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RISS 인기검색어
- 검색키워드
- 저자 : Nazmul Qais (검색결과 3 건)
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Arifur Rahman,Nazmul Hasan Naheed,Sabreena Chowdhury Raka,Nazmul Qais,AZM Ruhul Momen 경희대학교 융합한의과학연구소 2020 Oriental Pharmacy and Experimental Medicine Vol.20 No.4
Inhibition of BCR–ABL tyrosine kinase plays a crucial role in the management of chronic myelogenous leukemia (CML). The suppression of CML is getting harder because of a distinct pattern of resistance. Developing new types of ABL tyrosine kinase inhibitors along with ABL2, CSF1R, KIT, LCK, PDGFRA, and PDGFRB inhibitors is the main objective of this study that may overcome the drug resistance issue. The current study has been conducted using a kinase database containing 177,000 bioactive molecules, the top 135 molecules were selected with the best docking score and subjected to comprehensive ADMET profiling, multi-target analysis. Based on consensus molecular docking score (AutoDock, Chimera, Achilles, and Mcule), 22 molecules have been screened out which later undertaken for ADME/T profiling. After profiling of ADME/T data, selected molecules subjected to docking with multiple targets. Finally, molecular dynamics simulations had performed to screen the binding accuracy of the four lead molecules with ABL1. MD simulations of the desired complex (ABL1, ABL2, CSF1R, KIT, LCK, PDGFRA, and PDGFRB, among them ABL1 was the prime target) performed and found that PCID 10181160 and PCID 72724706 are the most promising inhibitors comparing to imatinib. These lead molecules are the potential CML inhibitors that could resolve the resistance pattern. Further chemical synthesis, wet lab analysis, and experimental validation deserve the utmost attention.
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Mahmud, Zobaer A.,Bachar, Sitesh C.,Qais, Nazmul 경희한의학연구센터 2011 Oriental Pharmacy and Experimental Medicine Vol.11 No.4
The ethanolic extracts of leaves and roots of $Premna$ $esculenta$ (Roxb.) were evaluated for antihyperlipidemic activity in poloxamer 407 induced hyperlipidemic rats and mice. The administration of the ethanolic extract of leaves induced a significant ($p$ <0.05) reduction in serum total cholesterol (TC), triglycerides (TG), low density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels as well as the atherogenic index compared to the P-407 induced hyperlipidemic control mice after 24 h of treatment at a single dose of 500 mg/kg p.o. Both the leaf and root extracts significantly ($p$ <0.05) reduced the serum TC, TG, VLDL and LDL levels as well as the atherogenic index compared to P-407 induced hyperlipidemic control rats after 4 days of pretreatment at a dose of 250 mg/kg/day p.o. The lipid lowering effects were compared with standard drug atorvastatin (50 mg/kg p.o.). Furthermore, both extracts showed potential to moderate scavenging activity of superoxide, nitric oxide and DPPH free radicals. In DPPH radical scavenging assay the $IC_{50}$ values of the leaf and root extracts were found to be 425.79 and 20.26 ${\mu}g$/ml, respectively while ascorbic acid has the $IC_{50}$ value 16.34 ${\mu}g$/ml. The $IC_{50}$ values of the leaf and root extracts against superoxide radicals were found to be 109.57 and 366.2 ${\mu}g$/ml, respectively which were comparable to that of ascorbic acid (99.66 ${\mu}g$/ml). The findings of the investigation demonstrated both antihyperlipidemic and antioxidant activities of the leaf and root extracts of $P.$ $esculenta$ which could help in prevention of hyperlipidemia associated disorders.
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Zobaer A. Mahmud,Sitesh C. Bachar,Nazmul Qais 경희대학교 융합한의과학연구소 2011 Oriental Pharmacy and Experimental Medicine Vol.11 No.4
The ethanolic extracts of leaves and roots of Premna esculenta (Roxb.) were evaluated for antihyperlipidemic activity in poloxamer 407 induced hyperlipidemic rats and mice. The administration of the ethanolic extract of leaves induced a significant (p<0.05) reduction in serum total cholesterol (TC), triglycerides (TG), low density lipoprotein (LDL) and very low density lipoprotein (VLDL)levels as well as the atherogenic index compared to the P-407induced hyperlipidemic control mice after 24 h of treatment at a single dose of 500 mg/kg p.o. Both the leaf and root extracts significantly (p<0.05) reduced the serum TC, TG, VLDL and LDL levels as well as the atherogenic index compared to P-407 induced hyperlipidemic control rats after 4 days of pretreatment at a dose of 250 mg/kg/day p.o. The lipid lowering effects were compared with standard drug atorvastatin (50 mg/kg p.o.). Furthermore, both extracts showed potential to moderate scavenging activity of superoxide,nitric oxide and DPPH free radicals. In DPPH radical scavenging assay the IC_(50) values of the leaf and root extracts were found to be 425.79 and 20.26 μg/ml, respectively while ascorbic acid has the IC_(50) value 16.34 μg/ml. The IC_(50)values of the leaf and root extracts against superoxide radicals were found to be 109.57 and 366.2 μg/ml,respectively which were comparable to that of ascorbic acid (99.66 μg/ml). The findings of the investigation demonstrated both antihyperlipidemic and antioxidant activities of the leaf and root extracts of P. esculenta which could help in prevention of hyperlipidemia associated disorders.
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