Novel α-mangostin derivatives as promising antiviral agents: Isolation, synthesis, and evaluation against chikungunya virus.

Investigations into fruit and vegetable processing residues (FVPRs) offer huge opportunities to discover novel therapeutics against many diseases. In this study, detailed investigation of Garcinia mangostana fruit peel extract led to the isolation and identification of ten known compounds (1-10). Further, a new series of α-mangostin derived sulphonyl piperzines, aryl alkynes and 1,2,3-triazole derivatives were synthesized using Huisgen 1,3-dipolar cyclo-addition reaction ("click" chemistry).

Synthesis of epoxyazadiradione-thiazole hybrid derivatives and evaluation of their cytotoxic activities.

In an attempt to develop natural product-based anticancer agents, a series of novel epoxyazadiradione-thiazole hybrids () were synthesised and evaluated for their anticancer activity. All the synthesised derivatives were assessed for cytotoxic activity against a panel of human cancer and normal cell lines and the results showed that most of the compounds exhibited significant cytotoxic activity against cancer cells and as well some of the compounds showed less cytotoxicity against normal cells. In particular, compound showed potent cytotoxic activity against tongue cancer cell lines.

Natural products: A potential immunomodulators against inflammatory-related diseases.

The incidence and prevalence of inflammatory-related diseases (IRDs) are increasing worldwide. Current approved treatments for IRDs in the clinic are combat against inhibiting the pro-inflammatory cytokines. Though significant development in the treatment in the IRDs has been achieved, the severe side effects and inefficiency of currently practicing treatments are endless challenge.

Brain tumor segmentation using neuro-technology enabled intelligence-cascaded U-Net model.

According to experts in neurology, brain tumours pose a serious risk to human health. The clinical identification and treatment of brain tumours rely heavily on accurate segmentation. The varied sizes, forms, and locations of brain tumours make accurate automated segmentation a formidable obstacle in the field of neuroscience.

Salazinic Acid and Norlobaridone from the Lichen : Antioxidant Activity, α-Glucosidase Inhibitory and Molecular Docking Studies.

The present study was intended for the identification of secondary metabolites in acetone extract of the lichen using UPLC-ESI-QToF-MS/MS and the detection of bioactive compounds. This study led to the identification of 22 metabolites based on their MS/MS spectra, accurate molecular masses, molecular formula from a comparison of the literature database (DNP), and fragmentation patterns. In addition, potent antioxidant and α-glucosidase inhibitory potentials of acetone extract of motivated us to isolate 10 metabolites, which were characterized as salazinic acid (), norlobaridone (), atranorin (), lecanoric acid (), lichesterinic acid (), protolichesterinic acid (), methyl hematommate (), iso-rhizonic acid (), atranol (), and methylatratate ( based on their spectral data.

An Imbalanced Generative Adversarial Network-Based Approach for Network Intrusion Detection in an Imbalanced Dataset.

In modern networks, a Network Intrusion Detection System (NIDS) is a critical security device for detecting unauthorized activity. The categorization effectiveness for minority classes is limited by the imbalanced class issues connected with the dataset. We propose an Imbalanced Generative Adversarial Network (IGAN) to address the problem of class imbalance by increasing the detection rate of minority classes while maintaining efficiency.

Piperazine tethered bergenin heterocyclic hybrids: design, synthesis, anticancer activity, and molecular docking studies.

In an attempt to develop natural product-based anticancer agents, a series of novel piperazine-linked bergenin heterocyclic hybrids bearing arylthiazolyl (5a-e), benzothiazolyl (10a-i), and arylsulfonyl (13a-o) were synthesized using the classical Mannich reaction and evaluated for their anticancer activity. All the synthesized derivatives were assessed for cytotoxic activity against a panel of human cancer and normal cell lines and the results showed that most of the compounds exhibited significant cytotoxic activity against cancer cells and mild cytotoxicity against normal cells. In particular, the compounds 5a, 5c, 10f, and 13o showed potent cytotoxic activity against tongue and oral cancer cell lines compared to the parent compound (<100 μM).

Synthesis of ring-A modified lupeol derivatives and their anti-proliferative activity: identification of potent lead active against MCF-7 breast cancer cells.

In continuation of our research program aimed at the development of new natural product-based anticancer agents, a series of lupeol derivatives (- and -) were prepared with the introduction of aryl functionalities and amino acids at C-3 position. All the synthesised derivatives were assessed for anticancer activity against four human cancer cell lines using MTT assay. Interestingly, the compounds , , and showed potent activity against MCF7 cells as compared with the parent compound.

Isolation, purification and structural elucidation of Mellein from endophytic fungus Lasiodiplodia theobromae strain (SJF-1) and its broad-spectrum antimicrobial and pharmacological properties.

In an on-going investigation of bioactive metabolites producing potential endophytic fungi, the strain Lasiodiplodia theobromae (SJF-1) was isolated from a medicinal plant Syzygium cumini. The cultural, morphological and molecular identification was done with the SJF-1 strain. The obtained gene sequence was deposited in NCBI with accession number MG 938644.

Chemical profiling of marine seaweed Halimeda gracilis using UPLC-ESI-Q-TOF-MS and evaluation of anticancer activity targeting PI3K/AKT and intrinsic apoptosis signaling pathway.

Marine seaweeds are predominant for nutraceuticals and have been food source since ancient times and are currently being used in Chinese medicines and Japanese traditional medicines. In the present study, the chemical profile analysis of Halimeda gracilis was performed using UPLC-ESI-Q-TOF-MS analysis and assessed for its anticancer activity. A cursory investigation of the total ion chromatograms of the both methanol (MHG) and ethyl acetate (EAHG) of H.

Design, synthesis and cytotoxic activity studies of alkyne linked analogues of Nimbolide.

A series of novel nimbolide derivatives bearing various substitutions on 28th position was designed and synthesized using Sonogashira (2a-2p) and Glaser coupling (3a-3e) reactions. The synthesized derivatives were assessed for in vitro cytotoxic activity against four different human cancer cell lines (A549 cells, MCF-7 cells, MDA-MB-231 cells, and HCT15 cells) and normal cell line (HEK cells) using MTT assay. Among the screened derivatives, the compound 3a showed potent activity against A549 cells with IC value of 0.

Isolation of a new steroid from phytochemical investigation on .

A new steroid (acylated C pregnane steroid) was isolated from chloroform extract in phytochemical screening of . The isolated compound is found to be 3β-hydroxy-14β-(6'- carboxyphenyl)propionyloxypregn-5-en-20-one based on spectroscopic studies (IR, H NMR, C NMR, DEPT, COSY, HSQC, HMBC and ESI-MS). The isolated new steroid was tested against four bacterial strains and the activity was related to the structure of the molecule.

Design, synthesis, cytotoxic, and anti-inflammatory activities of some novel analogues of aloe-emodin isolated from the rhizomes of .

In connection with our continuous efforts in the synthesis of derivatives from major compounds isolated from traditional medicinal plants, in the present study we have attempted to synthesize the furan-conjugated aloe-emodin derivatives () using a three-component reaction. The synthesized derivatives were assessed for anticancer activity against five different cancer cell lines using the MTT assay and the results showed that most of the derivatives are potent against cancer cells comparing with the control. Compounds and showed excellent activity against all the cancer cells with less than 12.

Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents.

In connection with our continuous efforts to generate new derivatives from lead compounds isolated from traditional medicinal plants, a series of aloe-emodin derivatives () were synthesized and assessed for their potential anticancer activity against a panel of cancer cell lines. The results showed that most of the derivatives are more active than the aloe-emodin and particularly, and manifested potent activity with IC values of 1.32 & 1.

Investigation of Cytotoxic Constituents from Seed Pulp of Entada Phaseoloides and Metabolite Profiling Using UPLC-QTOF-MSE.

Background: Entada phaseoloides (Linn.) Merr. (Family: Fabaceae) is a well-known, traditional, medicinal plant that has been extensively used in the Ayurvedic system of medicine for centuries to combat a wide range of ailments.

Investigation of Related Impurities in Metadoxine by a Reversed Phase High Performance Liquid Chromatography Technique.

A new reversed-phase high-performance liquid chromatography (RP-HPLC) method has been developed for the separation and identification of impurities present in metadoxine. Herein, we report that one of the impurities eluted from the metadoxine sample is 4-deoxypyridoxine hydrochloride (4-DPH). In HPLC analysis, the retention time (RT) of 4-DPH was observed to be at 13.

Synthesis and biological evaluation of Schizandrin derivatives as tubulin polymerization inhibitors.

A series of oxime ester-derivatives were prepared by utilizing the schizandrin (1), a major compound isolated from Schisandra grandiflora, which is deployed in different traditional system of medicine. The in vitro antiproliferative activities of the synthesized compounds were assessed against a selected panel of human cancer cell lines (A549, RKO P3, DU145 and Hela) and normal cell (HEK293). Several of these derivatives were found more potent in comparison to parent compound, schizandrin (1).

Bombax ceiba (Linn.) calyxes ameliorate methylglyoxal-induced oxidative stress via modulation of RAGE expression: identification of active phytometabolites by GC-MS analysis.

Non-enzymatic reactions between proteins and methylglyoxal (MG) result in the formation of advanced glycation end products (AGEs). These AGEs play a vital role in the development of diabetic complications by stimulating oxidative stress and acting upon their receptor RAGE (Receptor for Advanced Glycation End products). This study examined the effect of aqueous methanol extract of Bombax ceiba L.

Synthesis and biological evaluation of bergenin-1,2,3-triazole hybrids as novel class of anti-mitotic agents.

In continuation of our investigation of pharmacologically-motivated natural products, we have isolated bergenin (1) as a major compound from Mallotus philippensis, which is deployed in different Indian traditional systems of medicine. Here, a series of bergenin-1,2,3-triazole hybrids were synthesized and evaluated for their potentials against a panel of cancer cell lines. Several of the hybrid derivatives were found more potent in comparison to parent compound bergenin (1).

Isolation, semi-synthesis, free-radicals scavenging, and advanced glycation end products formation inhibitory constituents from .

Bioassay-guided separation of acetone extract from lichen (Delise ex Nyl.) Hale led to the isolation of six major phenolic constituents (). Compounds structures were established using NMR and mass spectral techniques.

Cerium Phosphate-Cerium Oxide Heterogeneous Composite Nanozymes with Enhanced Peroxidase-Like Biomimetic Activity for Glucose and Hydrogen Peroxide Sensing.

In the present work, we focus on the development of CePO-CeO composite nanorods with peroxidase mimetic activity for the sensitive detection of hydrogen peroxide and glucose. The Ce/PO molar ratio (CP10:1, CP5:1, CP2:1) in the hydrothermal reaction controlled the formation of pure CePO, CePO-CeO composite nanozymes with different percentages of CeO, and its crystal structure. A higher Ce/PO molar ratio (CP10:1 or CP5:1) was required to obtain CePO-CeO composite nanostructure, while a lower Ce/PO molar (CP2:1) ratio was sufficient to fabricate pure CePO nanorods.

Dehydrocostus lactone induces prominent apoptosis in kidney distal tubular epithelial cells and interstitial fibroblasts along with cell cycle arrest in ovarian epithelial cells.

Dehydrocostus lactone (DHCL), a sesquiterpene lactone is well-known for its antiulcer, anti-hepatotoxic and anticancer activity. However, the studies concerning the safety/toxicity potential of DHCL toward the cells of normal origin remain unclear. The present study is aimed at investigating the toxicity potential of DHCL in renal distal tubular and interstitial fibroblast cell lines (MDCK and NRK-49F cells, respectively), and also in ovarian epithelial cell line (CHO cells).

Synthesis and biological evaluation of Schizandrin derivatives as potential anti-cancer agents.

A new series of Schizandrin (1) derivatives were synthesized utilizing the C-9 position of the Schizandrin core and evaluated for their cytotoxic activities against HeLa (cervical cancer), A549 (lung cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer) cell lines. Among the synthesized series, 4e, 4f, 4g and 5 showed potent activities against tested cell lines. More significantly, compound 5 exhibited most potent cytotoxic activity against DU-145 with an IC value of 1.