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Insights into the Phytochemical Profile and Therapeutical Potential of Withania Somnifera (L.) Dunal
Authors: Mehak Katyal, Rajesh Kumar, Divya Jain, Nidhi Chatterjee and Kuldeep SinghAvailable online: 24 October 2024More LessWithania somnifera (L.) Dunal (W. somnifera) is an herb commonly known by its English name Winter Cherry, and Ashwagandha in Hindi. It has been used as a traditional Rasayana herb for a long time. It is a rich reservoir of bioactive compounds known as withanolides, namely, withaferin-A and withanolide-D. Its current research covers many aspects of human health, which include anti-stress, anti-tumor, 9immuno-modulatory, hypocholesterolemic, hepatoprotective, hypoglycemic, diuretic, anti-convulsant, neurotropic, adaptogenic, and cardioprotective properties. This overview W. somnifera traditional uses, phytochemical, and pharmacological activities. However, in-depth studies are needed on the clinical use of W. somnifera against human diseases. Besides, detailed toxicological analysis is also to be performed for its safe and efficacious use in preclinical and clinical studies and as a health-promoting herb.
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Bakuchiol and their Derivatives: Unveiling its Chemistry, SAR, Pharmacological Marvels and Therapeutic Odyssey
Available online: 09 October 2024More LessBakuchiol, a meroterpene natural product found in various plants, exhibits diverse biological activities, notably anticancer properties. Researchers have synthesized numerous analogs targeting different positions, such as alcoholic OH, ethenyl, and isopropylidene groups within bakuchiol, aiming to enlighten potent therapeutic agents with enhanced pharmaceutical characteristics. The review aims to focus on the extensive potential of the bioactive molecule, bakuchiol describing SAR that may lead to the development of a variety of bakuchiol derivatives. Literature survey has been carried out to determine the potential of bakuchiol and its derivatives. This review comprehensively outlines the biosynthesis, isolation, patent, and clinical studies of bakuchiol, and pharmacological potential of bakuchiol derivatives documented to date. Additionally, it explores the structure-activity relationships observed in its derivatives. Collectively, findings from various studies underscore the significant potential of bakuchiol and its derivatives in the development of potent anticancer and other therapeutic agents. Ultimately, this review serves as a valuable resource for researchers interested in both the chemistry and biology of bakuchiol, offering insights into its multifaceted applications and paving the way for further exploration in this field.
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Cucurbitacin-E; Curvularia lunata Secondary Metabolite as a BRCA 1 and 2 Regulator in Mice Associated Breast Cancer
Available online: 09 October 2024More LessBackgroundCucurbitacin-induced apoptosis and inhibition of cell growth can render several cancers ineffective. The microbial transformation of cucurbitacin-E-glucoside to cucurbitacin-E was carried out by Curvularia lunata (NRRL 2178). Moreover, in vitro anticancer activity against the MCF-7 cell line as well as in vivo anticancer activity against dimethylbenz (a) anthracene (DMBA)-induced breast cancer in mice using cucurbitacin-E was evaluated.
MethodsThe cucurbitacin-E-glucoside was biotransformed by Curvularia lunata to cucurbitacin-E, and the isolated compound was tested in vitro against the MCF-7 cell line, and its IC50 was calculated. LD50 of cucurbitacin-E was estimated in mice, and its protective activity against DMBA-induced cancer in mice was studied. Breast cancer induction was done by a single-dose subcutaneous administration of DMBA (50 mg). Plasma ALT, AST, ALP, and LDH, as well as GSH, SOD, GPx, MDA, TNF-α, IL-6, and tumor suppressor P53 assays, were used to assess cucurbitacin-E's capacity to protect the liver and breast against DMBA-induced toxicity. Moreover, by assessing the gene expression of tumor suppressor genes (BRCA 1 and 2) and conducting histopathological analysis, the suppressive effect of cucurbitacin-E was examined.
ResultsThe IC50 value of cucurbitacin-E against MCF-7 cell lines equals 72.15 ± 0.64 µg/ml. LD50 of cucurbitacin-E given orally in adult mice is equal to 1200 mg/kg b.w. The levels of plasma ALT, AST, ALP, and LDH were decreased significantly in DMBA-treated mice when administered with cucurbitacin-E at 1/50 LD50 (24 mg/kg/b.w.) and 1/20 LD50 (60 mg/kg/b.w.). In breast tissue, the levels of GSH, SOD, GPx, and P53 were significantly increased, as were decreased levels of TNF-α, IL-6, P53, and MDA. Conversely, there was a downregulation in the mRNA expression levels of BRCA1 and BRCA2. The histopathological analysis revealed that cucurbitacin-E management improved the tissue architecture of breast tumors.
ConclusionsThese findings demonstrate the ability of cucurbitacin-E to inhibit cancer cells in the rat breast by controlling oxidative stress and inflammatory biomarkers, as well as downregulating the mRNA expression levels of BRCA1 and BRCA2.
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An Assessment of Antidepressant Activity of Etlingera elatior Alone and in Combination with Fluoxetine
Available online: 09 October 2024More LessAimPresent study deals to access the antidepressant activity of Etlingera elatior leaves extract in rodent.
BackgroundEtlingera elatior is a species of herbaceous perennial plant in the family Zingiberaceae; native to Indonesia, Thailand, Malaysia and New Guinea. Depression is one of the most common mental disorders affecting humans, pathological basis of which is not fully understood. The current antidepressant drugs have several adverse effects including their effects on cognition. Therefore, natural product are being evaluated for their antidepressant activities.
ObjectiveIn this study, Etlingera elatior leaf extracts are being evaluated for antidepressant activity in rodent models. A wide range of synthetic medicines that can be used to treat depression which may exerts various side effects such as dry mouth, gastrointestinal problems, nausea, respiratory problems, cardiac arrhythmias, drowsiness, anxiety etc. Hence, it becomes essential to discover new anti-depressant drug with more potency, efficacy and safety profile than those of marketed synthetic drugs.
MethodsUsing the forced swimming test, the tail suspension test, mouse 5-HTP-induced head twitches and estimation of brain lipid peroxidation modelsthe antidepressant efficacy of Etlingera elatior ethanolic extract was examined. Imipramine was used as reference standards.
ResultsAccording to our study, Etlingera elatior significantly (p 0.01) reduced immobility in tail suspension, forced swimming, and 5-HTP-induced head twitches in mice with depression that were comparable to imipramine.
ConclusionBased on the results obtained we can conclude that Etlingera elatior leaves extract possess significant antidepressant activity. The antidepressant effectiveness of Etlingera elatior leaves extract can be confirmed in the future by adding more models, and attempts can also be made to isolate and characterise the phytoconstituents responsible for the pharmacological action.
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A Review on Recent Synthesis and Diverse Biological Activities of Isoquinolone
Available online: 08 October 2024More LessIsoquinolone scaffolds are among the most important core structures of nitrogen heterocyclic compounds, which possess vital roles in biological and physiological activities such as anti-tumor, anti-microbial, anti-leukemic, anti-malaria, anti-dengue, anti-HIV and anti-bacterial. Over the years, multiple studies have been done to synthesize these isoquinolone derivatives, and several authors have reported on various methods and synthetic routes to produce the target skeletons of isoquinolones. Therefore, many scientific communities have developed these compounds as the intended structure and evaluated their biological activities. Thus, this review confers several information on isoquinolone analogue synthetic strategies and their biological effects on mosquito-borne diseases.
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Podophyllotoxin: Current Perspectives
Authors: Ying Qian Liu, Liu Yang and Xuan Tian
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