The aim of the present study was to determine the antimicrobial and cytotoxic activities of eight novel titanium(III) based coordination complexes Ti(Pht)2(DL-serine)2, S1, Ti(Pht)2(glycine)2, S2), ...Ti(Pht)2(cystine)2, S3, Ti(Pht)2(DL-leucine)2, S4, Ti(Suc)2(L-leucine)2, S5, Ti(Suc)2(cystine)2, S6, Ti(Suc)2(cystein)2, S7 and Ti(Suc)2(DL-serine)2, S8 against several gram-positive and -negative bacteria, fungi and brine shrimp nauplii. The investigation showed that almost all of the complexes were moderately active against tested bacteria and fungi at high concentration (200 μg/disc) compared with the standard antibiotic, amoxicillin and the antifungal agent, nystatin. In vivo lethality bioassay experiment showed that only S7 and S8 among the complexes had better cytotoxic effect than standard gallic acid. The LC50 values of these two complexes were found to be 1.00 and 1.21 μg/ml, respectively. Thus the results suggest that only two complexes (S7, S8) among the titanium(III) based coordination complexes show the anticancer properties comparable to the standard cytotoxic agent, and further studies of these two complexes may be helpful for their clinical implication.
Active compounds of Swietenia mahagoni seed have power as anti diabetic that can be used in diabetes mellitus treatment. S. mahagoni seeds were extracted using methanol-maceration, followed by ...partitioning with petroleum ether (PE), chloroform (CL), ethyl acetate (EA), and dia-ion resin (DR). Column chromatography was used to further separate the dia-ion Resin fraction in order to get isolate purer compounds. One of the strategies is maintaining postprandial glucose level through inhibition of α-amylase and α-glucosidase. So that pre-prandial and post-prandial glucose levels can be controlled properly. The aim of this study was to determine in vitro inhibitory activity of Swietenia mahagoni seed by α-glucosidase, α-amylase. Inhibitory activity was measured using spectrophotometric method, α-amylase activity was measured at λ = 540 nm, α-glucosidase activity measured at λ = 405 nm. DRF inhibit both α-glucosidase and α-amylase better than acarbose as a positive control. This study showed that some extracts and some isolated compounds have inhibition activity of α-glucosidase and α-amylase. According to the findings, DR fraction (IC-50 = 328.22μg/mL) had a higher level of alpha-glucosidase inhibitory activity than acarbose (IC-50 = 336.95μg/mL). The six DR fractions compounds were separated using column chromatography. The DR fraction (40.62%), (50.39%), showed the highest inhibition activity.
•Phaleria macrocarpa is widely used as a remedy to reduce blood glucose levels.•GC–MS is a distinctive method dominating the metabolomics research area.•Chemometric analysis can be applied to resolve ...large data sets.
Phaleria macrocarpa is a medicinal plant widely available in Malaysia. The plant parts have been traditionally used as an antidiabetic remedy. This study aimed to identify the putative inhibitors of the α-glucosidase enzyme from P. macrocarpa using a gas chromatography-mass spectrometry (GC–MS)-based metabolomics approach and further subjected them to in silico molecular docking analysis to elucidate the possible mechanism of action. This study assessed the inhibitory potential of P. macrocarpa fruit extracts (aqueous, 20 %, 40 %, 60 %, 80 %, and 100 % ethanol) against the α-glucosidase enzyme using GC–MS and chemometric analysis. Orthogonal partial least squares (OPLS) combined with GC–MS analysis were applied to correlate the inhibition of enzyme activity to the metabolites profile of P. macrocarpa. All the potential inhibitors identified were further docked to the yeast (Saccharomyces cerevisiae) protein crystal structure (PDB3A4A). The generated score scatter plot of OPLS showed a recognizable separation of all the extracts into six different clusters. GC–MS, incorporated with multivariate data analysis techniques, was used to identify significant chemical markers. Methyl α-d-glucopyranoside, squalene, palmitic acid, myo-inositol and isoquinoline metabolites were identified as putative inhibitors against α-glucosidase activity from P. macrocarpa. In conclusion, the GC–MS-based metabolomics approach identified potential chemical markers of P. macrocarpa that could be utilized in the development of herbal based medicine.
Phaleria macrocarpa, known as “Mahkota Dewa”, is a widely used medicinal plant in Malaysia. This study focused on the characterization of α-glucosidase inhibitory activity of P. macrocarpa extracts ...using Fourier transform infrared spectroscopy (FTIR)-based metabolomics. P. macrocarpa and its extracts contain thousands of compounds having synergistic effect. Generally, their variability exists, and there are many active components in meager amounts. Thus, the conventional measurement methods of a single component for the quality control are time consuming, laborious, expensive, and unreliable. It is of great interest to develop a rapid prediction method for herbal quality control to investigate the α-glucosidase inhibitory activity of P. macrocarpa by multicomponent analyses. In this study, a rapid and simple analytical method was developed using FTIR spectroscopy-based fingerprinting. A total of 36 extracts of different ethanol concentrations were prepared and tested on inhibitory potential and fingerprinted using FTIR spectroscopy, coupled with chemometrics of orthogonal partial least square (OPLS) at the 4000–400 cm−1 frequency region and resolution of 4 cm−1. The OPLS model generated the highest regression coefficient with R2Y = 0.98 and Q2Y = 0.70, lowest root mean square error estimation = 17.17, and root mean square error of cross validation = 57.29. A five-component (1+4+0) predictive model was build up to correlate FTIR spectra with activity, and the responsible functional groups, such as –CH, –NH, –COOH, and –OH, were identified for the bioactivity. A successful multivariate model was constructed using FTIR-attenuated total reflection as a simple and rapid technique to predict the inhibitory activity.
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•In this study, a rapid and simple analytical method was developed using a Fourier transform infrared (FTIR) spectroscopy-based fingerprinting.•A five-component (1+4+0) predictive model was build up to correlate FTIR spectra with activity, and the responsible functional groups such as CH, NH, COOH, and OH were identified for the bioactivity.•A successful multivariate model was constructed using FTIR-ATR to predict the inhibitory activity.
The aim of the present study was to assess the cytotoxic and antimicrobial properties of seven new thiocyanato complexes: Ni(C9H11N2O)(SCN), Cu(C9H11N2O)(SCN), Pd(C9H11N2O)(SCN), Pt(C9H11N2O) (SCN), ...KTi(C9H11N2O)(SCN)3, Au(C9H11N2O)(SCN), and KV(O)(C9H11N2O)(SCN) (T1‐T7, respectively). All the complexes showed toxicity against brine shrimp nauplii (Artemia salina L.). The titanium‐based complex, T5, exhibited potent toxicity, with a lethal concentration 50% (the concentration of test compound that kills 50% of A. salina) value of 1.59 μg mL−1. These new complexes also exhibited promising antibacterial and antifungal properties. A macrodilution technique was used to estimate the minimum inhibitory concentrations of the seven bioactive complexes. Minimum inhibitory concentrations were found to be 8–64 μg mL−1 against the tested bacterial species.
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