
The discovery of the lead compound A57 has laid a research foundation for the development of class I diabetes drugs with China's independent intellectual property rights
.
Chen Yaqiong from Fudan University and Wang Jiang from Shanghai Institute of Materia Medica, Chinese Academy of Sciences are the co-first authors of the article; Professor Liu Xun from Fudan University, Professor Liu Hong from Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Professor Hu Lihong from Nanjing University of Traditional Chinese Medicine are the joint correspondents of the article author
.
Full text link: https:// Open for reprinting, welcome to forward to Moments and WeChat groups
.
The abnormal activity of hepatic gluconeogenesis is one of the main reasons for the persistently high blood sugar level in diabetic patients, and it is also the main culprit of fasting hyperglycemia in patients
.
Hepatic gluconeogenesis mediated by the key CREB/CRTC2 transcriptional complex in the liver is one of the main pathways of the body's blood glucose elevation
.
CREB/CRTC2 protein-protein interaction inhibitors can regulate the expression of downstream gluconeogenesis-related genes and reduce fasting blood glucose by inhibiting gluconeogenesis
.
Propolis is a viscous solid gelatinous substance formed by mixing plant resin collected by bees with secretions such as mandibular glands and wax glands
.
Propolis has been used for centuries as a traditional folk medicine to treat a variety of ailments, and it has been found to improve diabetes complications by lowering glucose and blood lipid levels
.
Although some of the characteristic compounds in propolis, such as polyphenols, flavonoids, and caffeic acid, have been reported to improve metabolic syndrome, identifying novel targets of active compounds from propolis and exploring their underlying mechanisms remains a serious challenge
.
On January 11, 2022, the team of Prof.
Liu Yu from Fudan University, Prof.
Liu Hong from Shanghai Institute of Materia Medica, Chinese Academy of Sciences, and Prof.
Hu Lihong from Nanjing University of Traditional Chinese Medicine published a paper entitled: A propolis-derived small molecule ameliorates metabolic rate in the journal Nature Communications.
Research paper on syndrome in obese mice by targeting the CREB/CRTC2 transcriptional complex
.
This study has made important progress in the research of CREB/CRTC2 protein-protein interaction inhibitor, a new target of diabetes
.
For the first time, it was verified that the main component of Brazilian propolis, artepillin C (artepillin C), can inhibit the CREB/CRTC2 protein-protein interaction, and it was verified that the natural product apidilin C binds to CREB and blocks CREB/CRTC2 protein- Protein interaction, regulating the expression of gluconeogenesis-related genes, and then exerting the therapeutic effect of reducing fasting blood sugar
.
In this study, the researchers verified for the first time that the main component of Brazilian propolis, artepillin C (artepillin C), can inhibit the CREB/CRTC2 protein-protein interaction, and at the same time reduce fasting blood glucose and increase insulin in db/db mice Sensitivity, lowers blood lipid levels in the body
.
Through in vitro and in vivo experiments, it was verified that the natural product Apidiline C binds to CREB, blocks the CREB/CRTC2 protein-protein interaction, regulates the expression of gluconeogenesis-related genes, and then exerts the therapeutic effect of reducing fasting blood sugar
.
In order to improve the inhibitory effect and druggability of the natural product Apideline C on the CREB/CRTC2 protein-protein interaction, the researchers comprehensively used a variety of structural optimization and design strategies in medicinal chemistry to conduct the CREB/CRTC2 protein-protein interaction inhibitor.
Structure-activity relationship study and pharmacological activity evaluation
.
Through multiple rounds of structural optimization, it was found that the lead compound A57 targeting the CREB/CRTC2 protein-protein interaction inhibitor has a strong inhibitory effect on the CREB/CRTC2 protein-protein interaction with IC50 reaching 0.
74 μM, which is a natural product of apidiline 30 times the inhibitory activity of C; Compound A57 significantly inhibited the transcription levels of gluconeogenesis rate-limiting enzyme genes Pck1 and G6pc; oral administration significantly reduced fasting blood glucose and blood lipid levels in db/db mice, but not in CRTC2 KO mice The glucose activity further verified the hypoglycemic mechanism of the lead compound A57
.
The research work provides a new target and a new treatment strategy for diabetic patients with poor fasting blood glucose treatment effect.
The discovery of the lead compound A57 has laid a research foundation for the development of class I diabetes drugs with China's independent intellectual property rights
.
Chen Yaqiong from Fudan University and Wang Jiang from Shanghai Institute of Materia Medica, Chinese Academy of Sciences are the co-first authors of the article; Professor Liu Xun from Fudan University, Professor Liu Hong from Shanghai Institute of Materia Medica, Chinese Academy of Sciences and Professor Hu Lihong from Nanjing University of Traditional Chinese Medicine are the joint correspondents of the article author
.
Full text link: https:// Open for reprinting, welcome to forward to Moments and WeChat groups