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    Antibacterial and Antioxidant Activity of Isoflavans from the Roots of Rhynchosia ferruginea and In Silico Study on DNA Gyrase and Human Peroxiredoxin
    (2021) Hussien, Kalid; Eswaramoorthy, Rajalakshmanan; Melaku, Yadessa; Annisa, Milkyas Endale
    Rhynchosia ferruginea (Udusalim, Afan Oromo) is a medicinal plant traditionally used to treat skin infection, intestinal problems and amoebiasis. Silica gel chromatographic separation of dichloromethane/methanol (1:1) roots extract yielded isoflavan (1), isoflavene (2) and 1, 3-dilinoleoyl-2- stearoylglycerol (3), reported herein for the first time from the genus. Antibacterial activity was examined using disc diffusion method against E. coli, S. aureus, P. aeruginosa and S. pyogenes. AutoDoc vina 4.2 software was used for molecular docking analysis of compounds against human peroxiredoxin 5 and DNA gyrase B enzymes. Isoflavan (1) displayed zone of inhibition of 9.67 ± 0.58 mm and 10.67 ± 0.58 mm whereas isoflavene (2) showed 10.33 ± 1.15 mm and 10 ± 1.00 mm against E. coli and S. aureus, respectively, compared to ciprofloxacin (15.67±0.58 mm for both strains). DPPH radical scavenging assay of the dichloromethane/methanol (1:1) roots extract and isoflavan (1) exhibited better radical scavenging activity with $IC_{50}$ value of 17.7 and 32, respectively. Molecular docking analysis revealed that 1 and 2 exhibited similar binding affinity of -7.4 kcal/mol compared to ciprofloxacin (-7.3 kcal/mol). In silico analysis against human peroxiredoxin 5 (PDB ID: 1HD2) revealed minimum binding affinity of - 3.7 and - 2.0 kcal/mol for compounds 1 and 2, respectively, compared to ascorbic acid (-4.9 kcal/mol). The in vitro antibacterial and antioxidant activity of compounds 1 and 2 suggest the potential use of these compounds as drug lead candidates which corroborate with the traditional uses of the roots of R. ferruginea.
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    Molecular Docking, Antibacterial and Antioxidant Activities of Compounds Isolated from Ethiopian Plants
    (2022) Melaku, Yadessa; Getahun, Tokuma; Addisu, Markos; Tesso, Hailemichael; Eswaramoorthy, Rajalakshmanan; Garg, Ankita
    This study evaluated the antibacterial and antioxidant activities of the constituents of L. tomentosa and S. longipedunculata. The in-silico molecular docking analysis of the isolated compounds was also reported herein for the first time. The GC-MS analysis of the essential oil of L. tomentosa led to the identification of eleven components with 2,5-dimethoxy-p-cymene identified as the principal constituent (59.39%). Lauric acid (1), ?-stigmasterol (2), chrysophanol (3), and emodin (4) were isolated from L. tomentosa using silica gel column chromatography. Likewise, 9H-xanthene-3,5-diol (5), 1,7- dihydroxy-4-methoxyxanthone (6), and oleic acid (7) were isolated from S. longipedunculata. The structures of the isolated compounds were elucidated using UV-Vis, IR, and NMR spectroscopic methods. Compounds 3 and 4 are new to the genus Laggera, while 5 and 6 are new to the species S. longipedunculata. Compounds 3-6 inhibited DPPH radical by 86, 92, 88, and 90%, respectively. Compounds 5 and 6 inhibited 79.2 and 81.9% peroxide formation, respectively. The antioxidant activities displayed by compounds 4- 6 suggest their use as a natural antioxidant. Compounds 4 and 6 inhibited the growth of bacteria by 18.00±0.10 and 16.06±0.22 mm, respectively. Compounds 3, 4, and 6 showed binding affinities of ?10.4, ?10.4, and ?9.9 kcal/mol against Staphylococcus aureus DNA Gyrase, respectively, while 4 showed ?10.4 kcal/mol against human topoisomerase II?. Therefore, the present study results showed that emodin and 1,7-dihydroxy-4- methoxyxanthone might be considered lead compounds for further development as antibacterial and anti-cancer agents. The findings also substantiate the traditional use of these plants against bacteria.
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    Öğe
    Pharmacokinetics, drug-likeness, antibacterial and antioxidant activity of secondary metabolites from the roots extracts of Crinum abyssinicum and Calotropis procera and in silico molecular docking study
    (2022) Tegegn, Getachew; Melaku, Yadessa; Eswaramoorthy, Rajalakshmanan; Annisa, Milkyas Endale
    Crinum abyssinicum and Calotropis procera were traditionally used for the treatment of different diseases such as hypertension, diabetes, hepatitis B, skin infection, anticancer, asthma, fever, and diarrhea. The structures of the compounds were characterized by 1H NMR, 13C NMR, and DEPT-135 spectra. Compounds 1-3 were reported herein for the first time from the species of C. abyssinicum. The DCM/MeOH (1:1) and MeOH roots extracts of C. abyssinicum showed significant inhibitory activity against S. aureus and P. aeruginosa with a mean inhibition zone of 16.67 ± 1.20 and 16.33 ± 0.33 mm, respectively. Compounds 4 and 5 showed promising activity against E. coli with a mean inhibition zone of 17.7 ? 0.8 and 17.7 ? 1.2 mm, respectively. The results of DPPH activity showed the DCM: MeOH (1:1) and MeOH roots extracts of C. abyssinicum inhibited the DPPH radical by 52.86 ? 0.24 % and 45.6 ? 0.11 %, respectively, whereas compound 5 displayed 85.7 % of inhibition. The drug-likeness analysis showed that compounds 2-4 satisfy Lipinski’s rule of five with zero violations. Compounds 2, and 6 showed binding affinities of ?6.0, and ?6.7 kcal/mol against E. coli DNA gyrase B, respectively, while 3 and 5 showed ?5.0 and ?5.0 kcal/mol, respectively against human peroxiredoxin 5. Therefore, the in vitro antibacterial, radical scavenging activity along with the molecular docking analysis suggest the potential use of the extracts of C. abyssinicum and compounds 2, 5, 6, and 3, 5 can be considered as promising antibacterial agents and free radical scavengers, respectively.