Synthesis, molecular modelling studies of artemisinin-chalcone derivatives and their antimalarial activity evaluation.

Twenty-two monomers and dimers of artemisinin having chalcone as a linker were synthesised, and their antimalarial activity against was determined, and a quantitative structure-activity relationship (QSAR) was developed. Artemisinin is a frontline antimalarial drug known worldwide but is threatened because of the rapidly emerging artemisinin-resistant strain , antimalarial IC (half-maximal inhibitory concentration) activity of a molecule against malaria parasites provides a good first screen for identifying the antimalarial potential of a particular molecule. The most active compound was artemisinin dimer dimethoxy chalcone as a linker with IC of 4.

Cu-catalyzed click reaction in synthesis of eugenol derivatives as potent antimalarial agents.

Eugenol(), a terpenoid found in Ocimum, has various biological activities. The present study aims at extraction, isolation of the plant secondary metabolite eugenol (), it's derivatisation and structure identification as bioactive molecules. Synthesis and antiplasmodial activity ( and ), of a series of fourteen novel eugenol-based 1,2,3-triazole derivatives was done in the present study.

Synergistic Antibacterial Activity of Gallic Acid Based Chalcone Indl 2 by Inhibiting Efflux Pump Transporters.

As a part of novel discovery of drugs from natural resources, present study was undertaken to explore the antibacterial potential of chalcone Indl-2 in combination with different group of antibiotics. MIC of antibiotics was reduced up to eight folds against the different cultures of E. coli by both chalcones.

Effect of liquiritigenin on chloroquine accumulation in digestive vacuole leading to apoptosis-like death of chloroquine-resistant P. falciparum.

Background: Malaria remains one of the major health concerns, especially in tropical countries. Although drugs such as artemisinin-based combinations are efficient for treating Plasmodium falciparum, the growing threat from multi-drug resistance has become a major challenge. Thus, there is a constant need to identify and validate new combinations to sustain current disease control strategies to overcome the challenge of drug resistance in the malaria parasites.

Assessment of Genetic Diversity, Micromorphology and Antimicrobial Activity in Nepeta cataria L.

The mosquito repellent Nepetalactone rich Nepeta cataria L. (catmint) plant has a variety of therapeutic and industrial potential. Reports on the genetic diversity of N.

Investigation of the potential of as a bioavailability enhancer of Vitamin B12.

Vitamin B12 deficiency is prevalent among individuals globally. Inadequate consumption of B12 rich diet and low bioavailability (due to diet based/physiological factors) are linked to the deficiency of Vitamin B12 inside the body. Bioavailability enhancers augment the bioavailability of an ingested substance (drug/nutrient) thus increasing their concentration inside the body and maximizing their therapeutic benefits.

Quebrachitol from Putranjiva roxburghii Wall. (Putranjivaceae) a potent antimalarial: Pre-clinical efficacy and its interaction with PfLDH.

Researchers are exploring natural resources in search of a new and effective anti-malarial compound to address the challenges in malarial treatment due to emerging incidences of drug-resistant strains. Following background knowledge of traditional medicine, we evaluated the in-vitro and in-vivo anti-malarial efficacy of Putranjiva P. roxburghii (Putranjivaceae) twigs ethanol extracts and fraction (PRT).

Cliv-92-Loaded Glycyrrhetinic Acid-Modified Chitosan Nanoparticles for Enhanced Hepatoprotection-Preparation, Characterization, and In Vivo Evaluation.

Cliv-92 is a mixture of three structurally similar coumarinolignoids and a proven hepatoprotective agent. Low aqueous solubility and poor bioavailability are notable hindrances for its further use. Therefore, glycyrrhetinic acid-linked chitosan nanoparticles loaded with Cliv-92 were prepared for active targeting to the liver.

Glabridin synergy with norfloxacin induces ROS in multidrug resistant Staphylococcus aureus.

Glabridin (Glb), a polyphenolic flavonoid inhibits the growth of MDRSA (Multidrug resistant S. aureus) 4627 by inducing ROS. Glb in combination with Norfloxacin (Nor) synergistically induced oxidative stress.

Inhibition of heme detoxification pathway in malaria parasite by 3-hydroxy-11-keto-β-boswellic acid isolated from Boswellia serrata.

Malaria eradication is still a major global health problem in developing countries, which has been of more concern ever since the malaria parasite has developed resistance against frontline antimalarial drugs. Historical evidence proves that the plants possess a major resource for the development of novel anti-malarial drugs. In the present study, the bioactivity guided fractionation of the oleogum-resin of Boswellia serrata Roxb.

Drug resistance reversal potential of multifunctional thieno[3,2-c]pyran via potentiation of antibiotics in MDR P. aeruginosa.

We explored the antibacterial potential (alone and combination) against multidrug resistant (MDR) Pseudomonas aeruginosa isolates KG-P2 using synthesized thieno[3,2-c]pyran-2-ones in combination with different antibiotics. Out of 14 compounds, two compounds (3g and 3l) abridged the MIC of tetracycline (TET) by 16 folds. Compounds was killing the KG-P2 cells, in time dependent manner, lengthened post-antibiotic effect (PAE) of TET and found decreased the mutant prevention concentration (MPC) of TET.

The Bioactive Potential of Culturable Fungal Endophytes Isolated From the Leaf of Catharanthus roseus (L.) G. Don.

Introduction: Endophyte is considered a source of natural bioactive secondary metabolites that provides an array of bioactive lead compounds. The present study was aimed to determine the antimicrobial and anti-inflammatory potential of fungal endophytes isolated from Catharanthus roseus.

Methods: A total of seven fungal endophytes crude extract were screened against bacterial pathogens.

4-Chlorothymol Exerts Antiplasmodial Activity Impeding Redox Defense System in .

Malaria remains one of the major health concerns due to the resistance of species toward the existing drugs warranting an urgent need for new antimalarials. Thymol derivatives were known to exhibit enhanced antimicrobial activities; however, no reports were found against spp. In the present study, the antiplasmodial activity of thymol derivatives was evaluated against chloroquine-sensitive (NF-54) and -resistant (K1) strains of .

4-chloro eugenol interacts synergistically with artesunate against drug resistant P. falciparum inducing oxidative stress.

4-chloro eugenol (4CE), a semisynthetic analog of phytomolecule eugenol exhibited potent antiplasmodial activity with IC in the range of 1.5-5 μM against sensitive as well as drug resistant strain of P. falciparum.

Detection of Natural Inhibitors against Human Liver Cancer Cell Lines through QSAR, Molecular Docking and ADMET Studies.

Background: Liver cancer is ranked as the fifth most prevalent and third most lethal cancer worldwide. The incidence rates of this cancer are on the rise, and only limited treatment options are available.

Methods: To identify and optimize the inhibitors of liver cancer cell-lines, a QSAR model was developed by using multiple linear regression methods.

Design, synthesis and drug resistance reversal potential of novel curcumin mimics Van D: Synergy potential of curcumin mimics.

Being crucial part of plant-based novel discovery of drug from natural resources, a study was done to explore the antibacterial potential of curcumin mimics in combination with antibiotics against multidrug resistant isolates of Pseudomonas aeruginosa. The best candidate Van D, a curcumin mimics reduced the MIC of tetracycline (TET) up to 16 folds against multidrug resistant clinical isolates. VanD further inhibited the efflux pumps as evident by ethidium bromide efflux and by in-silico docking studies.

Glabridin Averts Biofilms Formation in Methicillin-Resistant by Modulation of the Surfaceome.

is an opportunistic bacterium of the human body and a leading cause of nosocomial infections. Methicillin resistant (MRSA) infections involving biofilm lead to higher mortality and morbidity in patients. Biofilm causes serious clinical issues, as it mitigates entry of antimicrobials to reach the etiological agents.

Synthesis, molecular modelling studies of indolyl chalcone derivatives and their antimalarial activity evaluation.

Twenty one chalcone derivatives were synthesized using Claisen-Schmidt condensation, their antimalarial activity against was determined and quantitative structure-activity relationship (QSAR) was developed. Condensation of substituted acetophenones with various aromatic aldehydes at room temperature gave chalcones in 75-96% yield. Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities.

Molecular investigation against the resistant mechanism of PncA mutated pyrazinamide resistance and insight into the role of pH environment for pyrazinamide activation.

Pyrazinamide (PZA), a crucial component of anti-TB therapy, is a prodrug. PZA interacts with PncA protein to be converted into its functional form i.e.

Novel bioactive compound from the bark of Wall.

Wall, family - Putranjivaceae) is an Indian native medicinal plant used to treat many diseases such as treatment of mouth and stomach ulcers, hot swellings, smallpox, burning sensation and ophthalmopathy. The study of chemical constituents in the bark of resulted in a new triterpene () along with five known triterpenoids (-). The chemical characterisation was based on H, C, 2D-NMR experimentation, and ESI-MS data.

Usnic acid modifies MRSA drug resistance through down-regulation of proteins involved in peptidoglycan and fatty acid biosynthesis.

Multidrug-resistant Staphylococcus aureus infections place a huge burden on the healthcare sector and the wider community. An increasing rate of infections caused by methicillin-resistant Staphylococcus aureus (MRSA) has necessitated the development of alternative agents. We previously reported that usnic acid (UA) has activity against MRSA; here, we report the effect of UA in combination with norfloxacin on the drug resistance of MRSA clinical isolates.

Comparative Drug Resistance Reversal Potential of Natural Glycosides: Potential of Synergy Niaziridin & Niazirin.

Background: Due to the limited availability of antibiotics, Gram-negative bacteria (GNB) acquire different levels of drug resistance. It raised an urgent need to identify such agents, which can reverse the phenomenon of drug resistance.

Objective: To understand the mechanism of drug resistance reversal of glycosides; niaziridin and niazirin isolated from the pods of Moringa oleifera and ouabain (control) against the clinical isolates of multidrug-resistant Escherichia coli.

Silymarin, a polyphenolic flavonoid impede growth through interaction with heme.

A polyphenolic flavonoid, Silymarin isolated from is widely known for its hepatoprotective action. In the present study anti-plasmodial activity of Silymarin has been demonstrated for the first time having IC of 14 ± 0.33 μM against the NF-54 strain of with high selectivity index (>100).

AromaDb: A Database of Medicinal and Aromatic Plant's Aroma Molecules With Phytochemistry and Therapeutic Potentials.

In traditional, herbal medicine, and aromatherapy, use of essential oils and their aroma compounds have been known since long, for the management of various human diseases. The essential oil is a mixture of highly complex, naturally occurring volatile aroma compounds synthesized by medicinal and aromatic plants as secondary metabolites. Essential oils widely used in pharmaceutical, cosmetic, sanitary, food industry and agriculture for their antibacterial, antiviral, antifungal, antiparasitic, insecticidal, anticancer, neuroprotective, psychophysiological, and anti-aging activities.