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Synthesis and Biological Studies of Novel Biphenyl-3,5-dihydro-2H-thiazolopyrimidines Derivatives
Maddila, S.,Damu, G.L.V.,Oseghe, E.O.,Abafe, O.A.,Rao, C. Venakata,Lavanya, P. Korean Chemical Society 2012 대한화학회지 Vol.56 No.3
A new series of ethyl 2-(4-substitutedbenzylidene)-5-(3'-(ethoxycarbonyl)biphenyl-4-yl)-7-methyl-3-oxo-3,5-dihydro-2H-thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives ($\mathbf{8a-j}$) were synthesized. The newly synthesized compounds were characterized by $\mathbf{IR}$, $^1\mathbf{H}$ $\mathbf{NMR}$, $^{13}\mathbf{C}$ $\mathbf{NMR}$, $\mathbf{LCMS}$ $\mathbf{mass}$ and $\mathbf{C}$, $\mathbf{H}$, $\mathbf{N}$ analyses. All newly synthesized compounds were screened for their In vitro antioxidant activity (Scavenging of hydrogen peroxide, Scavenging of nitric oxide radical, and Lipid peroxidation inhibitory activity), antibacterial (Escheria coli, Pseudonmonas aeruginosa (gram-negative bacteria), Bacillus subtillis, Staphylococcus aureus (gram-positive bacteria)) and antifungal (Candida albicans Aspergillus niger) studies.
Kuo, Ping-Chung,Damu, Amooru G.,Cherng, Ching-Yuh,Jeng, Jye-Fu,Teng, Che-Ming,Lee, E-Jian,Wu, Tian-Shung The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.5
In the present study, the antioxidative and inhibitory activity of Zingiber officinale Rosc. Rhizomes-derived materials (on mushroom tyrosinase) were evaluated. The bioactive co mponents of Z. officinale rhizomes were characterized by spectroscopic analysis as zingerone and dehydrozingerone, which exhibited potent antioxidant and tyrosinase inhibition activities. A series of substituted dehydrozingerones [(E)-4-phenyl-3-buten-2-ones] were prepared in admirable yields by the reaction of appropriate benzaldehydes with acetone and the products were evaluated in terms of variation in the dehydrozingerone structure. The synthetic analogues were examined for their antioxidant and antityrosinase activities to probe the most potent analogue. Compound 26 inhibited Fe$^{2+}$-induced lipid peroxidation in rat brain homogenate with an IC$_{50}$ = 6.3${\pm}$0.4 ${\mu}$M. In the 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical quencher assay, compounds 2, 7, 17, 26, 28, and 29 showed radical scavenging activity equal to or higher than those of the standard antioxidants, like ${\alpha}$-tocopherol and ascorbic acid. Compound 27 displayed superior inhibition of tyrosinase activity relative to other examined analogues. Compounds 2, 17, and 26 exhibited non-competitive inhibition against oxidation of 3,4- dihydroxyphenylalanine (L-DOPA). From the present study, it was observed that both number and position of hydroxyl groups on aromatic ring and a double bond between C-3 and C-4 played a critical role in exerting the antioxidant and antityrosinase activity.
Huatao Li,Jinjin Tong,Damu Tang,Wenru Tian,Yun Liu 대한수의학회 2016 Journal of Veterinary Science Vol.17 No.2
Hematoporphyrin monomethyl ether (HMME) combined with He-Ne laser irradiation is a novel and promising photodynamic therapy (PDT)-induced apoptosis that can be applied in vitro on canine breast cancer cells. However, the exact pathway responsible for HMME-PDT in canine breast cancer cells remains unknown. CHMm cells morphology and apoptosis were analyzed using optical microscope, terminal deoxynucleotidyl transferase dUTP nick end labeling fluorescein staining and DNA ladder assays. Apoptotic pathway was further confirmed by Real-time-polymerase chain reaction and Western blotting assays. Our results showed that HMME-PDT induced significant changes in cell morphology, such as formation of cytoplasmic vacuoles and the gradual rounding of cells coupled with decreased size and detachment. DNA fragmentation and cell death was shown to occur in a time-dependent manner. Furthermore, HMME-PDT increased the activities of caspase-9 and caspase-3, and released cytochrome c from mitochondria into the cytoplasm. HMME-PDT also significantly increased both mRNA and protein levels of Bax and decreased P53 gene expression in a time-dependent manner, while the mRNA and protein expression of Bcl-2 were repressed. These alterations suggest that HMME-PDT induced CHMm cell apoptosis via the mitochondrial apoptosis pathway and had anti-canine breast cancer effects in vitro.
Ping-Chung Kuo,Amooru G. Damu,Ching-Yuh Cherng,Jye-Fu Jeng,Che-Ming Teng,E-Jian Lee,Tian-Shung Wu 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.5
In the present study, the antioxidative and inhibitory activity of Zingiber officinale Rosc. rhizomes- derived materials (on mushroom tyrosinase) were evaluated. The bioactive components of Z. officinale rhizomes were characterized by spectroscopic analysis as zingerone and dehydrozingerone, which exhibited potent antioxidant and tyrosinase inhibition activities. A series of substituted dehydrozingerones [(E)-4-phenyl-3-buten-2-ones] were prepared in admirable yields by the reaction of appropriate benzaldehydes with acetone and the products were evaluated in terms of variation in the dehydrozingerone structure. The synthetic analogues were examined for their antioxidant and antityrosinase activities to probe the most potent analogue. Compound 26 inhibited Fe2+-induced lipid peroxidation in rat brain homogenate with an IC50 = 6.3±0.4 µM. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical quencher assay, compounds 2, 7, 17, 26, 28, and 29 showed radical scavenging activity equal to or higher than those of the standard antioxidants, like α-tocopherol and ascorbic acid. Compound 27 displayed superior inhibition of tyrosinase activity relative to other examined analogues. Compounds 2, 17, and 26 exhibited non-competitive inhibition against oxidation of 3,4- dihydroxyphenylalanine (L-DOPA). From the present study, it was observed that both number and position of hydroxyl groups on aromatic ring and a double bond between C-3 and C-4 played a critical role in exerting the antioxidant and antityrosinase activity.