2 results about "Cucurbitacin B" patented technology

The present application relates to the technical field of biological medicine, and specifically discloses a small-molecule coupling compound targeting ASGPR, which has the following general formula: wherein X is a small-molecule ligand with the ability to target ASGPR; and Y is a derivative of cucurbitacin B. . The small-molecule coupling compound can be used in the preparation of a drug targeting ASGPR and having the functions of precise chemotherapy and radiotherapy sensitization. The small-molecule coupling compound prepared by the present application can achieve precise killing of liver cancer cells; the water solubility of cucurbitacin B is improved after coupling; the small-molecule coupling compound integrates precise chemotherapy and radiotherapy sensitization, and can significantly enhance the cancer-killing effect in combination with low-dose radiotherapy; and the small-molecule coupling compound has no obvious systemic toxicity and is well tolerated by patients.

The application discloses a cucurbitacin B derivative A2, a preparation method and application thereof, and the structural formula of the cucurbitacin B derivative A2 is provided. 50 The cucurbitacin B derivative A2 provided by the application has a strong inhibitory effect on the proliferation activity of a human non-small cell lung cancer cell line A549, and the IC value is only 0.009 muM, which is increased by nearly 10 times than the inhibitory activity of cucurbitacin B on the proliferation of A549, and the toxicity to normal cells L02 is reduced by nearly 10 times, and the selectivity coefficient is increased by nearly 100 times than cucurbitacin. The xenograft mouse experiment result is consistent with the cell result, and can be used as a candidate drug for treating human non-small cell lung cancer; the preparation method has the advantages of rich raw material source, mild reaction condition, convenient operation in reaction process, cheap and easily obtained reagent, low toxicity or non-toxicity, low cost and suitability for industrial production.