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New effect of old medicine, may provide new therapy for type 2 diabetes

2017-07-07 来源:转载自第三方
7 July 2017

  Researchers from the University of California, San Diego, and the University of Michigan recently published an article entitled "Inhibition of IKK? and TBK1 Improves Glucose Control in a Subset of Patients with Type 2 Diabetes" at "Cell Metabolism". Amlexanox, an anti-inflammatory and anti-allergy drug developed for the treatment of asthma 30 years ago, is likely to become a new treatment for type 2 diabetes.

  Amlexanox under the trade name Aphthasol, an inhibitor of both enzymes IKKε and TBK1, is an anti-inflammatory anti-allergic immunomodulator that is used clinically for the treatment of oral ulcers, allergic rhinitis, conjunctivitis and asthma. In the 1980s, it was developed by Japan, but soon it was replaced by more effective drugs. Recently, this old drug has brought new surprises to scientists: researchers from School of Medicine, the University of California, San Diego and the University of Michigan reported that 12 weeks after taking Amlexanox, the blood glucose showed significant reduce in a small part of patients with type 2 diabetes.
  This is not an accidental discovery, but through rigorous screening of modern drugs. As early as a few years ago, Dr. Alan R. Saltiel and his team found that both enzymes (IKKε and TBK1) were induced in obese mice, resulting in decreased energy consumption or reduced calorie consumption. Thus, they began to screen through the library of 150,000 kinds of chemical substances to find IKKε and TBK1 inhibitors. Eventually, they found Amlexanox. Amlexanox not only can lose weight in obese mice, but also increase their sensitivity to insulin and improve diabetes and fatty liver disease. And these responses also occur in humans.
  In order to verify the potential of Amlexanox in the treatment of diabetes, the team conducted a blindless safety test. Subsequently, 42 cases of obese type 2 diabetes patients were controlled by the test. The subjects measured blood glucose, insulin sensitivity, body weight and liver fat. A biopsy of adipocytes in the abdomen of each patient was collected before and after the test to measure changes in gene expression. The study showed that one-third of the participants who received Amlexanox had responded to Amlexanox.
  Why some patients respond to Amlexanox, while others do not respond to Amlexanox? Researchers carried out molecular analysis of fat cells from patients. The results showed that at the beginning of the study, the level of inflammation in the adipose cells was higher than that in the untreated group. This suggests that inflammation may trigger a patient response to Amlexanox. In addition, it is truly surprising that more than 1,100 genes have changed only in the responders.
  This result is exciting, old drugs, new use, Amlexanox may become a new therapy for type 2 diabetes. But there are many problems to be solved, such as drug dose, medication time, duration of efficacy and so on. Researchers are currently planning a new study to examine whether patients who are likely to respond based on potential inflammation can be differentiated, and that their use with another drug may be more effective in treating diabetes.
Edited by Suzhou Yacoo Science Co., Ltd.