Coumestrol (3,9-dihydroxy-6-benzofuran [3,2-c] chromenone) as a phytoestrogen and polyphenolic compound is a member of the Coumestans family and is quite common in plants. In this study, antiglaucoma, antidiabetic, anticholinergic, and antioxidant effects of Coumestrol were evaluated and compared with standards. To determine the antioxidant activity of coumestrol, several methods—namely N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD•+)-scavenging activity, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS•+)-scavenging activity, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH•)-scavenging activity, potassium ferric cyanide reduction ability, and cupric ion (Cu2+)-reducing activity—were performed. Butylated hydroxyanisole (BHA), Trolox, α-Tocopherol, and butylated hydroxytoluene (BHT) were used as the reference antioxidants for comparison. Coumestrol scavenged the DPPH radical with an IC50 value of 25.95 μg/mL (r2: 0.9005) while BHA, BHT, Trolox, and α-Tocopherol demonstrated IC50 values of 10.10, 25.95, 7.059, and 11.31 μg/mL, respectively. When these results evaluated, Coumestrol had similar DPPH•-scavenging effect to BHT and lower better than Trolox, BHA and α-tocopherol. In addition, the inhibition effects of Coumestrol were tested against the metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), and α-glycosidase, which are associated with some global diseases such as Alzheimer’s disease (AD), glaucoma, and diabetes. Coumestrol exhibited Ki values of 10.25 ± 1.94, 5.99 ± 1.79, 25.41 ± 1.10, and 30.56 ± 3.36 nM towards these enzymes, respectively. 相似文献
The reliance of tumor cells on aerobic glycolysis is one of the emerging hallmarks of cancer. Pyruvate kinase M2 (PKM2), an important enzyme of glycolytic pathway, is highly expressed in a number of cancer cells. Tumor cells heavily depend on PKM2 to fulfill their divergent energetic and biosynthetic requirements, suggesting it as novel drug target for cancer therapies. Based on this context, we performed enzymatic-assay-based screening of the in-house phenolic compounds library for the identification of PKM2 inhibitors. This screening identified silibinin, curcumin, resveratrol, and ellagic acid as potential inhibitors of PKM2 with IC50 values of 0.91 µM, 1.12 µM, 3.07 µM, and 4.20 µM respectively. For the determination of Ki constants and the inhibition type of hit compounds, Lineweaver–Burk graphs were plotted. Silibinin and ellagic acid performed the competitive inhibition of PKM2 with Ki constants of 0.61 µM and 5.06 µM, while curcumin and resveratrol were identified as non-competitive inhibitors of PKM2 with Ki constants of 1.20 µM and 7.34 µM. The in silico screening of phenolic compounds against three binding sites of PKM2 provided insight into the binding pattern and functionally important amino residues of PKM2. Further, the evaluation of cytotoxicity via MTT assay demonstrated ellagic acid as potent inhibitor of cancer cell growth (IC50 = 20 µM). These results present ellagic acid, silibinin, curcumin, and resveratrol as inhibitors of PKM2 to interrogate metabolic reprogramming in cancer cells. This study has also provided the foundation for further research to validate the potential of identified bioactive entities for PKM2 targeted-cancer therapies. 相似文献
The reactions of Cl3PN P(O)Cl2 ( 1 ) with primary and secondary amines have been studied. The following monophosphazenes, (RRN)3PN P(O)(NRR)2, and bis(phosphinoyl)amines, [(RRN)2P(O)]2NH were isolated: NRR = NHCH2Ph, Net2, NH(CH2)2CH3 groups for monophosphazenes, and Net2, NH(CH2)2CH3 for phosphinoyl amines. The unexpected geminal phosphazene, Cl(RRN)2PN P(O)Cl2, {RRN = N[CH(CH3)2]2}, was also obtained in moderate yield. The spectral data (IR, 1H, 13C, and 31P NMR, and MS) are presented. The structure of 1-(dichlorophosphinyl)-2-chloro-2,2-bis(diisopropylamino)phosphazene ( 5 ) was determined by X-ray crystallography. The basicities of these and related compounds in nonaqueous nitrobenzene solution were obtained by potentiometric titration. 相似文献
Silicon wafers are significantly utilized in integrated circuits and memory devices for the fabrication of novel semiconductor devices. As a result, a substantial amount of silicon wastes are generated every year. But recycling process of pure silicon waste is expensive with an additional problem related to chemical waste generation. Thus, the possibility of inevitable silicon waste conversion into potential nanostructures is not only beneficial for the semiconductor industry but also resolves current e-waste pollution. Hence, we successfully achieved hexagonal silicon carbide (SiC) nanowires under a strategic combination of waste silicon wafers and graphite powder by robust high-energy ball milling and heat treatment approaches. Structural, morphological, chemical, and optical properties of SiC nanowires are systematically studied by XRD, SEM, TEM, XPS, and optical absorbance. This facile experimental technique recognized the value of SiC nanowire generation for exploring multifunctional photoelectrochemical (PEC) water splitting and antibacterial activity. Accordingly, SiC nanowires achieved a photocurrent density of about 0.21 mA cm−2 vs. Ag/AgCl, which demonstrates enhanced light absorption capacity under reduced charge carrier recombination. Moreover, SiC nanowires prevailed decrement in the charge carrier resistance (27.53 Ω) under light state compared to the dark state (26.76 Ω). Specifically, potentiodynamic studies revealed superior exchange current density (− 3.17 mA cm−2), Tafel slope (80.1 mV dec−1), and limiting diffusion current density (− 1.49 mA cm−2) under light state than the dark state. Also, these results are certainly applicable for superior antibacterial activity against E. coli and L. monocytogenes about 90% and 75% under visible light, respectively.