Browsing by Author "Garima Tripathi"

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A 12-Crown-4 Ether Containing Dipeptide Boc-12-Crown-4-l-DOPA-Gly-OMe Induces Cell Cycle Arrest and Apoptosis in Rat Eggs Cultured in Vitro
(Springer Netherlands, 2016) Garima Tripathi; Anima Tripathi; Gurunath Ramanathan; Shail K. Chaube
The study was designed to investigate whether crown ether containing dipeptide Boc-12-crown-4-l-DOPA-Gly-OMe has potential to induce meiotic cell cycle arrest and apoptosis in rat eggs cultured in vitro. The immature female rats were subjected to superovulation induction protocol and ovulated eggs were collected from ampulla of the fallopian tube. Ovulated eggs arrested at metaphase-II (M-II) stage of meiotic cell cycle were cultured in media-199 with or without various concentrations (0.0, 0.025, 0.050, 0.10, and 0.20 mM) of dipeptide for 3 h in vitro. Morphological apoptotic changes, hydrogen peroxide (H2O2) concentration, cytochrome c level, caspase-3 level as well as activity and DNA fragmentation were analysed in eggs cultured in vitro. Culture of M-II arrested eggs in plain medium for 3 h in vitro induced meiotic exit from M-II arrest in majority of eggs as evidenced by initiation of extrusion of second polar body (II PB). The dipeptide induced maintenance of M-II arrest and morphological apoptotic features in a concentration-dependent manner prior to degeneration. The dipeptide-induced morphological features were associated with increased H2O2 and cytochrome c levels in treated eggs. The increased cytochrome c induced caspase-3 level and activity and thereby DNA fragmentation as evidenced by DAB positive staining in treated eggs. Our results suggest that dipeptide Boc-12-C-4-l-DOPA-Gly-OMe induces cell cycle arrest at M-II stage and apoptosis in rat eggs cultured in vitro. © 2015 Springer Science+Business Media New York.
Correction: Intervention of Phytochemicals During Endometriosis and Their Conceivable Mechanisms (Revista Brasileira de Farmacognosia, (2023), 33, 6, (1126-1140), 10.1007/s43450-023-00426-2)
(Springer Science and Business Media Deutschland GmbH, 2023) Safiya Ayesha; Alka Sharma; Jayhind Kumar Chauhan; Vivek Pandey; Garima Tripathi; Pawan K. Dubey; Anima Tripathi
The graphical abstract in the original online version of this article was incorrect. It has been corrected. © 2023, The Author(s) under exclusive licence to Sociedade Brasileira de Farmacognosia.
Drug development against tuberculosis: Impact of alkaloids
(Elsevier Masson SAS, 2017) Shardendu K. Mishra; Garima Tripathi; Navneet Kishore; Rakesh K. Singh; Archana Singh; Vinod K. Tiwari
Despite of the advances made in the treatment and management, tuberculosis (TB) still remains one of main public health problem. The contrary effects of first and second-line anti-tuberculosis drugs have generated extended research interest in natural products in the hope of devising new antitubercular leads. Interestingly, plethoras of natural products have been discovered to exhibit activity towards various resistant strains of M. tuberculosis. Extensive applications of alkaloids in the field of therapeutics is well-established and nowday's researches being pursued to develop new potent drugs from natural sources for tuberculosis. Alkaloids are categorized in quite a few groups according to their structures and isolation from both terrestrial and marine sources. These new drugs might be a watershed in the battle against tuberculosis. This review summarizes alkaloids, which were found active against Mycobacteria since last ten years with special attention on the study of structure-activity relationship (SAR) and mode of action with their impact in drug discovery and development against tuberculosis. © 2017 Elsevier Masson SAS
Energy transfer between Er3+:Sm3+codoped TeO2-Li2O glass
(2008) Garima Tripathi; Vineet Kumar Rai; A. Rai; S.B. Rai
The energy transfer in Er3+: Sm3+ codoped binary TeO2-Li2O (TLO) glass has been studied using 532 nm laser radiation on the basis of fluorescence intensity and the lifetime measurements. It is observed that the trace of erbium ion can be utilized to sensitize the samarium. The mechanism involved in the present case is found to be dipole-dipole. The energy transfer efficiencies, probabilities of energy transfer and the average donor acceptor distance has been evaluated. © 2008 Elsevier B.V. All rights reserved.
Energy-efficient Approach to Multicomponent Reaction for the Synthesis of Therapeutically Relevant Heterocycles
(Bentham Science Publishers, 2023) Ritwik Roy; Rahul Kumar; Md. Nurul Ansari; Gauri S. Deshmukh; Animesh Kumar Rai; Garima Tripathi; Abhijeet Kumar
Multi-component reactions have been used as an important synthetic strategy for the synthesis of diverse varieties of therapeutically useful heterocyclic scaffolds. High atom economy, one-pot reaction, and involvement of synthetically simple steps are some of the interesting features that make MCRs greener compared to conventional methods. The development of environmentally benign and eco-friendly synthetic methods has been a very demanding area of research in the past few decades. In particular, the development of energyefficient methods has attracted the attention of the research community due to heavy dependence on non-renewable energy resources, which is depleting fast. Therefore, the present review has highlighted the multi-component reactions developed under the energy efficient protocol, which mainly include the reactions developed under the microwave, ultra-sonication, mechanochemical, and photochemical reaction conditions for the synthesis of therapeutically relevant heterocycles. © 2023 Bentham Science Publishers.
Enhancement of upconverted luminescence in Er3+: Te O2 glass on increasing the temperature and concentration of Yb3+ beyond the critical limit
(2007) Anant Kumar Singh; Garima Tripathi; S.B. Rai; Anita Rai
Enhancement of upconverted luminescence in Er3+ Yb3+: Te O2 has been observed with increase in the concentration of Yb3+ on excitation with 780 nm laser radiation. It is further noted that the upconversion is increased even above the quenching limit on increasing the temperature of the glass. The incident radiation excites Yb3+ indirectly via Er3+ resulting in a strong blue emission from Yb3+ and green and red emissions from Er3+. The UV emission from Er3+ at 380 nm involves three near infrared photons when there is no Yb3+ in the glass but when Yb3+ is also present, this behaves as a two photon process. The lifetime of the S 32 4 level of Er3+ in glasses containing only Er3+ and also those containing both Er3+ and Yb3+ has also been measured in different conditions. © 2007 American Institute of Physics.
Flavonoids and their Conjugates: Potential Molecules for Therapeutics
(Bentham Science Publishers, 2025) Prerna Kumari; Anuradha Ambasta; Pradeep Harish Kumar; Sindhumani; Abhijeet Kumar; Garima Tripathi
Plants can produce a wide range of bioactive compounds. High concentrations of phytochemicals prevent the accumulation of free radical damage in fruits and vegetables. Flavonoids a group of natural products with different phenolic structures are found in fruits, vegetables, grains, bark, roots, stems, flowers, tea, and wine. These natural products are known for their health benefits, and thus efforts are being made to isolate these flavonoids. Flavonoids are now recognised as important components of many nutraceutical, medical, pharmaceutical, and cosmetic products. This is attributed to their antioxidant, anti-inflammatory, anti-mutagenic, and anti-cancer properties and their ability to alter the activity of important cellular enzymes. Information about how flavonoids work is still not fully understood. However, it has been widely known that plant-derived derivatives have had many biological activities for centuries. Current flavonoid research and development trends include the isolation, identification, characterisation, and activity of flavonoids and their potential health benefits. Bioinformatics information is also used to estimate economic potential and productivity. This article discusses current research, mechanisms of action, functions, and uses of flavonoids, predictions of flavonoids as potential anti-inflammatory agents, and future recommendations. Due to the antioxidant, anti-proliferative, anti-tumour, anti-microbial, estrogenic, acetylcholinesterase, and anti-inflammatory activities of flavonoids they are also used as therapeutics in cancer, cardiovascular diseases, neurodegenerative diseases, and other diseases. It also covers the mechanism of action of flavonoids, which highlights the role of flavonoids as kinase inhibitors and their effect on membrane-bound receptors. Tyrosinase is involved in several human pigmentation-related diseases, among which hyperpigmentation can be treated by using flavonoid-based drugs as tyrosinase inhibitors. This review will provide researchers in the discipline of medicinal chemistry with the opportunity to develop options, improve quality, and use various flavonoid derivatives and their conjugates as therapeutics and in the treatment of various diseases. © 2025 Bentham Science Publishers
Green Chemistry: Introduction, Application and Scope
(Springer Nature, 2022) Vinod K. Tiwari; Abhijeet Kumar; Sanchayita Rajkhowa; Garima Tripathi; Anil Kumar Singh
This book summarizes fundamentals and advanced topics of green chemistry and highlights the importance and impact of green chemistry over traditional synthetic methods. It discusses about the importance and scope of the catalytic protocols in green chemistry and their application in daily life. Alternate green energy approaches discussed in this book underline the importance of efficiency enhancement with simultaneous energy demand reduction by replacing the dependence on non-renewable energy resources. Various topics covered in this book include green solvents, energy-efficient approach for organic synthesis, catalysis, biocatalysis, and green approach in pharmaceutically important molecules and drugs. The book will be a valuable reference for beginners, researchers, and professionals interested in sustainable green chemistry and their scope in allied fields. © The Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd. 2022.
Intervention of Phytochemicals During Endometriosis and Their Conceivable Mechanisms
(Springer Science and Business Media Deutschland GmbH, 2023) Safiya Ayesha; Alka Sharma; Jayhind Kumar Chauhan; Vivek Pandey; Garima Tripathi; Pawan K. Dubey; Anima Tripathi
Endometriosis is a chronic and complex endocrine disorder that affects women of reproductive age. This syndrome is benign and is characterized by a combination of ovarian dysfunction and estrogen dependency symptoms, as well as pain and infertility. The most commonly stated symptoms include dysmenorrhea, significant dyspareunia, dyschezia, and dysuria. It is a severe public health issue. The prevalence rate is quite high and continues to rise on a daily basis. Starting with its diagnosis, pathophysiology, repercussions, and treatment options, there are numerous areas of disagreement. This study aims to provide an overview of the development of endometriosis diagnosis, symptoms, risk factors, etiology, medicinal plants, phytochemicals, and treatment, with a focus on research and the creation of novel therapeutic strategies. We conclude by making predictions and recommendations for the future of endometriosis-related research and prospective therapy approaches. Graphical Abstract: [Figure not available: see fulltext.] © 2023, The Author(s) under exclusive licence to Sociedade Brasileira de Farmacognosia.
Novel 3,4-diarylpyrazole as prospective anti-cancerous agents
(Elsevier Ltd, 2020) Vivek Pandey; Garima Tripathi; Dhruv Kumar; Abhijeet Kumar; Pawan K. Dubey
Cancer is a leading cause of death globally. Despite therapeutic advancements the mortality rate of cancer is continuously increasing. Thus, it is important to identify and design potential therapeutic agents which can specifically bind with most common targets of cancer and inhibit tumor progression. The present work discloses the potential therapeutic application of the novel 3,4-diaryl 1H-pyrazoles as prospective anti-cancerous agent. The in silico molecular docking studies performed with 3,4-disubstituted pyrazoles as ligand with targets including DNA, BCL-2 and F1-ATP Synthase revealed strong binding affinity with DNA (-7.5 kcal/mol), BCL-2 (-8.1 kcal/mol) and F1-ATP Synthase (-7.2 kcal/mol). Furthermore, the in silico finding was validated with the in vitro cytotoxicity assay with human breast cancer cell line (MDA-MB-231). MDA-MB-231 cells treated with 3,4-diarylpyrazole resulted in an increase in annexin-V positive cells, production of reactive oxygen species (ROS), dissipation of the mitochondrial membrane potential and activation of caspase-3. Taken together, this study demonstrate that a novel synthesized 3,4-diarylpyrazoles, showed strong binding affinity against DNA, anti-proliferative activity and executed apoptosis through ROS-dependent caspase-3-mediated mitochondrial intrinsic apoptotic pathway against MDA-MB-231 cells. These findings increase our understanding of the molecular mechanism (s) by which 3,4-diarylpyrazoles can exert their anticancer activity and may contribute towards development of novel therapeutic agent against breast cancer. © 2020 The Author(s); Pyrazole; Molecular docking; Apoptosis; Reactive oxygen species; MDA-MB-231; Chemistry; Organic chemistry; Pharmaceutical chemistry; Biological sciences; Cell biology; Bioinformatics © 2020 The Author(s)
Solvent-free Approaches towards the Synthesis of Therapeutically Important Heterocycles
(Bentham Science Publishers, 2024) Ambarish Priyadarshan; Garima Tripathi; Anil Kumar Singh; Sanchayita Rajkhowa; Abhijeet Kumar; Vinod Kumar Tiwari
The development of synthetic methodologies to obtain a diverse range of heterocyclic scaffolds has been a very attractive area of research due to their vast therapeutic importance. Conventional approaches that require the use of organic solvents, which are generally flammable, toxic, and not eco-friendly, are replaced either with greener alternatives or by completely avoiding their use. In literature, several solvent-free methods have already been reported for the synthesis of vast varieties of organic compounds. This review focuses on the solvent-free methods developed for the synthesis of different types of nitrogen and oxygen heterocycles which have exhibited diverse therapeutic applications. © 2024 Bentham Science Publishers.
Spectroscopic studies of Eu3+ doped calibo glass: Effect of the addition of barium carbonate, energy transfer in the presence of Sm3+
(2006) Garima Tripathi; Vineet Kumar Rai; S.B. Rai
Optical properties of Eu3+ doped calibo glass has been studied in presence and absence of BaO and their dependence on BaO concentration explored. It is found that the fluorescence intensity increases and approaches maximum for 10% of BaO content but get quenched for higher concentrations. The energy transfer between two asimilar rare earth ions (Sm3+:Eu3+) doped in calibo glass has been verified on the basis of changes in fluorescence yield. © 2006 Elsevier B.V. All rights reserved.
Spectroscopy and upconversion of Dy3+ doped in sodium zinc phosphate glass
(2005) Garima Tripathi; Vineet Kumar Rai; S.B. Rai
Optical absorption and fluorescence spectra of Dy3+ doped in sodium zinc phosphate glasses have been reported. Judd-Ofelt theory has been applied to analyze the spectra and determine the optical parameters such as transition probabilities, radiative lifetime, stimulated emission cross-section, etc. The fluorescence intensity of Dy3+ corresponding to 4F9/2 → 6H13/2 transition increases with increasing concentration of Dy3+ but at higher concentrations, concentration quenching is observed. The radiative lifetime of the 4F9/2 level at 1 mol% concentration of Dy3+ in this host is found to be 541 μs. Emission corresponding to 4F9/2 → 6H13/2 transition (570 nm) is observed on excitation with NIR radiation due to upconversion. An attempt is made to explain this observation. © 2005 Elsevier B.V. All rights reserved.
Synthesis of biologically relevant heterocyclic skeletons under solvent-free condition
(Elsevier, 2021) Garima Tripathi; Abhijeet Kumar; Sanchayita Rajkhowa; Vinod K. Tiwari
Heterocyclic compounds play an important role in drug discovery and development and therefore tremendous efforts have been made to develop convenient and green routes for their high yielding synthesis. In view of high impact of toxic organic solvents on health, environment, safety, and moreover, the overall cost of desired products, this chapter exclusively emphasizes on the solvent-free synthetic methodologies employed for the generation of heterocyclic skeletons of promising pharmacological importance. It mainly includes the synthesis of nitrogen and oxygen containing heterocycles as they represent a major proportion of the bioactive heterocyclic compounds as well as marketed drugs. © 2021 Elsevier Inc. All rights reserved.
Synthesis, crystallographic study, in silico and in vitro investigation of novel flavonol-amino acid conjugate as an anti-proliferative agent
(Elsevier B.V., 2025) Prerna Kumari; Pradeep Harish Kumar; Rakesh Kumar Gupta; Anima Tripathi; Pawan Kumar Dubey; Anuradha Ambasta; Jayhind Kumar Chauhan; Joydeb Goura; Abhijeet Kumar; Garima Tripathi
In this article, a flavonol-Aib conjugate; {(4-oxo-2-phenyl-4-H-chromen-3-yl-2-((start-butoxy-carbonyl) amino)-2-methyl-propanoate) (3A)} has been synthesized, purified and characterized through 1H and 13C NMR, mass spectrometry and X-ray crystallography. X-ray crystallography of these molecules revealed that this is a flavonol-Aib conjugate; there is no intramolecular hydrogen bond, while two intermolecular H-bonds occur between two molecules of flavonol-Aib conjugate, between O2 of C=O (flavonol ring) and H1 (Aib NH) is 2.183Å. This intermolecular interaction generates a stacked two-dimensional (2-D) structure. There are weak interactions between H3 of the flavonol-benzene ring and H18B of the tertiary Butyl-CH3 is 2.804Å., and the same H3 interaction with other molecules' H14 of phenyl of substituted flavonol is 2.332Å. The distance between O2 of C=O (flavonol ring) and H11 (other phenyl-substituted flavonol rings) is 2.610Å, giving a specific molecular conformation. A complete molecular structure investigation of the molecule shows that several inter- and intramolecular weak to strong interactions lead to a peculiar array of molecules in two and three dimensions. In silico studies, molecular docking via Auto doc vina reveals that flavonol with 2-aminoisobutyric acid conjugate, among conjugates of different amino acids (glycine, alanine, valine, leucine, Isoleucine), Aib conjugate shows highest binding affinity with CDC42 (-7.7), BCL2L1 (-8.9), GSK3B (-6.8), MAPK1 (-8.8), PPARG (-7.4), ICAM1 (-7.8), MMP9 (8.0), BCL2 (-8.9), ERBB2 (-9,0), HSP90A1 (9.5) gene. The result of in vitro studies exhibits remarkable inhibitory ability with IC50 values of 400 µg/ml. The overall outcome indicates that flavonol conjugated with 2-aminoisobutyric acid (Aib) can inhibit the growth of the MCF-7 cancer cell line by targeting multiple biological pathways. © 2025
THPM (1,2,3,4-Tetrahydro pyrimidine) and Berberine Exhibit Synergistic Impact on Inhibition of Cell Migration and Colonization Through ROS-Mediated Apoptotic Pathways in the Breast Cancer Cells
(John Wiley and Sons Inc, 2025) Rakesh Kumar Gupta; Ambarish Priyadarshan; Sonal Tiwari; Yashvant Patel; Arun K. Bind; Garima Tripathi; Anima Tripathi; Abhijeet Kumar; Pawan Kumar Dubey
Breast cancer is one of the major causes of death in females worldwide. Considering the polypharmacological trend, small molecules like pyrimidine along with berberine, a bioactive anticancer agent may act as effective anticancer drugs having multiple targets with minimal side effects. However, it has never been tested. The present work discloses the efficacy of the combination of 1,2,3,4,-Tetrahydro pyrimidine (THPM) and Berberine (BBR) in inhibiting cancer progression in human breast cancer cell line, i.e., MCF-7. THPM were synthesized and characterized, and their anti-cancerous potential was evaluated by in silico study. The MCF-7 cells were exposed in vitro with THPM (200 µM), BBR (20 µM/ml) alone or in combination of THPM + BBR (200 µm + 20 µm/ml) for 24 h. Intracellular ROS, annexin-V staining, cell migration, colony formation assay, and gene expression analysis were performed. THPM and BBR both exhibited solid binding affinity against the BCL-2 protein. Interestingly, co-treatment of THPM + BBR significantly increased ROS level, annexin-V positive cells, the expression level of Bax, and Caspase-3 and inhibited migration and proliferation of MCF-7 cells. In conclusion, co-treatment of THPM + BBR exhibits a synergistic impact via inhibiting cell proliferation and inducing ROS-mediated apoptosis in MCF-7 cells suggesting that THPM and BBR could be used as novel therapeutic agents against breast cancer. © 2025 Wiley-VCH GmbH.
Transition-Metal Free Arylation of Therapeutically Important Heterocycles
(John Wiley and Sons Inc, 2024) Ambarish Priyadarshan; Garima Tripathi; Naresh Murty Venneti; Kaushal Kishor; Anil Kumar Singh; Abhijeet Kumar
The transition-metal-free synthesis of organic compounds especially heterocycles is in resonance with one of the twelve principles proposed by Prof. Paul Anastas in his renowned work towards the sustainable development of green chemistry. Traditional-metal-catalyzed reactions often involve expensive or toxic metal catalysts, and there is a growing interest in developing more sustainable and environmentally friendly methods. The arylation of heterocycles is an important area of research in organic chemistry, particularly in the synthesis of biologically active compounds and pharmaceuticals. Arylation of heterocycles at different positions enhances the potency and stability of biologically and pharmaceutically important scaffolds. In this review, an overview of the synthetic protocols developed for the arylation of a variety of heterocyclic compounds including, pyrroles, pyridines, thiophene, indole, oxindoles, purines, xanthene, etc. has been described. © 2024 Wiley-VCH GmbH.
Upconversion and temperature sensing behavior of Er3+ doped Bi2O3-Li2O-BaO-PbO tertiary glass
(Elsevier, 2007) Garima Tripathi; Vineet Kumar Rai; S.B. Rai
Spectroscopic properties of Er3+ doped bismuth glass has been reported on the basis of J-O theory. The upconversions observed due to energy transfer in Er3+ doped bismuth glass have been studied and explained. The effect of temperature on the luminescence intensity of the bands has been monitored and it is inferred that these may be used to sense the temperature with appreciable sensitivity. The nephalauxetic effect, covalency and bonding parameters for Er3+ in the present glass have been determined. © 2006 Elsevier B.V. All rights reserved.
Upconversion in Er3+-doped Bi2O3-Li2O-BaO-PbO tertiary glass
(2007) Garima Tripathi; Vineet Kumar Rai; D.K. Rai; S.B. Rai
Radiative properties of Er3+-doped tertiary bismuth glass has been analyzed by the Judd-Ofelt theory. NIR to visible upconversion in the Er3+-doped glass has been reported. The mechanism for the upconversion is explained on the basis of quadratic dependence on excitation power and on the energy-matching scheme. Energy transfer is noted as the dominant process including the long-lived 4I11/2 level as the intermediate state for the green and red upconversion emissions. The effect of temperature on the fluorescence intensity of the two bands due to 2H11/2 → 4I15/2 and 4S3/2 → 4I15/2 transitions as well as on the transitions due to Stark components of the 4S3/2 level have been monitored and it is concluded that their intensity ratio may serve as better temperature sensing device. © 2006 Elsevier B.V. All rights reserved.