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.

Organ-Specific Metabolomics of Aerial Parts of Melochia corchorifolia for Antibiofilm and Wound Healing Activities.

Melochia corchorifolia is a well-known perennial herb and has been used in traditional medicine for the treatment of a wide number of diseases. However, the phytochemical investigation in the different organs of the M. corchorifolia was poorly understood.

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.

Repurposing of Antifungal Drug Flucytosine/Flucytosine Cocrystals for Anticancer Activity against Prostate Cancer Targeting Apoptosis and Inflammatory Signaling Pathways.

This study aimed to repurpose the antifungal drug flucytosine (FCN) for anticancer activity together with cocrystals of nutraceutical coformers sinapic acid (SNP) and syringic acid (SYA). The cocrystal screening experiments with SNP resulted in three cocrystal hydrate forms in which two are polymorphs, namely, FCN-SNP F-I and FCN-SNP F-II, and the third one with different stoichiometry in the asymmetric unit (1:2:1 ratio of FCN:SNP:HO, FCN-SNP F-III). Cocrystallization with SYA resulted in two hydrated cocrystal polymorphs, namely, FCN-SYA F-I and FCN-SYA F-II.

Nickel-doped vanadium pentoxide (Ni@VO) nanocomposite induces apoptosis targeting PI3K/AKT/mTOR signaling pathway in skin cancer: An in vitro and in vivo study.

In the present study, the vanadium pentoxide (VO) nickel-doped vanadium pentoxide (Ni@VO) was prepared and determined for in vitro anticancer activity. The structural characterization of the prepared VO and Ni@VO was determined using diverse morphological and spectroscopic analyses. The DRS-UV analysis displayed the absorbance at 215 nm for VO and 331 nm for Ni@VO as the primary validation of the synthesis of VO and Ni@VO.

NLRP3 inhibitors: Unleashing their therapeutic potential against inflammatory diseases.

The NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome has been linked to the release of pro-inflammatory cytokines and is essential for innate defence against infection and danger signals. These secreted cytokines improve the inflammatory response caused by tissue damage and associated inflammation. Consequently, the development of NLRP3 inflammasome inhibitors are viable option for the treatment of diverse inflammatory disorders.

Synthesis of aminomethyl linked (+)-usnic acid derivatives the Mannich reaction and evaluation of their biological activities.

(+)-Usnic acid (UA), a natural dibenzofuran derivative, abundantly produced by lichens and possess wide number of biomedical applications including antibacterial, anti-inflammatory, anti-oxidant and anticancer activities. In the present study, as series of usnic acid derivatives () were synthesised using Mannich reaction assessed for their antioxidant, α-glucosidase, and anticancer activities. The antioxidant activity showed that compound displayed potent antioxidant activity by scavenging the activities of DPPH and ABTS.

Comprehensive metabolomic analysis of Mangifera indica leaves using UPLC-ESI-Q-TOF-MS for cell differentiation: An in vitro and in vivo study.

The comprehensive metabolic profiling was performed in the leaf extracts of Mangifera indica and assessed for their significant therapeutic application in tissue engineering and regenerative medicine in both in vitro and in vivo studies. About 147 compounds were identified in the ethyl acetate and methanol extracts of M. indica using MS/MS fragmentation analysis and the selected compounds were quantified using LC-QqQ-MS analysis.

Synthesis of novel thiazoles bearing lupeol derivatives as potent anticancer and anti-inflammatory agents.

Lupeol is one of the most important metabolite in the class of terpenoids and possess excellent anticancer, anti-inflammatory, anti-diabetic activities etc. In the present study, the different thiazoles and oxazoles bearing lupeol derivatives were prepared to enhance their biological activity. Initially, the cytotoxic activity results showed that the synthesized lupeol derivatives ( and ) showed significant activity against various cancer cells and the compounds and exhibited excellent activity against CAL27 cells.

UPLC-ESI-Q-TOF-MS-based metabolomics analysis of sap and evaluation of osteogenic activity in mouse osteoblast cells.

Investigation of phytochemicals and bioactive molecules is tremendously vital for the applications of new plant resources in chemistry, food, and medicine. In this study, the chemical profiling of sap of Acer mono (SAM), a Korean syrup known for its anti-osteoporosis effect, was performed using UPLC-ESI-Q-TOF-MS analysis. A total of 23 compounds were identified based on the mass and fragmentation characteristics and most of the compounds have significant biomedical applications.

N-(2-hydroxyphenyl)-2-phenazinamine from Nocardiopsis exhalans induces p53-mediated intrinsic apoptosis signaling in lung cancer cell lines.

The present study aims to investigate the effect and the molecular mechanism of N-(2-hydroxyphenyl)-2-phenazinamine (NHP) isolated from Nocardiopsis exhalans against the proliferation of human lung cancer cells. The cytotoxic activity of NHP against A549 and H520 cells was determined using MTT assay. The cytotoxic activity of NHP against A549 and H520 lung cancer cells showed excellent activity at 75 μg/mL and damage the mitochondrial membrane and nucleus by generating oxidative stress.

Synthesis of quercetin functionalized wurtzite type zinc oxide nanoparticles and their potential to regulate intrinsic apoptosis signaling pathway in human metastatic ovarian cancer.

In the present study, the wurtzite (WZ) type of zinc oxide (ZnO) nanoparticles were synthesized and functionalized with quercetin (ZnO@Quercetin) for the treatment of ovarian cancer. Initially, the chemical synthesis of ZnO nanoparticles was confirmed with DRS UV-vis spectroscopy and the bandgap of the ZnO revealed that the WZ type of nanoparticles. The electron microscopy analysis showed the hexagonal shape, monocrystalline nature of nanoparticles with an average size of 20-25 nm and the SAED pattern showed the interplanar planes for WZ type nanoparticles.

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.

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.

Highly efficient visible light driven photocatalytic activity of zinc/ferrite: Carbamazepine degradation, mechanism and toxicity assessment.

In this present study, spherical shaped zinc ferrite (Zn/FeO) was prepared as uniformly sized (65 ± 0.5 nm) nanoparticles with band gap (2.00 eV) in a visible light regime and employed for the photocatalytic degradation of carbamazepine (CBZ).

Enhanced visible light-driven photocatalysis of iron-oxide/titania composite: Norfloxacin degradation mechanism and toxicity study.

A simulated visible light-mediated iron oxide-titania (IoT) nanocomposite was employed to degrade the antibiotic norfloxacin (NFN) photocatalytically. The photocatalyst were prepared using a sol-gel method with controlled titania loadings to iron oxide by altering the fabrications step. The nanocomposites were structurally characterized by field emission scanning electron microscopy (FE-SEM), energy-dispersive X-ray spectroscopy (EDX), field emission high-resolution transmission electron microscopy (HR-TEM), X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, Diffuse reflectance UV-visible spectra (DRS-UV) spectroscopy, cyclic voltammetry, and X-ray photoelectron spectroscopy (XPS).

Human Prostate Epithelial Cells Activate the AIM2 Inflammasome upon Cellular Senescence: Role of POP3 Protein in Aging-Related Prostatic Inflammation.

Increased levels of type I (T1) interferon (IFN)-inducible POP3 protein in myeloid cells inhibit activation of the AIM2 inflammasome and production of IL-1β and IL-18 proinflammatory cytokines. The mRNA levels were significantly higher in benign prostate hyperplasia (BPH) than the normal prostate. Further, human normal prostate epithelial cells (PrECs), upon becoming senescent, activated an inflammasome.

Identification of Meat Quality Determining Marker Genes in Fibroblasts of Bovine Muscle Using Transcriptomic Profiling.

In the present study, we comparatively analyzed the transcriptomic profiling of fibroblasts derived from two different muscles, biceps femoris and longissimus dorsi with significant difference in the meat quality and tenderness. EBSeq algorithm was applied to analyze the data, and genes were considered to be significantly differentially expressed if the false discovery rate value was <0.05, the value was <0.

Titanium decorated iron oxide (Ti@FeO) regulates the proliferation of bovine muscle satellite cells through oxidative stress.

In the present study, the titanium decorated iron oxide (Ti@FeO) nanocomposites are synthesized using the chemical method. The as-prepared nanocomposite was characterized for successful formulation and the elemental spectra showed the composition of Fe (44%), Ti (0.71%) and O (55%) is confirmed the homogenous distribution.

Enhanced visible light-driven photocatalytic activity of reduced graphene oxide/cadmium sulfide composite: Methylparaben degradation mechanism and toxicity.

Reduced graphene oxide/cadmium sulfide (RGOCdS) nanocomposite synthesized through solvothermal process was used for methylparaben (MeP) degradation. The crystallinity of the nanocomposite was ascertained through X-ray diffraction. High resolution transmission electron microscope (HRTEM) results proved the absence of any free particle beyond the catalyst surface ensuring the composite nature of the prepared material.

In situ one-step synthesis of polymer-functionalized palladium nanoparticles: an efficient anticancer agent against breast cancer.

Breast cancer is the most common malignancy among women worldwide, and researchers are working to discover effective treatments to eradicate breast cancer. In the present study, we prepared PVP-functionalized palladium nanoparticles (PVP-PdNPs) for the treatment of human breast cancer MCF7 cells. Initially, the PVP-functionalized PdNPs were synthesized by an in situ method and confirmed with DRS-UV spectrometric analysis.