Browsing by Author "Jaitak V."

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Asparagus racemosus (Shatavari) targeting estrogen receptor a: - An in-vitro and in-silico mechanistic study
(Taylor and Francis Ltd., 2018) Sharma R.; Jaitak V.
Breast cancer is a disease where cells in the tissue of the breast, grow and divide without normal control. Breast cancer is second major cause for death in world wide. Importance of natural product increase due to adverse effect of existing synthetic drugs. Asparagus racemosus comprises phytoestrogens which can be used for the treatment of breast cancer. In the current study, In vitro antiproliferative activity of the extracts of A. racemosus is performed in T47D cancer cell lines. Outcomes of the result indicated that aqueous methanol and methanol extract showed excellent antiproliferative activity as compared to bazedoxifene (standard), ethyl acetate and petroleum ether extract. In silico study of reported phytochemical constituents of A. racemosus was performed for understand the molecular mechanism and prospect pharmacophore development. Furthermore, compound 26 (rutin) which has been earlier reported and isolated from alcoholic extract exhibited the remarkable binding profile with estrogen receptor ?. For that reason, our study proposed that A. racemosus could be used as a new source for the treatment of breast cancer.
Chemical composition and biological activity of essential oils of dracocephalum heterophyllum and hyssopus officinalis from western himalaya
(Natural Product Incorporation, 2015) Stappen I.; Wanner J.; Tabanca N.; Wedge D.E.; Ali A.; Kaul V.K.; Lal B.; Jaitak V.; Gochev V.K.; Schmidt E.; Jirovetz L.
The essential oils of two representatives of the Lamiaceae, Dracocephalum heterophyllum Benth. And Hyssopus officinalis L., are described for their antifungal, antibacterial, larvicidal and inect biting deterrent activities. Additionally, the chemical compositions of the essential oils, analyzed by simultaneous GC-MS and GC-FID, and odor descriptions are given. The main components of H. officinalis oil were pinocarvone, cis-pinocamphone, and-pinene. Citronellol was found as the main compound of D. heterophyllum essential oil. Antibacterial testing by agar dilution assay revealed greater activity of D. heterophyllum against Staphylococcus aureus compared with H. officinalis. D. heterophyllum essential oil also showed promising antifungal activity against Colletotrichum species and was more toxic to Aedes aegypti larvae in a larvicial bioassay. Both essential oils showed high activity in the biting deterrent bioassay.
Coumarin Derivatives as Anticancer Agents for Lung Cancer Therapy: A Review
(NLM (Medline), 2018) Kumar M.; Singla R.; Dandriyal J.; Jaitak V.
BACKGROUND: The prevalence of lung cancer is 14% among the newly diagnosed cancer cases worldwide. Currently, the number of drugs that are in clinical practice is having a high prevalence of side effect and multidrug resistance. Researchers have made an attempt to expand a suitable anticancer drug that has no MDR and side effect. OBJECTIVE: Extensive exploration of Coumarin derivatives as a potent inhibitor of variety of proteins including EGFR, tyrosine kinase, ERK1/2, PI3K, HSP 90, Bax, STAT proteins, NF-?B and telomerase which have been associated with lung cancer. METHOD: The recent literature was surveyed utilizing the online resources and databases including scifinder, pubchem, EMBL, scopus and google scholar. RESULTS: Upon analyzing the structure-activity relationship, it was found that N-aryl carboxamide, phenyl substitution at the C-3 position and 1,2,3- triazolyl, trihydroxystilbene, amino substitution at the C-4 position of the coumarin nucleus were the most effective in targeting lung cancer. CONCLUSION: This review is a collaborative and extensive compilation of synthetic strategies, mechanism of action, and the structure-activity relationship thereof for the management of lung carcinoma. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-?)
(Elsevier Masson SAS, 2018) Singla R.; Gupta K.B.; Upadhyay S.; Dhiman, Monisha; Jaitak V.
In the course of efforts to develop novel selective estrogen receptor modulators (SERMs), indole-benzimidazole hybrids were designed and synthesised by fusing the indole nucleus with benzimidazole. All the compounds were first inspected for anti-proliferative activity using ER-? responsive T47D breast cancer cell lines and ER-? binding assay. From this study, two representative bromo substituted compounds 5f and 8f were found to be most active and thus were escalated for gene expression studies for targeting ER-?. Cell imaging experiment clearly suggest that compounds were able to cross cell membrane and accumulate thus causing cytotoxicity. RT-PCR and Western blotting experiments further supported that both compounds altered the expression of mRNA and receptor protein of ER-?, thereby preventing the further transactivation and signalling pathway in T47D cells lines. Structural investigation from induced fit simulation study suggest that compound 5f and 8f bind in antagonistic conformation similar to bazedoxifene by extensive hydrogen bonding and Van der Waals forces. All these results strongly indicate that compound 5f and 8f represents a novel potent ER-? antagonist properties and will proved promising in the discovery of SERM for the management of breast cancer.
Plant-derived natural alkaloids as new antimicrobial and adjuvant agents in existing antimicrobial therapy
(Bentham Science Publishers, 2019) Pal Mittal R.; Jaitak V.
Infectious diseases, instigated by pathogenic microorganisms are the cause of numerous health problems in developing countries. Infectious diseases got a place in the list of top ten death causes worldwide. The reason behind that level of severity is antimicrobial resistance. Antimicrobial resistance makes the antimicrobial agents useless when used in the treatment of infectious diseases. Microbes have very smartly achieved resistance against synthetic and semi-synthetic antimicrobial agents for their survival. Therefore, the handling of these diseases has become challenging. The resistance developing power is the reason for their existence since a million years. Due to their highly dangerous nature, proper treatment of infectious diseases has become a topic of concern. This leads the scientists or researchers to focus their research towards natural agents. Plants synthesize secondary metabolites to cope up with biotic and abiotic changes in the environment. Alkaloids are one of the secondary metabolites, synthesized by plants. Alkaloids protect the plant from predators and help them to fight with pathogens. The protecting nature of alkaloids can be used as a strong weapon in battle with resistant microorganisms. The purpose of this review is to provide information about the antimicrobial activity of alkaloids obtained from different plants and their combination with synthetic antimicrobials. Their mechanism of action against microorganisms is also given in the review.
Recent development in indole derivatives as anticancer agents for breast cancer
(Bentham Science Publishers, 2019) Kaur K.; Jaitak V.
Background: Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Therefore, there is an urgent need for the development of more effective and safer anti BC agents. Objective: This article explored in detail the possibilities of indole-based heterocyclic compounds as anticancer agents with breast cancer as their major target. Methods: Recent literature related to indole derivatives endowed with encouraging anti BC potential is reviewed. With special focus on BC, this review offers a detailed account of multiple mechanisms of action of various indole derivatives: aromatase inhibitor, tubulin inhibitor, microtubule inhibitor, targeting estrogen receptor, DNA-binding mechanism, induction of apoptosis, inhibition of PI3K/AkT/NFkB/mTOR, and HDAC inhibitors, by which these derivatives have shown promising anticancer potential. Results: Exhaustive literature survey indicated that indole derivatives are associated with properties of inducing apoptosis and disturbing tubulin assembly. Indoles are also associated with the inhibition of NFkB/mTOR/PI3K/AkT and regulation of estrogen-mediated activity. Furthermore, indole derivatives have been found to modulate critical targets such as topoisomerase and HDAC. These derivatives have shown significant activity against breast cancer cells. Conclusion: In BC, indole derivatives seem to be quite competent and act through various mechanisms that are well established in case of BC. This review has shown that indole derivatives can further be explored for the betterment of BC chemotherapy. A lot of potential is still hidden which demands to be discovered for upgrading BC chemotherapy.
Stevia rebaudiana targeting ?-amylase: An in-vitro and in-silico mechanistic study
(Taylor and Francis Ltd., 2019) Singla R.; Singla N.; Jaitak V.
Diabetes mellitus (DM) is the fastest growing metabolic disorder in the world. Recently, more attention is paid to the study of natural products due to side effects of synthetic drugs. Stevia rebaudiana (Bertoni) is considered an encouraging starting point for the antidiabetic lead development. In the present study, the in vitro ?-amylase inhibitory activity of the extracts of S. rebaudiana is investigated. In order to understand the molecular mechanism and future pharmacophore development, in silico study of secondary metabolites isolated from S. rebaudiana was carried out. Results indicated that water extract shows highest ?-amylase inhibitory activity as compared to other extracts. Moreover, compound 20 (rebaudioside A) which has been previously reported and isolated from water extract showed the impressive binding profile with ?-amylase. Therefore, our study suggests that S. rebaudiana could be used in the development of therapeutic drugs for the treatment of diabetes.