Browsing by Author "Jaitak, Vikas"
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Item Anticancer activity of cassia fistula linn through invitro and insilicoapproach(Central University of Punjab, 2014) Sharma, Akanksha; Jaitak, VikasCassia fistula L. (Leguminoseae) is a plant species called "Aragvadha" that means "disease killer". C. fistula consists of plethora of medicinal properties. A detailed discussion is depicted of the therapeutic potential and chemical composition of C. fistula that is responsible for its highly important medicinal properties. C. fistula contains many chemical components like anthraquinones, anthocyanindins, proanthocyanidins, flavanoids, polyphenols, alkaloids, saponins, coumarins, tannins, etc. These constituents are reported to possess various biological properties such as antioxidant, antimicrobial, antidiabetic, antitumor, antimelasmic activities etc. In the current dissertation work we limited our study to cancer; specifically, Lung cancer (LC) and Breast cancer (BC) which are spread all over the world to a threatening level. The present study is an effort to contribute to such a multi-targeting moiety from the plant C. fistula, on the basis of in vitro and simulated analysis. To explore the anticancer activity of C. fistula; in vitro (cytotoxicity studies) on different extracts and in silico studies using MMGBSA (Molecular Mechanics - the Generalized Born model and Solvent Accessibility) on the earlier reported molecules was performed; to study protein - ligand binding interactions on four different targets. The different extracts (Petroleum v ether (SVA-1) (for defatting), Ethyl acetate (SVA-2), Methanol (SVA-3), Hydro- methanolic (SVA-4) Extracts) were prepared in order of their increasing polarity. In- vitro cytotoxicity studies done using MTT (3-(4, 5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) assay on the extracts of plant and their IC50 values were calculated. It was performed to identify plant's cytotoxic activity. Targets studied via performing in silico protein-ligand binding interactions of majorly mutated yet interlinked pathways of tyrosine kinase and serine/ threonine kinase family; that are namely EGFR, PI3K, Akt and mTOR receptors on which reported molecules of plant were studied. In silico studies were performed using maestro 9.6 Schrodinger software. MMGBSA and ADMET analysis were performed to discover and understand protein - ligand interactions between the chosen ligands of Cassia fistula and selected kinase receptors. On conducting MMGBSA (Molecular Mechanics ' the Generalized Born model and Solvent Accessibility) studies 5,3,4-tri-hydroxy-6-methoxy-7-O-?-L- rhamnopyranosyl-(1?2)-O-?-D-galactopyranoside along with few other moieties illustrated fine binding interactions against standard inhibitors of all the protein targets. From in vitro experiment, it was found that Hydromethanolic extract (SVA-4) showed prominent cytotoxicity against MCF-7, A-549 and H-460 cell lines particularly near 50?g/ml of concentration. Results were found in comparable with the NCI criteria limits for IC50 values of extracts obtained in assay. Also extracts were stable in DMSO solvent even when kept at the ambient temperature for 30 days and gave consistent results against cancer cell lines. As per the results of the in silico studies, the 5,3,4-tri- hydroxy-6-methoxy-7-O-?-L-rhamnopyranosyl-(1?2)-O-?-D-galactopyranoside (dG Bind score -98.7866kcal/mol) for EGFR in comparison to gefitinib (dG Bind score - 86.5585kcal/mol); (dG Bind score -87.3524kcal/mol) for Akt as compared to AZD 5363 (dG Bind score -76.5959); (dG Bind score -87.1051kcal/mol) for PI3K as compared to wortmannin (dG Bind score -79.0654kcal/mol) and for mTOR it has shown the (dG Bind score of -81.964kcal/mol) against sirolimus (dG Bind score -192.354kcal/mol) is reported to have fair pharmacokinetic profile along with attractive binding interactions with EGFR, PI3K, Akt and mTOR receptors.Item Anticancer activity of essential oils: A review(2013) Bhalla, Yashika; Gupta, Vinay Kumar; Jaitak, VikasNatural essential oil constituents play an important role in cancer prevention and treatment. Essential oil constituents from aromatic herbs and dietary plants include monoterpenes, sesquiterpenes, oxygenated monoterpenes, oxygenated sesquiterpenes and phenolics among others. Various mechanisms such antioxidant, antimutagenic and antiproliferative, enhancement of immune function and surveillance, enzyme induction and enhancing detoxification, modulation of multidrug resistance and synergistic mechanism of volatile constituents are responsible for their chemopreventive properties. This review covers the most recent literature to summarize structural categories and molecular anticancer mechanisms of constituents from aromatic herbs and dietary plants. ? 2013 Society of Chemical Industry.Item Antimicrobial and repellent activity of the essential oils of two lamiaceae cultivated in Western Himalaya(Bentham Science Publishers B.V., 2015) Stappen, Iris; Ali, Abbas; Tabanca, Nurhayat; Khan,Ikhlas A.; Wanner, J�rgen; Gochev, Velizar K.; Singh, Virendra; Lal, Brij; Jaitak, Vikas; Kaul, Vijay K.; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Ali, A.; Tabanca, N.; Khan, I.A.; Wanner, J.; Gochev, V.K.; Singh, V.; Lal, B.; Jaitak, V.; Kaulh, V.K.; Schmidt, E.; Jirovetz, L.The essential oils of two Lamiaceae cultivated in Western Himalaya were examined on their antimicrobial, biting deterrent as well as larvicidal activity. Additionally their odors are described and their chemical compositions analyzed by GC-MS are given. The main component of Nepeta cataria oil was 4a?,7?,7a?-nepetalactone (85%), whereas camphor (27%) and 1,8-cineol (27%) were dominant in the oil of Rosmarinus officinalis. The studied essential oils demonstrated high to moderately antimicrobial activity against reference strains, clinical and food spoilage isolates of Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella abony and Candida albicans (MIC 160-640 ?g/ml) and indicated low activity against Pseudomonas aeruginosa and P. fluorescens. Both oils showed biting deterrent activity above solvent control but lower than DEET. Nepeta catarica essential oil exhibited high toxicity with LD50 value of 20.2 whereas R. officinalis oil showed only 50% mortality at the highest tested dose of 125 ppm against 1-day old Aedes aegypti larvae at 24-hour post treatment. ? 2015 Bentham Science Publishers.Item Antiproliferative activity of Asparagus racemosus extracts(Central University of Punjab, 2018) Sharma, Ram; Jaitak, VikasCancer is regarded as uncontrolled progression and spread of cells. Cancer is not a singular, specific disease but a group of variable tissue responses that result in uncontrolled cell growth. Healthy cells have a specific size, structure, function and growth rate that best serves the needs of the tissues they compose. Cancer is one of the leading of morbidity and mortality worldwide, with approximately 14 million new cases in 2017. Breast cancer (BC) is a disease where cells in the tissue of the breast cancer grow and divide without normal control. Estrogen receptor is a group of proteins (or a twelve helix protein) present inside the cells of the female reproductive tissues or located in the nucleus of cells. ER?, ER? and ER gamma have different responses and they are located in different tissues. Quinone forms of catechol estrogen binds to DNA and forms adduct. Semi Quinone intermediates are free radicals can bind with oxygen to producing superoxide radicals. Superoxide radicals can attack and alter the structure of DNA and causing Breast cancer. Various synthetic drugs (Tamoxifen & Raloxifene) are used for treatment of breast cancer, but numerous side effects like menopausal symptoms, vaginal dryness, low libido, mood swings and Nausea. The discovery of novel natural drugs is important for reduction of side-effects, high selectivity, low toxicity, and better killing of cancer cells. Phytoestrogens are one the best category of natural products used for treatment of breast cancer. Phytoestrogens have similar structure to the endogenous estrogen. Distance between the hydroxyl groups is 14.5 A0 is similar to estrogen. Asparagus racemosus contain large number of phytoestrogens. In this context, the aim of the present study was to explore the roots of Asparagus racemosus in the terms of its medicinal values for Breast cancer. Anticancer activity of different extracts were evaluated by performing In vitro study by using Breast cancer cell lines T-47 D. from the Preliminary phytochemical investigation of extracts demonstrated that methanolic extract and Aqueous methanolic extract contain large number of phytoestrogens. Aqueous methanolic extract and methanolic extract showed maximum IC50 value as compare to other extract. Isolation of molecules from methanol extract, total four molecules isolated from methanol extract and three molecules from aqueous methanol extract. Moreover, in silico study of reported phytoestrogen from Asparagus racemosus was also carried out using glide docking to investigate interaction pattern with estrogen receptor ? and estrogen receptor ?. The top docking score was obtained for Rutin (Estrogen receptor ?) and Quercetin (Estrogen receptor ?). Tamoxifen and raloxifene used as standard for estrogen receptor ? and oestradiol used as standard for estrogen receptor ?. From the ADME study demonstrated that maximum flavonoids has highest oral absorption as compare to other. The results showed that phytoestrogens are expected prospective candidate for regulatory tumor progression with a special emphasis in breast cancer progression.Item Chemical Composition and Biological Activity of Essential Oils from Wild Growing Aromatic Plant Species of Skimmia laureola and Juniperusmacropoda from Western Himalaya(NPC (Natural Product Communication), 2015) Stappena,Iris; Tabanca, Nurhayat; Ali, Abbas; Wedge, David E.; Wanner, J�rgen; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar K.; Schmidt, Erich; Jirovetz, LeopoldThe Himalayan region is very rich in a great variety of medicinal plants. In this investigation the essential oils of two selected species are described for their antimicrobial and larvicidal as well as biting deterrent activities. Additionally, the odors are characterized. Analyzed by simultaneous GC-MS and GC-FID, the essential oils’ chemical compositions are given. The main components of Skimmia laureola oil were linalool and linalyl acetate whereas sabinene was found as the main compound for Juniperus macropoda essential oil. Antibacterial testing by agar dilution assay revealed highest activity of S. laureola oil against all tested bacteria, followed by J. macropoda oil . Antifungal activity was evaluated against the strawberry anthracnose causing plant pathogens Colletotrichum acutatum , C. fragariae and C . gloeosporioides . Juniperus macropoda essential oil indicated higher antifungal activity against all three pathogens than S. laureola oil. Both essential oils showed biting deterrent activity above solvent control but low larvicidal activity.Item Chemical composition and biological activity of essential oils of dracocephalum heterophyllum benth And Hyssopus officinalis L Collected wild from Western Himalay(Sage, 2015) Stappena, Iris; Wannerb Jürgen; Tabanca, Nurhayat; Wedge, David E.; Ali, Abbas; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar K.; Schmidt, Erich; Jirovetz, LeopoldThe 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.Item Chemical composition and biological effects of Artemisia essential oils from Western Himalaya(Theime, 2014) Stappen, Iris; Wanner, J, rgen; Tabanca, Nurhayat; Wedge, David E.; Ali, Abbas; Khan, Ikhlas A.; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar; Girova, Tania; Stoyanova, Albena; Schmidt, Erich; Jirovetz, LeopoldArtemisia species possess pharmacological properties that are used for medical purposes worldwide. In this paper, the essential oils from the aerial parts of Artemisia nilagirica and Artemisia maritima from the western Indian Himalaya region are described. The main compounds analyzed by simultaneous GC/MS and GC/FID were camphor and 1,8-cineole from A. maritima, and camphor and artemisia ketone from A. nilagirica. Additionally, the oils were evaluated for their antibacterial, antifungal, mosquito biting deterrent, and larvicidal activities. A. nilagirica essential oil demonstrated nonselective antifungal activity against plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides, whereas A. maritima did not show antifungal activity. Both Artemisia spp. exhibited considerable mosquito biting deterrence, whereas only A. nilagirica showed larvicidal activity against Aedes aegypti. Antibacterial effects assessed by an agar dilution assay demonstrated greater activity of A. maritima essential oil against Staphylococcus aureus and Pseudomonas aeruginosa compared to A. nilagirica.Item Chemical composition and biological effects of artemisia maritima and artemisia nilagirica essential oils from wild plants of Western Himalaya(Georg Thieme Verlag, 2014) Stappen, Iris; Wanner, J, rgen; Tabanca, Nurhayat; Wedge, David E.; Ali, Abbas; Khan, Ikhlas A.; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar; Girova, Tania; Stoyanova, Albena; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Wanner, J.; Tabanca, N.; Wedge, D.E.; Ali, A.; Khan, I.A.; Kaul, V.K.; Lal, B.; Jaitak, V.; Gochev, V.; Girova, T.; Stoyanova, A.; Schmidt, E.; Jirovetz, L.Artemisia species possess pharmacological properties that are used for medical purposes worldwide. In this paper, the essential oils from the aerial parts of Artemisia nilagirica and Artemisia maritima from the western Indian Himalaya region are described. The main compounds analyzed by simultaneous GC/MS and GC/FID were camphor and 1,8-cineole from A. maritima, and camphor and artemisia ketone from A. nilagirica. Additionally, the oils were evaluated for their antibacterial, antifungal, mosquito biting deterrent, and larvicidal activities. A. nilagirica essential oil demonstrated nonselective antifungal activity against plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides, whereas A. maritima did not show antifungal activity. Both Artemisia spp. exhibited considerable mosquito biting deterrence, whereas only A. nilagirica showed larvicidal activity against Aedes aegypti. Antibacterial effects assessed by an agar dilution assay demonstrated greater activity of A. maritima essential oil against Staphylococcus aureus and Pseudomonas aeruginosa compared to A. nilagirica.Item Chemical composition, in�vitro and in silico evaluation of essential oil from Eucalyptus tereticornis leaves for lung cancer(Taylor and Francis Ltd., 2022-08-08T00:00:00) Anju; Kumar, Amit; Yadav, Poonam; Navik, Umashanker; Jaitak, VikasChemical composition of the essential oil (EO) of Eucalyptus tereticornis leaves was studied by gas chromatography�mass spectrometry. Forty-five constituents were identified in the oil hydrodistilled from the sample collected from Ghudda Village, Bathinda (Pb), India of which eucalyptol (34.39%) and ledol (9.92%) were the major constituents. In vitro antioxidant and anticancer potential of EO was analysed by DPPH 2,2-diphenylpicrylhydrazyl (DPPH) and MTT assay. The percentage free radical scavenging activity was found to be 63.77%. The antiproliferative activity was analysed using MTT assay in adenocarcinomic human alveolar basal epithelial A549 cancer cell line and showed IC50 value of 47.14 �g/ml. In silico study of EO, constituents were performed using Maestro 12.9 against EGFR (PDB ID-2RGP). Five constituents from EO showed high dockscore as compared to standard Mobicertinib which indicated the effectiveness of oil constituents against lung cancer. � 2022 Informa UK Limited, trading as Taylor & Francis Group.Item Chemical Investigation and Antiproliferative screening of extracts from Stevia rebaudiana (Bertoni)(Central University of Punjab, 2018) Saxena, Aditi; Jaitak, VikasCancer is the uncontrolled development of abnormal cells in the body. It is considered as the leading public health problem in both developed and the developing countries. As no drug of cancer is establish to be completely efficient and safe as anticancer therapy and is responsible for the prolonged toxicity and also causes various side effects. Chemoprevention of cancer by natural products is beneficial, as these compounds have the nominal side effects and short of toxicity compared to the synthetic compounds. The phenomena of Carcinogenesis is very complex and includes so many signaling pathways. Thus Phytochemicals are measured as the right candidates for developing the anticancer drug. The study for developing more potent candidates which can obstruct or slow down the expansion of the cancer cells without c au s in g any side effects from these phytochemicals are still in progress and Many new phytochemicals and its derived analogs have been recognized as potential candidates for anticancer therapy among these one of the potent plant is Stevia rebaudiana. The leaves of Stevia rebaudiana tends to possess zero calories, and consists mainly of ent kaurene diterpene glycosides generally recognized as steviol glycosides. Stevioside is the main sweet component found in S. rebaudiana. studies suggest that the stevioside along with v other associated compounds including rebaudioside A, steviol, and isosteviol tends to have therapeutic benefits including anticancer activity. Taking in consideration the above mentioned factors we have investigated the Anticancer potential of extracts of S. rebaudiana. Four extracts was prepared using petroleum ether, chloroform, ethyl acetate and aqueous methanol. T47D cell line have been used to evaluate the anticancer potential using MTT assay. AD-2 that is chloroform extract showing IC50 value of 7.79μg/ml. Moreover IC50 value of AD-4 that is aqueous methanol was also comparatively better and found to be 9.53 μg/ml and AD-1 that is petroleum ether had shown IC50 value of 9.58μg/ml. Thus, various extracts have shown good Antiproliferative activity and S. rebaudiana can be further investigated for its anticancer potential. Furthermore docking study on estrogen receptor–alpha, androgen receptor and aromatase receptor discovered that the phytochemicals of the plant have good binding affinity towards all the three mentioned receptors and can be suitably customized to search its anticancer potential. Moreover unfavorable ADME profile can be overcome by structure modification. Thus on the basis of in-vitro and in-silico data we can conclude that S. rebaudiana extracts have promising anticancer potential. further isolation of compounds have been done successfully and total four compounds have been isolated. two compounds ASP-2 and ASP-4 have been successfully characterized and found to be Stevioside and Rebaudioside A respectively which are already known compounds.Item Coumarin Derivatives as Anticancer Agents for Lung Cancer Therapy: A Review.(Bentham Science, 2018) Kumar, Manvendra; Singla, Ramit; Jandriyal, Jyoti; Jaitak, VikasBackground: 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-κB 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.Item Coumarins as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies(Elsevier Masson SAS, 2015) Thakur, Anuradha; Singla, Ramit; Jaitak, VikasAbstract Coumarins are fused benzene and pyrone ring systems which prompt biological investigation to assess their potential therapeutic significance. It possesses immeasurable anticancer potential with minimum side effects depending on the substitutions on the basic nucleus. Coumarins have a tremendous ability to regulate diverse range of cellular pathways that can be explored for selective anticancer activity. This is the first standalone review that emphasis on the assorted retrosynthetic approaches, important targets for molecularly targeted cancer therapy and structure activity relationship studies that highlight the chemical groups responsible for evoking the anticancer potential of coumarin derivatives reported from 2011 to 2014. ? 2015 Elsevier Masson SAS.Item Design, Synthesis and Evaluation of Indole Based Compounds as Putative Anticancer Agents(Central University of Punjab, 2018) Singla, Ramit; Jaitak, VikasIn the course of efforts to develop new chemotherapeutic agent for targeting breast cancer, indole-benzimidazole, indole-xanthendione, indole-chromene carbonitrile and indole-dihydropyridine derivatives were computationally designed and synthesized. All the compounds were first analyzed for antiproliferative activity using ER-α responsive T47D breast cancer cells line and cytotoxicity using hPBMC. Further, all the synthesized compounds were also evaluated for ER-α binding affinity. Lead compounds 5f and 8f of series 1 and 2; 10e and 10f of series 3, 11c and 12d of series 4 and 5 were found to be most active at both cellular and receptor level hence were biologically evaluated for gene expression studies for targeting ER-α. Cell imaging experiment clearly suggest that compounds were able to cross cell membrane and accumulate thus causing cytotoxicity. Semiquantitative RT-PCR and Western blotting experiments further supported that lead compounds altered the expression of mRNA and protein of ER-α, thereby preventing the further transactivation and signaling pathway in T47D cells line. Structural investigation from induced fit simulation study suggest that lead compounds binds in a conformation similar to bazedoxifene by extensive hydrogen bonding and Van der Waals forces. All these results indicate that compounds 5f, 8f, 10e, 10f, 11c and 12d represents new putative anticancer agents and can be proved promising in the discovery of antiestrogens for the management of breast cancer.Item Drug target strategies in breast cancer treatment: Recent developments(Bentham Science Publishers B.V., 2014) Mayank; Jaitak, Vikas; Mayank, Jaitak, V.Breast cancer (BC) is the leading cause of death among women all over the world. Estrogen receptor (ER) based therapy is one of the major approaches to target BC and is associated with various problems such as primary as well as secondary resistance. ER signaling is a complex pathway as many factors are involved; including several types of ERs and their associated co-regulators. Increasing understanding of ER signals results in new approaches targeting towards BCs. In this context, ER co-regulators have been explored and many modulators of ER co-regulators have been found out. EGFR and mTOR pathways also have significant impact on BC endocrine therapy because of the complex crosstalk mechanism which is responsible for primary and secondary resistance. Triple negative breast cancer (TNBC) is majorly associated with BRCA mutations. Currently there is no approved targeted therapy available in such form of cancer. Although PARP inhibitors seem to be suitable candidates for it. The present review is focused on the current scenario of ER, EGFR, as well as mTOR signaling target therapy. We have also discussed the current status of PARP inhibitors in BC chemotherapy. ? 2014 Bentham Science Publishers.Item Drug Targeting Strategies in Breast Cancer Treatment(Bentham Science, 2014) Mayank; Jaitak, VikasBreast cancer (BC) is the leading cause of death among women all over the world. Estrogen receptor (ER) based therapy is one of the major approaches to target BC and is associated with various problems such as primary as well as secondary resistance. ER signaling is a complex pathway as many factors are involved; including several types of ERs and their associated co-regulators. Increasing understanding of ER signals results in new approaches targeting towards BCs. In this context, ER co-regulators have been explored and many modulators of ER co-regulators have been found out. EGFR and mTOR pathways also have significant impact on BC endocrine therapy because of the complex crosstalk mechanism which is responsible for primary and secondary resistance. Triple negative breast cancer (TNBC) is majorly associated with BRCA mutations. Currently there is no approved targeted therapy available in such form of cancer. Although PARP inhibitors seem to be suitable candidates for it. The present review is focused on the current scenario of ER, EGFR, as well as mTOR signaling target therapy. We have also discussed the current status of PARP inhibitors in BC chemotherapy.Item Effectiveness of Selective Estrogen Receptor Modulators in Breast Cancer Therapy: An Update(Bentham Science Publishers, 2022-10-06T00:00:00) Das, Agnidipta; Lavanya, Kanamarlapudi Joshna; Nandini; Kaur, Kamalpreet; Jaitak, VikasBackground: Breast cancer is considered to be 2nd most common cancer sub-type investigated worldwide. It is mainly prevalent in postmenopausal women. Estrogen Receptor (ER) is a primary transcription factor for the survival and growth of tumors. Around 80% BCs of all classes are ER-positive (ER+). Powerful evidence for estrogen proved to be involved in BC pathogenesis both exogenously and endogenously. It brings the concept of ER inhibitors to treat BC with distinct mechanisms into focus and ER PROTACs (Proteolysis-Targeting Chimeras), AIs (Aromatase inhibitors), SERMs (Selec-tive estrogen receptor modulators), and SERDs (Selective estrogen receptor degrader) were developed. For over 30 years, Tamoxifen, a triphenylethylene SERM, was the drug of choice solely to treat ER+BC patients. Although several SERMs got approval by US FDA after tamoxifen, complicacies remain because of dangerous adverse effects like en-dometrial carcinoma, hot flashes, and VTE (Venous thromboembolism). In addition to that, drug-resistant tumors put a surging need for novel, potent candidates with no or low adverse effects for ER+ BC prevention. Objectives: This article explores the possibilities of SERMs as effective BC agents. Methods: A detailed literature survey of the history and recent advancements of SERMs has been carried out, taking BC as the primary target. This review provides information about ER structure, signaling, pharmacological action, chemical classification with SAR analysis, and benefits and adverse effects of SERMs as potential BC agents. Results: Exhaustive literature studies suggested that SERMs having an agonistic, antago-nistic or mixed activity to ER could efficiently inhibit BC cell proliferation. Conclusion: Each chemical class of SERMs comprises some salient features and poten-tials, which may be further investigated to obtain novel effective SERMs in BC therapy. � 2023 Bentham Science Publishers.Item Engagement of phytoestrogens in breast cancer suppression: Structural classification and mechanistic approach(Elsevier Masson s.r.l., 2020-11-24T00:00:00) Tanwar, Ankur Kumar; Dhiman, Neha; Kumar, Amit; Jaitak, VikasCancer is the world's devastating disease, and breast cancer is the most common reason for the death of women worldwide. Many synthetic drugs and medications are provided with their beneficial actions, but all of these have side effects and resistance problems. Natural remedies are coming forward to overcome the disadvantages of synthetic drugs. Among the natural categories, phytoestrogens having a structural similarity of mammalian oestradiol proves its benefit with various mechanisms not only in the treatment of breast cancer but even to prevent the occurrence of postmenopausal symptoms. Phytoestrogens are plant-derived compounds that were utilized in ancient medications and traditional knowledge for its sex hormone properties. Phytoestrogens exert pleiotropic effects on cellular signalling and show effects on estrogen-dependent diseases. However, because of activation/inhibition of steroid hormonal receptor ER-? or ER-?, these compounds induce or inhibit steroid hormonal (estrogen) action and, therefore, have the potential to disrupt hormone (estrogen) signalling pathway. In this review, we have discussed and summarize the effect of certain phytoestrogens and their possible mechanisms that can substantiate advantageous benefits for the treatment of post-menopausal symptoms as well as for breast cancer. � 2020 Elsevier Masson SASItem Erratum: Chemical Composition and Biological Effects of Artemisia maritima and Artemisia nilagirica Essential Oils from Wild Plants of Western Himalaya (Planta Medica (2014) 80:13 (1079-1087) DOI: 10.1055/s-0034-1382957)(Georg Thieme Verlag, 2014) Stappen, I.; Wanner, J.; Tabanca, N.; Wedge, D.E.; Ali, A.; Khan, I.A.; Kaul, V.K.; Lal, B.; Jaitak, Vikas; Gochev, V.; Girova, T.; Stoyanova, A.; Schmidt, E.; Jirovetz, L.[No abstract available]Item Essential Oils: An Impending Substitute of Synthetic Antimicrobial Agents to Overcome Antimicrobial Resistance(Bentham Science, 2019) Pal, Rajinder; Rana, Abhilash; Jaitak, Vikasntimicrobial resistance (AMR) is an emerging problem in the world that has a significant impact on our society. AMR made conventional drugs futile against microorganisms and diseases untreatable. Plant-derived medicines are considered safe alternatives to synthetic drugs. The active ingredients and the mixtures of these natural medicines have been used for centuries, due to their easy availability, low cost, and negligible side effects. Essential oils (EOs) are the secondary metabolites that are produced by aromatic plants to protect them from microorganisms. However, these EOs and their constituents have shown good fighting potential against drug-resistant pathogens. These oils have been proved extremely effective antimicrobial agents in comparison to antibiotics. Also, the combination of synthetic drugs with EOs or their components improves their efficacy. So, EOs can be established as an alternative to synthetic antimicrobial agents to eradicate tough form of infectious microorganisms. Due to a number of constituents, it can interact with multiple target sites, like the destruction of cytoplasm membrane or inhibition of protein synthesis and efflux pump. The purpose of this review is to provide information about the antimicrobial activity of EOs attained from different plants, their combination with synthetic antimicrobials. In addition, mechanism of antimicrobial activity of several EOs and their constituents was reported.Item Essential Oils: New Perspectives in Human Health and Wellness.(Hindawi, 2014) Firenzuoli, Fabio; Jaitak, Vikas; Horvath, Gyorgyi; Bassole, Imael Henri Nestor; Setzer,William N.; Gori, LuigiEssential oils are natural products, derived from aromatic plants, traditionally used all over the world for disinfection, as anti-inflammatory, relaxing, and stimulating substances, and with potential and modern exploitation in clinical medicine. The earliest recorded mention of the techniques and methods used to produce essential oils is believed to be that of Ibn al-Baitar (1188�1248). The chemical composition of these essential oils varies widely depending upon the geographical location, botanical origin, genetics, bacterial endophytes, and extraction techniques. Essential oils are commonly used in food and cosmetic industries. They can be used as natural alternatives to synthetic preparations to prevent and treat infectious diseases. They are used traditionally to treat other diseases like respiratory tract, digestive system, gynecological, andrological, endocrine, cardiovascular, nervous system, and skin infections. Many of them have shown anticancer activities, too.