Cancer remains a global health challenge, necessitating the exploration of novel therapeutic agents. Current treatment options are unable to overwhelm and cure the cancer burden. Hence, identifying new bioactive molecular entities with potent anticancer activity is the need of the hour.
View Article and Find Full Text PDFProgesterone Receptor Membrane Component 1 (PGRMC1) is a candidate oncogene with a prominent involvement in the pathogenesis of diverse cancers (ovarian, thyroid, breast, colon, head, and neck). Our study ascertains the ability of PGRMC1 to influence WNT members in the non-small cell lung cancer subtype-lung adenocarcinoma (LUAD) and participates in augmented cell proliferation and migration. Both computational and in vitro experimental analyses were performed in this study.
View Article and Find Full Text PDFUnlabelled: Methylated gallic acid (MGA) is a potent anticancer biomolecular entity (BME). Loading MGA into a nano-vesicular (NV) drug delivery system using nanotechnology approaches can increase the efficiency of the drug and its release characteristics. This study aimed to develop an ethosomal nano-vesicular (ENV) system loaded with MGA that shows augmented entrapment efficiency, release rate, and cytotoxic potential against oral cancer.
View Article and Find Full Text PDFTriple-negative breast cancer (TNBC) is one of the most fatal and aggressive type of cancer in younger population. TNBC is poorly diagnosed, detected only at later stages with low survival rate and high chemoresistance. The expression of the cancer stem cell (CSC) markers has critical role in chemoresistance and recurrence.
View Article and Find Full Text PDFIntroduction: Bromelain belongs to the cysteine protease endopeptidase class of enzymes isolated from the stem and fruit tissue component of . The commercial and translational therapeutic potential of bromelain is ever increasing due to its augmented stability, easier purification, and salubrious pan-cancer effects.
Areas Covered: This paper presents the current state of knowledge about the isolation methods of bromelain, its safety, efficacy and tolerability.
Background: Homologous recombination repair (HRR) accurately repairs the DNA double-strand breaks (DSBs) and is crucial for genome stability. Genetic polymorphisms in crucial HRR pathway genes might affect genome stability and promote tumorigenesis. Up to our knowledge, the present study is the first to investigate the impact of HRR gene polymorphisms on BC development in South Indian women.
View Article and Find Full Text PDFEndocr Metab Immune Disord Drug Targets
July 2022
Progesterone receptor membrane component 1 (PGRMC1) is a trans-membrane evolutionarily conserved protein with a cytochrome b5 like heme/steroid binding domain. PGRMC1 clinical levels are strongly suggested to correlate with poor patient survival and lung cancer prognosis. PGRMC1 has been reported to possess pleiotropic functions, such as participating in cellular and membrane trafficking, steroid hormone signaling, cholesterol metabolism and steroidogenesis, glycolysis and mitochondrial energy metabolism, heme transport and homeostasis, neuronal movement and synaptic function, autophagy, anti-apoptosis, stem cell survival and the list is still expanding.
View Article and Find Full Text PDFWith ever increasing evidences on the role of fusion genes as the oncogenic protagonists in myriad cancers, it's time to explore if fusion genes can be the next generational drug targets in meeting the current demands of higher drug efficacy. Eliminating cancer stem cells (CSC) has become the current focus; however, we have reached a standstill in drug development owing to the lack of effective strategies to eradicate CSC. We believe that fusion genes could be the novel targets to overcome this limitation.
View Article and Find Full Text PDFComp Biochem Physiol C Toxicol Pharmacol
September 2021
Non-alcoholic fatty liver disease (NAFLD), also known as hepatic steatosis, is highly prevalent in developed countries despite advancements in clinical modalities. Therefore, there is a need for identifying the bioactive molecular entity (BME) that can therapeutically intervene with liver steatosis progression. In this study, we investigated the efficacy of one such BME - ellagic acid (EA) to ascertain its molecular therapeutic potential against iodoacetamide (IAA) mediated liver steatosis in an adult zebrafish model.
View Article and Find Full Text PDFBackground: Functional variants of the xenobiotic-metabolizing genes (XMG) might modulate breast cancer (BC) risk by altering the rate of metabolism and clearance of myriad types of potent carcinogens from the breast tissue. Despite mounting evidence on the role of XMG variants on BC risk, the current knowledge regarding their influence on BC development is still fragmentary.
Methods: The present study examined the candidate genetic variants in CYP1A1, NQO1, GST-T1, GST-M1, and GST-P1 in 1002 subjects (502 BC patients and 500 disease-free women).
Globally, one of the alarming problems is the prevalence and burden of liver diseases, which accounts for 2 million cases per year. Chronic liver aetiologies such as hepatitis infections, alcoholic or non-alcoholic liver disease, environmental agents, and drug-induced toxicity are invariably responsible for liver fibrosis progression to finally hepatocellular carcinoma. Current treatment options are unable to overwhelm and cure liver diseases.
View Article and Find Full Text PDFTriple-negative breast cancer (TNBC) is a heterogeneous breast cancer subtype that lacks targeted therapy due to the absence of estrogen, progesterone, and HER2 receptors. Moreover, TNBC was shown to have a poor prognosis, since it involves aggressive phenotypes that confer significant hindrance to therapeutic treatments. Recent state-of-the-art sequencing technologies have shed light on several long non-coding RNAs (lncRNAs), previously thought to have no biological function and were considered as genomic junk.
View Article and Find Full Text PDFJ Biomol Struct Dyn
May 2022
Cardiovascular disease (CVD) is the leading cause of mortality among the human species, however the non-existence of successful therapies to curtail the effect of Myocardial Infarction (MI) is a disquieting reality. Even though successful herbal formulations using (COC) is available, however, it is not recognized as an alternative medicine due to the lack of explanation on the molecular mechanism of COC extract on CVD conditions. studies revealed that COC extract significantly prevented caspase activation in conditions like post-MI; however, the role of a specific secondary metabolite that could be involved in this action is under quest.
View Article and Find Full Text PDFEndocr Metab Immune Disord Drug Targets
November 2021
MicroRNAs regulate gene expression at the posttranscriptional level by binding to the mRNA of their target genes. The dysfunction of miRNAs is strongly associated with the inflammation of the colon. Besides, some microRNAs are shown to suppress tumours, while others promote tumour progression and metastasis.
View Article and Find Full Text PDFThe Global cancer incidence and mortality data released by the World Health Organization proposes that out of 18.1 million new cancer cases diagnosed, 9.8 million deaths occurred globally in 2018.
View Article and Find Full Text PDFQuercetin is a bioactive compound with anti-inflammatory, antioxidant and anticancer properties. This study exemplifies the differential cytotoxic activity of Quercetin on two human colonic cancer cell lines, HT29 and HCT15. IC of Quercetin for HT29 and HCT15 cells were 42.
View Article and Find Full Text PDFSnake venom 5'-nucleotidase (5'NUC) plays a very important role in envenomation strategies; however, apart from its modulation of hemostatic functions, its other pharmacological effects are not yet well characterized. Several studies have used specific inhibitors of enzyme toxins as a biochemical or pharmacological tool to characterize or establish its mechanism of action. We report here for the first time vanillin mandelic acid (VMA), an analog of vanillin, to potentially, selectively, and specifically inhibit venom 5'NUC activity among other enzymes present in venoms.
View Article and Find Full Text PDFIn spite of availability of moderately protective vaccine and antibiotics, new antibacterial agents are urgently needed to decrease the global incidence of Klebsiella pneumonia infections. MurF ligase, a key enzyme, which participates in the bacterial cell wall assembly, is indispensable to existence of K. pneumonia.
View Article and Find Full Text PDFContext: Rubia cordifolia Linn. (Rubiaceae) is a medicinal plant used in the ayurvedic system of medicine. It is also known as Indian Madder or Manjistha and is traditionally used as an antiinflammatory, antiseptic, and galactopurifier, but its anticancer propertis are yet not known.
View Article and Find Full Text PDFHere we investigated the in vivo effect of morin (500ppm in diet) in fostering apoptosis in diethylnitrosamine (DEN) (200mg/kg bodyweight) mediated experimental hepatocellular carcinogenesis model. We analyzed the expression of cytosolic protein Akt and their important apoptotic downstream targets like caspase-9, Bcl-2, Bax, GSK-3betain vivo, by immunoblot analysis. In silico docking studies indicated that morin could serve as a better inhibitor than the classical PI3K inhibitor LY294002.
View Article and Find Full Text PDFMorin (3,5,7,2',4'-pentahydroxyflavone), a plant-derived flavonoid belonging to the subclass of flavonol is believed to play a role in chemoprevention and cancer chemotherapy. In this study, we found that the cotreatment of morin (500 ppm in diet) for 16 weeks to N-nitosodiethylamine-induced (200 mg/kg bodyweight in drinking water) rats provides protection against the oxidative stress caused by the carcinogen and thereby prevents hepatocellular carcinogenesis. On administration of the carcinogen, the level of lipid peroxidation increased markedly, but was found to be significantly lowered by morin treatment.
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