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Kenyan PhD student from SAJOREC participated in the development of drug candidates with anti-pruritic function


 Itching, also known as pruritus, is the most frequent skin disease. It has a significant impact on people's mental health and social life. Repeated scratching by patients who suffer from itching will lead to the release of itching factors and to the aggravation of skin lesions, thereby seriously affecting the patients' mental health and quality of life. The etiology of pruritus is extremely complex, involving hematologic malignancy, renal failure, endocrine and metabolic changes, and other internal factors, as well as environmental factors such as constantly changing humidity and occasional chemical stimulation. Given the complexity of the causes of itching, developing safe and effective drugs to treat it is extremely difficult.


Recently, a selective TRPV3 antagonist has been identified by Ren Lai’s research group from Sino-Africa Joint Research Center, Kunming Institute of Zoology, Chinese Academy of Sciences. The research results were published in the British Journal of Pharmacology under the title 'A plant-derived TRPV3 inhibit or suppressing pain and itch'. (2021, 178(7):1669-1683), and has been applied for invention patent protection. Peter Muiruri Kamau, a PhD student from Kenya, is co-first author of the paper.


The transient receptor potential vanilloid 3 (TRPV3) channel is a promising target for treating pruritus. FlexStation and calcium fluorescence imaging were conducted to track the functional compounds. Whole-cell patch clamp was used torecord itch-related ion channel currents. Homologous recombination and site-directed mutagenesis were employed to construct TRPV3 channel chimeras and point mutations in order to explore the pharmacological mechanism. Mouse models were used for in vivo anti-pruritus assays. An acridone alkaloid (citrusinine-II) was purified and characterized from Atalantia monophylla. Citrusinine-II directly interacts with Y564 within the S4 helix of TRPV3 to selectively inhibit the channel with a half maximal inhibitory concentration (IC50) of 12.43 μM. Citrusinine-II showed potential efficacy to alleviate both chronic and acute itch. Intradermal administration of citrusinine-II (143ng/skin site) almost inhibited itching completely. It also showed significant analgesic effects. Little side effects of the compound have been observed. By acting as a selective and potent inhibitor of TRPV3 channel, citrusinine-II showed valuable therapeutic effects in pruritus animal models and is a promising candidate drug and/or lead molecule for the development of anti-pruritus drugs.