Development of multi-drug resistance (MDR) bacteria in the past five decades have led to increasing research in search of a drug candidate to address this AMR issue. A fully synthetic broad-spectrum antibiotic, Iboxamycin, provides hope to treat both Gram-positive and Gram-negative bacteria via a bacteriostatic mechanism.
Kikundi cha Lincosamide antibiotics comprising particularly of clindamycin is a safe common antibiotic available orally. It is a bacteriostatic agent and acts by binding to bacterial ribosomes. Lincomycin, the first antibiotic of this group was isolated from soil bacteria Streptomyces lincolnensis mnamo 1963 na kutumika dhidi ya Gram positive vimelea.
Clindamycin, the semi-synthetic version of lincomycin has been in use for the last 50 years as an antibacterial (and antimalarial drug), particularly for the treatment of dental and bone infections. Because of its widespread use for about five decades, multiple resistance genes have now evolved, making clindamycin less effective against several bacteria in the community. Also, no other antibiotic in this group saw light of the day despite hard efforts in the past few decades.
Hivi karibuni watafiti wameripoti usanisi wa kemikali wa Iboxamycin (IBX), riwaya ya lincosamide ambayo imegundulika kuwa na ufanisi mkubwa dhidi ya bakteria zote za Gram-chanya na Gram-negative vitro na katika vivo animal studies. Through structure-based design and component-based synthesis, they developed a scaffold and linked that to the amino-octose residue of clindamycin. The result is Iboxamycin, an antibiotic which has been found to be exceptionally potent against a wide range of pathogenic bacteria in pre-clinical studies on mice. It targets wild-type and resistant bacteria and exhibits prolonged bacteriostatic effects following even brief exposure.
Development of this broad-spectrum antibiotic candidate is very significant in the current times, when commonly used antibiotics have increasingly lost shine due to evolution of multiple drug-resistance (MDR), caused mainly as a result of indiscriminate use of antibiotics, hivyo kutengeneza antibiotic resistance a serious threat to global health.
Kwa kuongeza, tofauti na Lincomycin na Clindamycin ambazo ni za asili na nusu-synthetic kwa mtiririko huo, mgombea mpya wa Iboxamycin (IBX) ameundwa kikamilifu, ikimaanisha kuwa upatikanaji wake hauwezi kutegemea vyanzo vya asili, na hivyo uzalishaji wake wa viwanda unaweza kuongezwa kwa urahisi. kukidhi mahitaji ya juu. Pia, usanisi wa analogi kadhaa pia inawezekana kwani mchakato unategemea sehemu. Uthibitisho zaidi wa ufanisi na usalama wake utapatikana baada ya kuanzishwa kwa majaribio ya kimatibabu, ambayo yatafanyika tu wakati tasnia ya maduka ya dawa itajihusisha na kupata haki za hataza kutoka kwa wavumbuzi, ili kuongezeka zaidi.
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Vyanzo:
- Mitcheltree, MJ, Pisipati, A., Syroegin, EA et al. Kikundi cha dawa za syntetisk zinazoshinda upinzani wa dawa nyingi za bakteria. Iliyochapishwa: 27 Oktoba 2021. Nature (2021). DOI: https://doi.org/10.1038/s41586-021-04045-6
- Mason J., et al 2021. Usanisi wa Kitendo wa Gram-Scale wa Iboxamycin, Mgombea Mwenye Uwezo wa Kupambana na Viuavijasumu. J. Am. Chem. Soc. 2021, 143, 29, 11019–11025. Tarehe ya Kuchapishwa: Julai 15, 2021. DOI: https://doi.org/10.1021/jacs.1c03529 Inapatikana kwenye kiungo
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