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- 저자 : 콩가라다무다 (검색결과 2 건)
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이주미,콩가라다무다,이연택,이재용,전성호,이정태 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.8
The first synthesis of novel hybrid compounds 3?6 from epinastine (1) and salicylic acid (2) has been achieved via amide bond using molecular hybridization approach and their in vitro inhibitory activity towards nitric oxide (NO) formation in lipopolysaccharide (LPS) induced RAW 264.7 macrophages as a sign of anti-inflammatory activity has been evaluated. All the hybrid compounds synthesized 3?6 displayed better inhibitory effect against NO production than individual compounds, 1 and 2. Especially, directly conjugated hybrid compound 3 displayed concentration-dependent strong inhibition of NO production with an IC50 value of 12.78??M, which was significantly lower than the parent compounds 1 (IC50?>?100??M) and 2 (IC50?>?100??M). These preliminary results indicate that further studies are needed to be carried out to demonstrate the mechanism by which compound 3 exerts its inhibitory activity.
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이주미,콩가라다무다,Yeontaek Lee,Hyeong Ryeol Woo,서홍원,전성호,이정태 대한화학회 2020 Bulletin of the Korean Chemical Society Vol.41 No.4
A set of novel epinastine (1) and mefenamic acid (2) hybrids (3?7) tethered via amide bond were designed and synthesized with the artistry of molecular hybridization. Then their inhibitory effect on nitric oxide (NO) production in LPS-induced RAW-264.7 macrophages and the expression levels of prostaglandin (PG) synthesis regulatory genes were evaluated in vitro. All the hybrids were found to have remarkable NO production inhibitory potential with IC50 values ranging in between 27.69?±?3.06 and 40.19?±?5.52??M without notable cytotoxicity (CC50?≥?100??M) except 6. Comparing the inhibitory effects, cytotoxicity and in vitro efficacy index (iEI), 4 (IC50 = 32.09?±?4.04??M; iEI = 6.23) and 7 (IC50 = 27.69?±?3.06??M; iEI = 6.40) were better suited than other hybrids as well as their parent compounds EH and MA. This outcome was further harmonized with the reduced microsomal prostaglandin E synthase-1 expression and unaltered housekeeping COX-1 expression by hybrids 4 and 7 treatment. Altogether, our findings signify that hybrids 4 and 7 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.
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