Identification of new modulator of DNA repairing pathways based on natural product (±)-peharmaline A.

The complex heterogenic environment of tumour mass often leads to drug resistance and facilitate chemo insensitivity triggering more malignant phenotypes among cancer patients. Major DNA-damaging cancer drugs have been consistently proven unsuccessful in terms of elevating chemo-resistance. (±)-peharmaline A, a hybrid natural product isolated from seeds of Peganum harmala L.

Identification of Lipoxygenase gene repertoire of Cannabis sativa and functional characterization of CsLOX13 gene.

Lipoxygenase (LOX) enzymes play a pivotal role in the biosynthesis of oxylipins. The phyto-oxilipins have been implicated in diverse aspects of plant biology, from regulating plant growth and development to providing tolerance against biotic and abiotic stresses. C.

BF-EtO Promoted Heteronucleophilic Addition Reactions for the Synthesis of Unsymmetrical -Diarylmethyl Thioethers.

Herein, we present the BF/BF mediated activation of diphenyl phosphite for the formation of thionium ions from aldehydes and thiophenols. These reactive species subsequently undergo reaction with generated phenol, resulting in the synthesis of diarylmethyl thioethers. It was demonstrated that the addition of external phenol in the reaction produced unsymmetrical -diarylmethyl thioethers in good yields.

HPLC-PDA Method for Quantification of Bioactive Compounds in Crude Extract and Fractions of Falc. and Cytotoxicity Studies against Cancer Cells.

Falc. (Synonym: Saussurea costus (Falc.) Lipsch.

Medicinal plants traditionally used in the health care practices by the indigenous communities of the Trans-Himalayan region of Ladakh, India.

Ethnopharmacological Relevance: Ladakh, "the land of high-rising passes," is a cold arid desert located in the India's northernmost part of the Trans-Himalayan region. Traditional knowledge of medicinal plants in this fragile ecosystem is an important part of the primary healthcare system, particularly in remote areas where modern medical facilities are not fully operational. There is a need to update the traditional information on medicinal plants from time to time to understand any addition of plants or uses to assist in developing new drugs through pharmacological and phytochemical studies.

Ellagic Acid Exerts Dual Action to Curb the Pathophysiological Manifestations of Sickle Cell Disease and Attenuate the Hydroxyurea-Induced Myelosuppression in Berkeley Mice.

The use of adjuvant therapy is an attractive approach to manage sickle cell disease (SCD) symptomatically. The present study aimed to investigate the potential of ellagic acid as an adjuvant therapy with hydroxyurea (HU), a key drug for SCD with myelosuppressive toxic effects. A panel of experiments was performed using SCD patient's blood (ex vivo) and transgenic mice model of SCD (in vivo).

Total Synthesis and Absolute Configuration Determination of the α-Glycosidase Inhibitor (3,4)-6-Acetyl-3-hydroxy-2,2-dimethylchroman-4-yl ()-2-Methylbut-2-enoate from .

Herein, we report the first total synthesis of α-glycosidase inhibitor (3, 4)-6-acetyl-3-hydroxy-2,2-dimethylchroman-4-yl ()-2-methylbut-2-enoate as well as its enantiomer. Our synthesis confirms the chromane structure separately proposed by Navarro-Vazquez and Mata, on the basis of DFT computations. Furthermore, our synthesis allowed us to determine the absolute configuration of the natural compound as (3, 4) and not (3, 4).

Recent bioanalytical methods for the isolation of bioactive natural products from genus Codonopsis.

Introduction: Chromatography and spectroscopy are nowadays well-validated techniques allowing to isolate and purify different class of natural products from the genus Codonopsis. Several categories of phytochemicals with drug like properties have been selectively extracted, isolated, characterised by this methodology.

Objectives: The present review aims to provide up-to-date and comprehensive information on the chromatography, phytochemistry and pharmacology of natural products of Codonopsis with an emphasis on the search for natural products having various biological activities and the semi-synthetic derivatives of bioactive ones and to highlight current gaps in knowledge.

Base-Mediated Transformation of Glycals to Their Corresponding Vinyl Iodides and Their Application in the Synthesis of C-3 Enofuranose and Bicyclic 3,4-Pyran-Fused Furanose.

A simple method for the iodination of unsaturated sugars to form sugar vinyl iodides was developed under oxidant-free conditions using NaH/DMF/iodine as a reagent system at ambient temperature. 2-Iodoglycals bearing ester, ether, silicon, and acetonide protection were synthesized in good to excellent yield. 3-Vinyl iodides derived from 1,2:5,6-diacetonide glucofuranose were transformed to C-3 enofuranose and bicyclic 3,4-pyran-fused furanose via Pd-catalyzed C-3 carbonylation and intramolecular Heck reaction, respectively, as the key step.

Gold nanoblackbodies-based multifunctional nanocomposite for multimodal cancer therapy.

Multifunctional nanocomposites are of potential use to achieve complete tumor elimination and, thus, to avoid tumor recurrence. Herein, polydopamine (PDA)-based gold nanoblackbodies (AuNBs) loaded with indocyanine green (ICG) and Doxorubicin (DOX) termed as A-P-I-D nanocomposite were investigated for multimodal plasmonic photothermal-photodynamic-chemotherapy. Upon near-infrared (NIR) irradiation, A-P-I-D nanocomposite showed enhanced photothermal conversion efficiency of 69.

Orally bioavailable styryl derivative of rohitukine-N-oxide inhibits CDK9/T1 and the growth of pancreatic cancer cells.

The chromone alkaloid is one of the classical pharmacophores for cyclin-dependent kinases (CDKs) and represents the first CDK inhibitor to reach clinical trials. Rohitukine (1), a chromone alkaloid isolated from Dysoxylum binectariferum inspired the discovery of several clinical candidates. The N-oxide derivative of rohitukine occurs naturally, with no reports on its biological activity.

Discovery of SDS-347 as a specific peptide competitive inhibitor of G9a with promising anti-cancer potential.

Background: G9a is a histone H3K9 methyltransferase enzyme found highly upregulated in many cancers. H3 binds to the rigid I-SET domain and the cofactor, S-adenosyl methionine, binds to the flexible post-SET domain of G9a. Inhibition of G9a is known to inhibit the growth of cancer cell-lines.

Utilization of xylose enriched extract from spent lemongrass hydrolysate for clavulanic acid production using Streptomyces clavuligerus (MTCC 1142).

The main goal of this study was to provide possible alternative production medium containing xylose enriched spent lemongrass hydrolysate with glycerol as a feedstock and corn gluten meal as a nitrogen source for their ability to support the cell growth of the Streptomyces clavuligerus MTCC 1142 for the production of clavulanic acid. The xylose was extracted from spent lemongrass by using 0.25% dilute nitric acid and further partial purification of acid spent hydrolysate was performed using ion exchange resin.

Microbial production of nutraceuticals: Metabolic engineering interventions in phenolic compounds, poly unsaturated fatty acids and carotenoids synthesis.

Nutraceuticals have attained substantial attention due to their health-boosting or disease-prevention characteristics. Growing awareness about the potential of nutraceuticals for the prevention and management of diseases affecting human has led to an increase in the market value of nutraceuticals in several billion dollars. Nevertheless, limitations in supply and isolation complications from plants, animals or fungi, limit the large-scale production of nutraceuticals.

A small animal model of NASH with progressive steatohepatitis -induced by fast food diet and alcohol in C57BL/6J mouse with high human pathophysiological proximity.

Non-alcoholic steatohepatitis (NASH) and alcoholic steatohepatitis (ASH) both can progress to end-stage liver disease (ESLD). No relevant animal models are available for studying the toxic consequences of concurrent fast food diet and alcohol usage in fibrosing NASH. As a result, dependable and short-term in-vivo models capable of recapitulating human disease pathophysiology are required for deciphering mechanistic insights and preclinical drug discovery programs.

Methoxy-naphthyl-Linked -Benzyl Pyridinium Styryls as Dual Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Structure-Activity Relationship.

The multifaceted nature of Alzheimer's disease (AD) indicates the need for multitargeted agents as potential therapeutics. Both cholinesterases (ChEs), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), play a vital role in disease progression. Thus, inhibiting both ChEs is more beneficial than only one for effectively managing AD.

Piperine analog PGP-41 treatment overcomes paclitaxel resistance in NCI/ADR-RES ovarian cells by inhibition of MDR1.

Chemoresistance is one of the leading causes of the failure of chemotherapy. Overexpression of P-glycoprotein (P-gp) in cancer cells is one of the most important contributing factors toward the development of chemoresistance. This study was designed to synthesize the derivatives of dihydronaphthyl and to evaluate the P-gp inhibition activity of these compounds.

GC-MS based untargeted metabolomics reveals the metabolic response of earthworm (Eudrilus eugeniae) after chronic combinatorial exposure to three different pesticides.

In this study GC-MS-based untargeted metabolomics was used to identify the metabolic response of earthworm; Eudrilus eugeniae exposed to sub-lethal concentrations of chlorpyrifos-CHL, cypermethrin-CYP, Glyphosate-GLY, and Combined-C (all three pesticides) at the concentrations of 3, 6, and 12 mg/kg. Principal component analysis of the obtained datasets revealed a clear distinction between the control and treatment groups. The mean weight of the worms in the treated groups decreased significantly (p < 0.

Lavender Plant: Farming and Health Benefits.

Natural remedies from a range of sources, including plants, animals, microorganisms, and marine life, have made a significant contribution to the treatment of many ailments. Lavender is a Mediterranean shrub from the Lamiaceae family. Lavender flowers (Lavandula flores) include active ingredients (3%), anthocyanins, sugars, phytosterols, minerals, and tannins and are majorly used for herbal applications.

Improving microbial and lipid oxidative stability of cheddar cheese using cricket protein hydrolysates pre-treated with microwave and ultrasonication.

The study was carried out to investigate cricket protein hydrolysates' (CPH) potential to enhance the storage stability of cheddar cheese. The cricket protein (CP) samples pre-processed with microwave (T), ultrasonication (T) or without pre-treatment (T) were used for developing the CPH using alcalase enzyme (3%). Freeze-dried CPH were incorporated in the cheese samples (CPH-T, CPH-T and CPH-T) at the maximum level of 1.

Antifibrotic Agent Mediated Tumor Microenvironment Modulation and Improved Nanomedicine Delivery in Solid Tumor.

The unique physiology of tumors limits the efficacy of chemotherapeutics. In efforts to improve the effectiveness of the existing chemotherapy drugs, nanomedicine emerged as a new hope but proved inadequate due to the transport barriers present within the tumor tissues, which limits the potential of nanomedicine. Dense collagen networks in fibrotic tissues contribute to hindering the penetration of molecular- or nano-scale medicine through tumor interstitium.

Flurbiprofen inhibits heme induced NLRP3 inflammasome in Berkeley sickle cell disease mice.

Sickle cell disease (SCD) is accompanied by several complications, which emanate from the sickling of erythrocytes due to a point mutation in the -globin chain of hemoglobin. Sickled erythrocytes are unable to move smoothly through small blood capillaries and therefore, cause vaso occlusion and severe pain. Apart from pain, continuous lysis of fragile sickled erythrocytes leads to the release of heme, which is a strong activator of the NLRP3 inflammasome, thus producing chronic inflammation in sickle cell disease.

Bacillinaphthin A: A New Naphthohydroquinone from the Endophyte Bacillus subtilis NPROOT3.

The present study explores the endophyte associated with the halophyte Salicornia brachiata for uncovering new biologically important compounds. Thus, HPLC-PDA guided chemical investigation of the ethyl acetate extract of the Bacillus subtilis NPROOT3 led to the isolation of a new compound named bacillinaphthin A (1) along with previously known rubinaphthin A (2). The structure of 2 was determined by a comparison of HR-ESI-MS, H and C nuclear magnetic resonances (NMR) with those of reported data, whereas the structure of new compound 1 was elucidated by interpretation of 1D- and 2D-NMR and MS data.