According to the latest report released by the World Health Organization, bacterial resistance to well-known and widely available antibacterial drugs has become a significant and severe global health ...concern and a grim challenge to tackle in order to cure infections associated with multidrug-resistant pathogenic microorganisms efficiently. Consequently, various strategies have been orchestrated to cure the severe complications related to multidrug-resistant bacteria effectively. Some approaches involved the retardation of biofilm formation and multidrug-resistance pumps in bacteria as well as the discovery of new antimicrobial agents demonstrating different mechanisms of action. In this regard, natural products namely alkaloids, terpenoids, steroids, anthraquinone, flavonoids, saponins, tannins, etc., have been suggested to tackle the multidrug-resistant bacterial strains owing to their versatile pharmacological effects. Amongst these, flavonoids, also known as polyphenolic compounds, have been widely evaluated for their antibacterial property due to their tendency to retard the growth of a wide range of pathogenic microorganisms, including multidrug-resistant bacteria. The hydroxylation of C5, C7, C3', and C4'; and geranylation or prenylation at C6 have been extensively studied to increase bacterial inhibition of flavonoids. On the other hand, methoxylation at C3' and C5 has been reported to decrease flavonoids' antibacterial action. Hence, the latest information on the antibacterial activity of flavonoids is summarized in this review, with particular attention to the structure-activity relationship of this broad class of natural compounds to discover safe and potent antibacterial agents as natural products.
A number of research were conducted on the pyran and thiophene derivatives, which were attributed to have a wide range of biological activities, including anti-plasmodial, as well as acting as ...caspase, hepatitis C and cancer inhibitors.
The multicomponent reactions of the 5-acetyl-2-amino-4-(phenylamino)-thiophene-3-carbonitrile produced biologically active target molecules like pyran and their fused derivatives. Comparison between regular catalytic multi-component reactions and solvent-free ionic liquids immobilized multicomponent was studied.
The multicomponent reactions in this work were carried out not only under the reflux conditions using triethylamine as a catalyst but also in solvent-free ionic liquids immobilized magnetic nanoparticles (MNPs) catalysts.
Through this work, thirty-one new compounds were synthesized and characterized and were evaluated toward the six cancer cell lines, namely A549, HT-29, MKN-45, U87MG, and SMMC-7721 and H460. The most active compounds were further screened toward seventeen cancer cell lines classified according to the disease. In addition, the effect of compound 11e on the A549 cell line was selected to make further morphological changes in the cell line. The Molecular docking studies of 11e and 11f were carried and promising results were obtained.
The synthesis of heterocyclic compounds derived from thiophene derivatives has been receiving significant attention. After a detailed optimizing study, it has been found that the solvent-free ionic liquids immobilized multi-component syntheses afforded a high yield of compounds, opening a greener procedure for this synthetically relevant transformation. Many of the synthesized compounds can be considered anticancer agents, enhancing further studies.
The chalcone compound DHPO was synthesized through a chemical reaction between 1-(2-hydroxyphenyl)-ethanone and 3,4-dimethoxy benzaldehyde under ultrasound irradiation. The interaction between the ...DHPO compound and several metal ions was studied using fluorescence behavior, revealing that the chalcone function as a “turn on and turn off” switch fluorescent sensor, for selectively and sensitively detecting Fe
3+
ions. The process of fluorescence quenching and complexation of DHPO with Fe
3+
ion was further studied using methods such as Benesi-Hildebrand, Stern-Volmer plot, and job plot.
Neuronal models are an important tool in neuroscientific research. Hydrogen peroxide (H2O2), a major risk factor of neuronal oxidative stress, initiates a cascade of neuronal cell death. Polygonum ...minus Huds, known as ‘kesum’, is widely used in traditional medicine. P. minus has been reported to exhibit a few medicinal and pharmacological properties. The current study aimed to investigate the neuroprotective effects of P. minus ethanolic extract (PMEE) on H2O2-induced neurotoxicity in SH-SY5Y cells. LC–MS/MS revealed the presence of 28 metabolites in PMEE. Our study showed that the PMEE provided neuroprotection against H2O2-induced oxidative stress by activating the Nrf2/ARE, NF-κB/IκB and MAPK signaling pathways in PMEE pre-treated differentiated SH-SY5Y cells. Meanwhile, the acetylcholine (ACH) level was increased in the oxidative stress-induced treatment group after 4 h of exposure with H2O2. Molecular docking results with acetylcholinesterase (AChE) depicted that quercitrin showed the highest docking score at −9.5 kcal/mol followed by aloe-emodin, afzelin, and citreorosein at −9.4, −9.3 and −9.0 kcal/mol, respectively, compared to the other PMEE’s identified compounds, which show lower docking scores. The results indicate that PMEE has neuroprotective effects on SH-SY5Y neuroblastoma cells in vitro. In conclusion, PMEE may aid in reducing oxidative stress as a preventative therapy for neurodegenerative diseases.
Herein, we report a strategy to synthesize zinc oxide nanoparticles (ZnO NPs) from
Clitoria ternatea
flower extract through green synthesis platform. The bioactive components in the
C. ternatea
...flower extract acts as a stabilizing and capping agent, which enables the synthesis of ZnO NPs without the use of chemical reagents. Synthesis of of ZnO NPs through green platform was confirmed by analytical characterization techniques such as UV–Vis spectrophotometry, XRD, FTIR, DLS, Zeta potential, TEM, and EDX methods. The surface morphology and average size of ZnO NPs investigated through TEM and DLS results indicates rod shaped structure with average particle size of 84 nm. Green synthesized ZnO NPs shows excellent antibacterial, antibiofilm, and antioxidant activity which is dose-dependent. These ZnO NPs have cytotoxicity against breast cancer cells (MCF-7). The MTT test revealed a concentration-dependent inhibitory effect on MCF-7 cells, with IC
50
being 12.1 g/ml, and their anticancer potential was detected utilizing live and dead cell assays LDH release, Ao/EtBr), DAPI, ROS, and caspase-3 activation assays. Finally, the findings of these results shows that ZnO NPs derived from
C. ternatea
flower extract are highly potential candidates to treat bacterial infection and human breast cancer.
Recent studies have highlighted the necessity to thoroughly evaluate medicinal plants due to their therapeutic potential. The current study delves into the phytochemical profile, antioxidant ...capacity, and hepatoprotective effect of Andrographis paniculata. The investigation specifically targets its effectiveness in mitigating liver dysfunction induced by carbon tetrachloride (CCl4) in Wistar albino rats, aiming to uncover its promising role as a natural remedy for liver-related ailments. A. paniculata leaf extract was screened for phytoconstituents and antioxidant and hepatoprotective effects in Wistar albino rats against CCl4-induced liver dysfunction. Phytochemical analysis revealed the presence of flavonoids, alkaloids, and phenolic compounds in all extracts. The phenolic concentration ranged from 10.23 to 19.52 mg gallic acid per gram of the sample, while the highest flavonoid concentration was found in the ethanol fraction (8.27 mg rutin equivalents per gram). The antioxidant activity varied from 10.23 to 62.23. GC-MS analysis identified several phytochemicals including octadecanoic acid, stigmasterol, phenanthrenecarboxylic acid, and others. Effects of the ethanol extract of A. paniculata were evaluated in four groups of animals. Biochemical estimations of serum glutamine oxaloacetate transaminase, serum glutamine pyruvate transaminase, and serum bilirubin were significantly higher (p < 0.05) in the CCl4-treated group. Treatment with 300 mg/kg b.w. of the ethanol extract of A. paniculata significantly (p < 0.05) decreased these serum enzymes. Lipid peroxidation levels in carbon tetrachloride-treated animals showed a substantial (p < 0.05) rise when compared to untreated animals, while the lipid peroxidation levels were considerably (p < 0.05) reduced after treatment with ethanol extract at 300 mg/kg b.w. Liver biochemical catalase activities were significantly reduced in the carbon tetrachloride-treated animals. The results of this study conclusively demonstrate that A. paniculata extracts are a rich source of phytochemicals and possess significant antioxidant, free radical scavenging, and hepatoprotective properties.
Cu-Cu2O combination showed synergic effects in catalyzing intramolecular Ullmann coupling reaction for halo-Betti bases to afford fused benzo-xanthenes from both electron-rich and electron-deficient ...aromatic systems in good yield under mild reaction conditions. The sterically hindered halo-Betti bases also provided products in excellent yield. Under optimized condition, a gram scale reaction was also performed to afford the product in excellent yield. However, without ortho-halo substituted Betti-bases failed to afford fused benzo-xanthene derivatives. Exploring the reaction optimization without Cu metal, serendipitously it was produced 1,3-oxazine derivatives in excellent yield via intramolecular cross-dehydrogenative coupling (CDC) reaction. Similarly, electron-rich, electron-deficient and sterically hindered Betti-bases provided the products in good to excellent yield under mild condition.
Quinoline derivatives have been reported to possess multi-therapeutic potential owing to the manifestations of different pharmacological effects. The current research work describes about the design ...and synthesis of a series of novel benzoquinoline analogues with an objective to evaluate their antiproliferative structure–activity relationship against colon, breast and hepatocellular cancers. Upon synthesis, all derivatives’ chemical structures were elucidated through FTIR, 1HNMR and 13CNMR spectroscopic analysis. All derivatives were investigated for their in vitro anti-proliferative property against three different cancer cell lines (viz., colon carcinoma HT29, Caucasian breast adenocarcinoma MCF7, hepatocellular carcinoma HepG2) and a normal non-transformed human foreskin fibroblast Hs27 cell line. All derivatives demonstrated varied degrees of strong anticancer effect against all of the cell lines with the 2-Amino-4-(4-nitrophenyl)-5,6-dihydrobenzohquinoline-3-carbonitrile (CNMP, 2) exhibited the most potent antiproliferative effect viz. LC50 21.23 μM for breast, 8.24 μM for colon, and 26.15 μM for the hepatocellular, respectively. Molecular docking studies against all the the target crystal structures of cancer proteins (1HK7, 3EQM, 3IG7 and 4FM9) revealed significant binding affinities via hydrophobic and H-bonding interactions with all the compounds in conformity with the wet lab results. CNMP showed the highest binding energy of −7.55 in the HT29, −6.9 (both in MCF7 HepG2) kcal/mol. Based on the results obtained from wet lab and dry lab experiments, it can be proposed that CNMP might prove to be a potential lead structure for the design and synthesis of more potent anticancer candidates.
Phaleria macrocarpa fruit has been reported to be effectively used in Malaysia and neighboring countries to prevent obesity. Despite its anti-obesity potential, no research has ever predicted the ...compound-lipase, compound-HMG-CoA reductase interactions and in vivo investigations to further confirm its anti-obesity properties. Thus, the purpose of this study was to assess the anti-obesity and antihyperlipidemic effects of P. macrocarpa by in vitro, computational (in silico), and in vivo assays.
Initially, fruit was extracted through liquid CO2 and heating under reflux extraction methods to obtain liquid CO2 extracts (LCE-1 and LCE-2) and heating under reflux extract (HRE), respectively. Subsequently, all three extracts were assessed for antioxidant potentials through in vitro bioassays and FTIR analysis to identify different types of functional groups present in the existing bioactive compounds. Successively, the most active fraction (LCE-2) was subjected to GCMS analysis for the identification of lipid lowering and lipase inhibitors through molecular docking approach. Finally, anti-obesity and lipid lowering effects were further confirmed through an in vivo assay using mice.
LCE-2 exhibited higher DPPH (IC50 = 0.172 mg/mL) and FRAP (78.98 AAEmg/g) antioxidant activities and showed more potent peaks in FTIR chromatograms than LCE-1 and HRE. Among the identified tentative bioactive compounds viz. methyl palmitate, palmitic acid, ethyl palmitate, methyl oleate, oleic acid, cis-vaccenic acid, 3-deoxyestradiol and phenol, 2,2′-methylenebis6-(1,1-dimethylethyl)-4-methyl- were found as an anti-obesity and lipid lowering compounds whose protein–ligand interaction was confirmed by binding affinity, amino acid residues and bonding interactions. Similarly, anti-obesity and lipid lowering findings were also found in a mice model after 6 weeks treatment at a dose of 250 mg/kg b.w.
Based on the aforementioned in vitro, in silico and in vivo findings, it is concluded that the LCE-2 possesses lipase and HMG-CoA reductase inhibitors that can assist to develop this plant’s extract as an alternative safe lipid lowering herbal medicine in future.
A series of some novel sulphur and nitrogen containing ferrocenyl linked heterocyclic compounds were synthesized by multistep reactions and evaluated for in vitro antimicrobial activity against 15 ...ATCC strains out of which 8 were bacterial (Pseudomonas aeruginosa, Streptococcus bovis, Enterococcus faecalis, Klebsiella pneumoniae, Escherichia coli, Enterobacter cloacae, Methicillin-resistant Staphylococcus aureus and Streptococcus mutans) and 7 were fungal (Candida albicans, Candida dubliniensis, Candida glabrata, Candida parapsilosis, Candida tropicalis, Candida kefyr and Candida krusei) strains. The results clearly depict that the compounds (1–12) gave an average antimicrobial activity against the tested strains with an exception of compound 12 which stood out in terms of its activity against the tested organisms. All these compounds gave a range of MIC value between 32–64μg/ml against S. bovis, E. coli and C. tropicalis except compound 12 which gave a MIC of 16μg/ml against each of them. The MIC values of all these compounds against biofilm forming P. aeruginosa and S. mutans were 64–256μg/ml and 64–128μg/ml respectively which is apparently high, concluding that these compounds hold immense potential to be employed as a two in one formulation of antibacterial as well as antifungal agents.
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