Application of PKC enzyme inhibitor in preparing drug for improving and protecting islet beta cell functions
A technology of inhibitors and uses, applied in the field of medicine, can solve problems such as unoptimistic control of type 2 diabetes, loss of islet beta cell function, and aggravation of diabetes, etc., to improve and protect islet beta cells, endoplasmic reticulum stress inhibition, good inhibitory effect
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Embodiment 1
[0031] This example is illustrated with the non-selective PKC enzyme inhibitor Ro31-8220. The structure of the compound Ro31-8220 is as follows:
[0032]
[0033] The non-selective PKC enzyme inhibitor Ro31-8220 can inhibit the apoptosis of beta cells induced by thapsigargin (THAP) at a lower concentration (1.25μM). Ro31-8220 can also significantly inhibit the expression of TXNIP at a lower concentration, and can also effectively inhibit the expression of mRNA and protein related to endoplasmic reticulum stress. It can be further developed as a drug for treating diabetes and has broad application prospects. The following experiments are used for verification.
[0034] 1. The experiment of Ro31-8220 inhibiting the apoptosis of INS-1 cells induced by THAP
[0035] INS-1 cells are rat pancreatic tumor cells, which are one of the most widely used cells in diabetes research. It is reported that THAP can induce endoplasmic reticulum stress, inflammatory response, autophagy and...
Embodiment 2
[0070] Sotrastaurin, a non-selective PKC enzyme inhibitor, inhibits the expression of TXNIP induced by thapsigargin (THAP)
[0071] TXNIP plays an important role in INS-1 cells, it can mediate the endoplasmic reticulum stress of INS-1 cells, induce inflammation and promote apoptosis and autophagy, and the overexpression of TXNIP can also inhibit INS-1 Cellular insulin secretion, in order to verify that other PKC inhibitors also have this effect, so the inhibitory level of Sotrastaurin on the expression of TXNIP protein was detected under a series of concentration gradients, so as to confirm the inhibitory effect of other PKC inhibitors, which can further clarify the effect of PKC inhibitors on INS- 1 Effects on cell function.
[0072] The experimental steps are as follows:
[0073] 1 Collect the total cell protein: INS-1 cells were treated with Sotrastaurin and THAP drugs, extract the protein for 24 hours: wash the cells with cold PBS, add RIPA lysate to each well of the 6-we...
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