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.
ກຸ່ມ Lincosamide ຂອງ ຢາຕ້ານເຊື້ອ comprising particularly of clindamycin is a safe common ຢາຕ້ານເຊື້ອ available orally. It is a bacteriostatic agent and acts by binding to bacterial ribosomes. Lincomycin, the first ຢາຕ້ານເຊື້ອ of this group was isolated from soil bacteria Streptomyces lincolnensis ໃນປີ 1963 ແລະນໍາໃຊ້ຕໍ່ກັບ Gram positive ເຊື້ອແບັກທີເຣັຍ.
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 ຢາຕ້ານເຊື້ອ in this group saw light of the day despite hard efforts in the past few decades.
ບໍ່ດົນມານີ້, ນັກຄົ້ນຄວ້າໄດ້ລາຍງານການສັງເຄາະທາງເຄມີຂອງ Iboxamycin (IBX), lincosamide ໃຫມ່ທີ່ພົບວ່າມີປະສິດທິພາບສູງຕໍ່ກັບເຊື້ອແບັກທີເຣັຍ Gram-positive ແລະ Gram-negative ໃນ. ໃນ vitro ແລະ in 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 ຢາຕ້ານເຊື້ອ 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 ຢາຕ້ານເຊື້ອ candidate is very significant in the current times, when commonly used ຢາຕ້ານເຊື້ອ have increasingly lost shine due to evolution of multiple drug-resistance (MDR), caused mainly as a result of indiscriminate use of ຢາຕ້ານເຊື້ອ, ດັ່ງນັ້ນຈຶ່ງເຮັດໃຫ້ ຢາຕ້ານເຊື້ອ resistance a serious threat to global health.
ນອກຈາກນັ້ນ, ບໍ່ເຫມືອນກັບ Lincomycin ແລະ Clindamycin ທີ່ເປັນທໍາມະຊາດແລະເຄິ່ງສັງເຄາະຕາມລໍາດັບ, Iboxamycin (IBX) ຜູ້ສະຫມັກທີ່ຖືກພັດທະນາໃຫມ່ແມ່ນສັງເຄາະຢ່າງສົມບູນ, ຫມາຍຄວາມວ່າການມີຢູ່ຂອງມັນອາດຈະບໍ່ຂຶ້ນກັບແຫຼ່ງທໍາມະຊາດຢ່າງເຕັມທີ່, ແລະດັ່ງນັ້ນການຜະລິດອຸດສາຫະກໍາຂອງມັນສາມາດຂະຫຍາຍອອກໄດ້ຢ່າງງ່າຍດາຍ. ເພື່ອຕອບສະຫນອງຄວາມຕ້ອງການທີ່ສູງຂຶ້ນ. ນອກຈາກນີ້, ການສັງເຄາະຂອງ analogs ຫຼາຍແມ່ນເປັນໄປໄດ້ຍ້ອນວ່າຂະບວນການແມ່ນອີງໃສ່ອົງປະກອບ. ຫຼັກຖານເພີ່ມເຕີມຂອງປະສິດທິພາບແລະຄວາມປອດໄພຂອງມັນຈະສາມາດໃຊ້ໄດ້ຫຼັງຈາກການລິເລີ່ມຂອງການທົດລອງທາງດ້ານການຊ່ວຍ, ເຊິ່ງຈະເກີດຂຶ້ນພຽງແຕ່ໃນເວລາທີ່ອຸດສາຫະກໍາການຢາໄດ້ມີສ່ວນຮ່ວມແລະໄດ້ຮັບສິດທິບັດສິດທິບັດຈາກ inventors, ເພື່ອຂະຫຍາຍຕື່ມອີກ.
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ແຫລ່ງທີ່ມາ:
- Mitcheltree, MJ, Pisipati, A., Syroegin, EA et al. ປະເພດຢາຕ້ານເຊື້ອສັງເຄາະທີ່ເອົາຊະນະຄວາມຕ້ານທານຢາຂອງແບັກທີເລຍ. ຈັດພີມມາ: 27 ຕຸລາ 2021. ທໍາມະຊາດ (2021). DOI: https://doi.org/10.1038/s41586-021-04045-6
- Mason J., et al 2021. Practical Gram-Scale Synthesis of Iboxamycin, a potent antibiotic candidate. J. ອຳ. ເຄັມ. Soc. 2021, 143, 29, 11019–11025. ວັນທີເຜີຍແຜ່: 15 ກໍລະກົດ 2021. DOI: https://doi.org/10.1021/jacs.1c03529 ມີຢູ່ໃນ ການເຊື່ອມຕໍ່
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