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Current Indian Science - Current Issue
Volume 1, Issue 1, 2023
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Phytochemical and Pharmacological Aspects of Hygrophila Spinosa: An Overview
Authors: Smruti Gaikwad, Lata Kothapalli and Asha ThomasBackgroundA plant from the Acanthaceae family, Hygrophila spinosa T. Ander is geographically distributed throughout Asia and is noted for its diuretic and aphrodisiac properties in Ayurvedic literature. In the last four decades, various research teams have conducted experiments with the plant Hygrophila spinosa to screen the plant for hepatoprotective, anti-urolithiasis, diuretic, anti-hypertensive, anti-diabetic, chemoprotective, and anticancer activities along with analgesic and anti-inflammatory activity. Flavonoids, alkaloids, steroids, and triterpenoids are among the phytochemicals separated from different plant components, along with vitamins and minerals.
ObjectiveConsidering the therapeutic value of the plant, focus on using current technology to quantify and confirm the pharmacological effects with in vitro and in vivo assays was felt and to shed light on in silico investigations.
ResultsRelevant analytical tools for characterizing and quantifying phytoconstituents in the plant, along with emphasis on well-established pharmacological screening experiments on parts and whole plant extracts, commercially available formulations of H.spinosa have been elaborated. It has been discussed how to further validate the pharmacological effects using in silico methods and predictions from ADME/T analyses. H. spinosa based Phyto fabricated nanoparticle systems with gold and silver have broadened the use of plant extract as a metal. carrier which minimizesmetal. toxicity to further boost its synergistic effects in response to the growing need for targeted medicine delivery systems.
ConclusiónIn light of the necessity to investigate a specific mechanism of action for each of the specific phytoconstituents contained in the plant, the present review summarizes the phytochemical and pharmacological importance of the plant in chronic illness.
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Advancement of Nanocarriers-based Therapeutics for Effective Management of Colorectal Cancer
BackgroundColorectal cancer is still challenging for scientists and healthcare professionals. Conventional treatment methods are associated with various limitations at a clinical bed and patient’s compliance. Novel nanocarrier based approaches opened a new window for improved therapy and new future perspective.
IntroductionCancer is the deadliest disease globally and is challenging to healthcare systems. Colorectal cancer (CRC) is the third most common cancer in the world, affecting all age groups and the most common cancer in 23 countries, as per the World Health Organization (WHO).
MethodsIn this review, we addressed nanocarriers based strategic treatment of colorectal cancer, major findings, limitations, and future perspective. For this, we seriously reviewed literature downloaded from prime sources such as Google Scholar, Web of Science, PubMed, and Publon. To filter the exact need of data, we used keyword alone in combination. Various relevant articles were obtained from the reference section of the selected papers.
Results and DiscussionIt is necessary to have an effective and targeted treatment option to control CRC compared to available remedies. Nanotechnology has been widely used to diagnose and treat several cancer types. Advances in nanomedicine and phytonanomedicine promoted novel identification methods to treat colorectal cancer patients. There are several nanocarriers recommended for clinical purposes. However, to date, only a few clinically approved nanocarriers can load anticancer moieties and selectively bind to cancer cells. Some nanocarriers transport and release treatments to the target colorectal area but provide few benefits.
ConclusionIn this review, various nanoparticles (NPs) with unique properties have been discussed in relation to managing colorectal cancer, major outcomes of clinical trials, and successful patents published so far.
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Evaluation of Wound Healing Activity of Statin Impregnated Collagen Scaffold in Wistar Albino Rats
Authors: Talasila Gopala Krishna Murthy and Bodepudi Sudheer ChowdaryBackgroundWound healing is a dynamic process that is affected by various processes. Medications involved in wound healing can interfere with clot formation, inflammation reduction, and cell proliferation. Collagen is the natural existing compound that has the ability to enhance tissue regeneration. Various drugs used for healing have cons like inhibiting DNA, RNA, or protein synthesis, resulting in decreased fibroplasias and neovascularisation of wounds.
ObjectiveThe objective of this work is the formulation of the collagen scaffold impregnated with the Atorvastain using cow urine as solvent.
MethodsThe methodology involves the isolation of the collagen from the bones of the animals by using acetic acid. The obtained collagen was subjected to homogenization and sonification to get a fine powder. To this solvent, Atorvastatin and glycerine were added then it was dried at 60°C for 24 hrs to get the impregnated scaffold. The formulated scaffold was evaluated for wound healing activity by using the excision wound model.
ResultsThe result shows that the scaffolds are good in nature and meet all the standards of the standard scaffold. The wound healing activity is assessed by using the excision wound healing model in rats. The results show the significant value of 99% wound healing activity from the statin-impregnated scaffold. The biological parameters like total collagen, hexosamine, and uronic acid were evaluated and these observations indicated higher values of 4.024 ± 0.069, 304 ± 4.11, and 75.83 ± 1.93 compared with the plain scaffold.
ConclusionThe optimised formulation exhibited good mechanical strength with better wound healing activity. The percent wound healing activity and antimicrobial activity observed from the collagen scaffold was found to be more significant compared with the scaffolds not containing statins.
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A Parametric View of Hubble Parameter for Scalar Field Dark Energy Model
Authors: Sangita Goswami and Sudipta DasPurpose of the studyIn our present work, we have considered a simple parametric form of the Hubble parameter (H) for a canonical scalar field model described within a spatially flat FRW spacetime framework. Here we have considered a well-behaved parametrization scheme of the normalized Hubble parameter to explain the expansion history of the universe.
MethodsUnder this scenario, we have obtained the analytic solutions for various relevant cosmological parameters. We have also reconstructed the potential function V(φ) for the scalar field φ.
ResultsIt has been found that the deceleration parameter (q) shows exactly the nature which is well expected, i.e., an accelerated expansion for low z limit and deceleration for high z limit, which is essential for the structure formation of the Universe. Detailed data analysis has been carried out to check the viability of the proposed theoretical model by using combined dataset SNIa+H(z)+BAO/CMB and put constraints on the cosmological parameters, viz. the present value of the Hubble parameter H0.
ConclusionAs it has been observed that the deceleration parameter undergoes a smooth transition from an accelerating phase to decelerating expansion, this result supports the structure formation at the early time and the late time cosmic acceleration measurements. The results are found to be closer to the value obtained by the PLANCK collaboration.
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Investigation of Developmental Toxicity Profile of Edible Lablab (Lablab purpureus (l.) Sweet Purpurea) bean Extract using Brine Shrimp and Zebrafish
BackgroundDevelopmental toxicology deals with the effects of compounds on fertility and with birth defects that could occur at any stage of the reproductive cycle. In this study, we evaluated the teratogenic effects of Lablab purpureus (L.) Sweet beans on zebrafish embryo.
ObjectivesThe developmental toxicity study was carried out to evaluate the toxicity induced by Lablab purpureus (L.) Sweet beans on zebrafish embryo. We also studied the cytotoxicity of Lablab purpureus (L.) Sweet beans.
MethodsZebrafish embryos were exposed to a methanolic extract of Lablab purpureus (L.) Sweet beans at concentrations of 10,25,50, and 100 μg/ml starting from 24 hours post fertilization (HPF) to 72 HPF. Developmental defects, if any, were observed under a microscope. Cytotoxicity of Lablab purpureus (L.) Sweet beans were also evaluated by using brine shrimp and the corresponding LC50 value of the methanolic extract of Lablab purpureus (L.) Sweet beans were also calculated.
ResultsThe LC50 value of the methanolic extract of Lablab purpureus (L.) Sweet beans were found to be 77 μg/ml. However, some forms of developmental toxicity were observed in zebrafish embryos when treated with different concentrations of Lablab purpureus (L.) Sweet beans extract.
ConclusionThe methanolic extract of Lablab purpureus (L.) Sweet beans were found to be cytotoxic in brine shrimp, and the LC50 value was found to be 77 μg/ml. However, there was some level of developmental toxicity in the Zebrafish embryo model at different concentrations of Lablab purpureus (L.) Sweet beans extract.
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The Activity of Several Medicinal Herbs such as Anti-inflammatories, Anti-Pyretic, Analgesics and Antioxidants
Authors: Neha Dangi, Shikha Sharma, Praveen Goyal and Jeyabalan GovindasamyBackgroundPeople have been using different plants to treat a wide variety of illnesses ever since the dawn of human civilisation, medicinal plants have been employed. According to the World Health Organization, approximately 80% of people living in developing countries lack the financial means to purchase synthetic drugs. As a result, these individuals turn to traditional medicines, the majority of which are derived from plants, to satisfy their fundamental requirements for health care. Plants have been used as medicine from the beginning of time to cure a broad variety of ailments, including gastrointestinal disorders, genitourinary problems, hepatobiliary discomfort, as well as psychiatric and respiratory issues.
MethodsIn order to get the necessary data, the procedure involves scouring multiple search engines, such as PubMed, ScienceDirect, and Sci Finder, for citations that pertain to the topic at hand. Regarding anti-inflammatories, anti-pyretic, analgesics, and antioxidants.
ResultsFor a considerable amount of time, many different plants have been used as a treatment for fever, and recent scientific research has demonstrated that these treatments reduce the temperature of the human body. The significance of medicinal plants as a kind of treatment for fever is brought into sharp focus by this analysis.
ConclusionThis review can also assist researchers and scientists in locating new antioxidants, antipyretic compounds, and plants that have been utilized for a considerable amount of time.
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Regulation of Genome-edited Technologies: Indian Policy Perspective
Authors: Amita Prasad and Murali Krishna ChimataThe rapid technological advances in the field of biotechnology have resulted in the formulation of effective and robust regulatory policy frameworks by different countries to ensure the safety of the products that are being developed through the application of genome editing techniques both in terms of environment and health safety perspectives. With over two and half decades of use of products derived from the application of genetic engineering technologies, this technology has stemmed the emergence of an even more advanced and precise targeted technology to address the most complicated and intrinsic challenges in a more precise manner which is now considered as Genome Editing. It is astounding to note that, at a time when several nations were debating and discussing the regulatory hurdles regarding the regulation of this technology, India has emerged as one nation with a clear policy framework with well-defined definitions in Rules 1989 itself, wherein, the definition of Gene Technology and Genetic Engineering clearly states that any alteration in the genome needs to be regulated and accordingly, India needs to regulate the products that would be developed through this novel genome editing technology. However, recognizing the global developments and after a thorough assessment of safety aspects, India, in the year 2022 promulgated the “ Guidelines for the Safety Assessment of Genome Edited Plants” wherein, it is explicitly detailed that products that are derived from SDN-1 and SDN-2 techniques and which are free of exogenous introduced DNA, are exempted from the provisions of Rules 7 to 11 (both inclusive) of the above said Rules 1989 and products derived from SDN-3 would be regulated as per provisions of Rules, 1989. If required, the concerned regulatory agencies may stipulate additional safety evaluation tests through better risk evaluation methodologies and a greater number of laboratories could also be set up along with empowering the human resource capacities for undertaking such state-of-the-art and precise techniques for the development of safe and beneficial products for the public without compromising on the safety.
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Decoding Artificial Intelligence in Neuroscience: Applications Beyond Diagnosis
Authors: Sagar Salave, Dhwani Rana, Derajram Benival and Aakanchha JainBackgroundArtificial Intelligence has witnessed exponential expansion in health care applications. The article pronounces the dynamic excellence AI is achieving in the healthcare discipline of neuroscience.
ObjectiveThe paper highlights basic concepts of AI and acmes the interdisciplinary collaboration of Computational neuroscience, Cognitive science, and AI. Also, the article draws out important findings related to AI in neuroscience amongst its diverse application in the various disciplines. An ephemeral overview of applications of AI-based constructs in neurological disorders namely Neuroinflammation, Schizophrenia, Parkinson’s disease, Epilepsy, Autism spectrum disorder, Alzheimer’s disease, Brain tumor and Anesthesiology has been demonstrated in the present work.
MethodsThe method includes the collection of data from different search engines like google Scholar, PubMed, ScienceDirect, SciFinder, etc. to get coverage of relevant literature for accumulating appropriate information regarding AI, neuroscience, and their linkages.
ResultsThese considerations are made to expand the existing literature on the progressing role of AI in the management of neurological disorders.
ConclusionThe exponential expansion in the development of AI-based systems might aid in addressing the prevailing limitations in the domain of neurological disorders and neuroscience.
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Traditional Ayurvedic Treatment Practices by Vaidyas of the Northern Region of India
Authors: Mishra Bhawana and Pant DeepakAims:The present study aims to investigate the current scenario of utilization and importance of medicinal plants used by traditional Vaidyas. This study also provides information about the views and awareness of the current generation towards ayurvedic knowledge, which in turn explains the decline of traditional healthcare practices.
Background:Ayurvedic medicine is one of the oldest and most traditional healthcare systems in India. There is limited documentation available regarding the information of traditional medicinal uses of plants even though various rural folks and elders have long been using plant-based formulations for curing human ailments. Hence, there is an urgent need to document this traditional knowledge to endorse the Ayurveda or Indigenous medicinal system before such valuable knowledge becomes inaccessible and extinct.
Objective:The present study was carried out to profile the current status of medicinal plants used by Traditional Vaidya’s/practitioners/locals, and discuss the status of Ayurveda and indigenous systems in the Northern states of India i.e., Haryana and Rajasthan.
Methods:To study currently available medicinal plants used by traditional Vaidyas in Northern states of India such as Haryana and Rajasthan, a survey among 50 Vaidyas of each state was undertaken. Information was gathered through interview and questionnaires consisting of 20 questions regarding their knowledge, expertise, targeted ailments, herbal formulations, and preservation techniques.
Results:According to the collected information, these Vaidyas have almost 4 to 40 yrs. of experience and acquired their knowledge in a variety of ways, including from academic institutions or their ancestors. By feeling the pulse in the wrist, these Vaidyas were able to diagnose ailments associated with the three doshas (Vata, Pitta, and Kapha) with medical precision via sensing the wrist's pulse. Different illnesses associated with kidney, lungs, digestive system, leukosis, diabetes, blood pressure etc. were treated by these traditional Vaidyas. In addition to prescribing medicines, Vaidyas carefully observe the patient's routine, physical health and their age group for better medication. Several indigenous medicinal herbs such as Ashwagandha, safed musli, gokhru, garmunda, bawli ghans, giloy, triphala, ginger, patthar chatta, Aloe vera, Stevia, and many other herbs are being used by these traditional Vaidyas for their herbal formulations.
Conclusion:This survey highlights Ayurveda and its use of plants in the field of medicine, through validation based on knowledge of traditional Vaidyas. This article also highlights the indigenous system and some important Indian medicinal plants of Haryana and Rajasthan and their therapeutic use in daily life. This survey enlightens the traditional Vaidyas and their knowledge of the Ayurveda medicinal system. This step might strengthen the validity of these products and provide a lead to target new formulation preparations. Many high-profile formulations could be prepared in the future, if most of these reputed traditional Vaidyas get organized.
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Discovering the Potential of Plants in Wound Healing: A Mechanistic Review
Authors: Ishan Durvasha, Mehak Sharma and Shweta AgarwalPlants are admired for their taste, fragrance, and therapeutic characteristics. Herbs are used in multiple traditions, including cooking, medicine, and spirituality. Medicinal plants have been used to treat a number of illnesses and disorders from ancient times to the present day. The main reason for this is that therapeutic plants have no negative side effects. With a diverse spectrum of plant species and widespread access to traditional medical practices, India is one of the world's largest biodiversity reservoirs. According to WHO data and other relevant sources, herbal medicinal products are used by more than 80% of the world's population. The goal of this review article is to describe the importance of herbal agents in therapeutics, such as the use of crude plant extract for the medicinal purpose. Complex interaction of blood cells, tissues, soluble mediators, cytokines, and numerous growth factors is required for wound healing, whether it is accidental or surgical. Plants have enormous potential for wound management and therapy, as well as regeneration of damaged tissues, due to the presence of a variety of useful active phytoconstituents. This review presents comprehensive data on some important plants and their extracts used in wound healing along with their mechanism of action and the scientific research reported on these plants.
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Bioactive Furanocoumarin 'Alloimperatorin': Therapeutic Importance and Pharmacological Activities in Medicine
More LessBackgroundPlants and their derived phytochemicals commonly called secondary metabolites have been used in medicine as a good source of medicine for the treatment of numerous kinds of human disorders and associated complications. Herbal medicines have been used in modern medicine for the treatment of some chronic disorders, including cancer. Coumarins class phytochemicals are important in medicine and mainly derived from plant sources, including Angiosperms. Coumarins have numerous biological activities including antimicrobial, antibacterial, antifungal, antioxidant, antitumor, anti-HIV, antihypertension, anticoagulant, anticancer, antiviral, anti-inflammatory, analgesics, antidiabetic, and anti-depressive.
MethodsHere in the present work, numerous scientific data were collected from different scientific databases and analyzed in order to know the biological potential of alloimperatorin in medicine. Google, Google Scholar, PubMed, and Scopus databases were searched and analyzed to know the medicinal properties and therapeutic potential of alloimperatorin. Therapeutic potential of alloimperatorin was investigated in the present work through scientific data analysis of different scientific research work. Pharmacological activities of alloimperatorin were analyzed in the present work to know the beneficial health aspects of alloimperatorin against various forms of human disorders.
ResultsScientific data analysis of different research work revealed the therapeutic potential of alloimperatorin in medicine. Alloimperatorin is a coumarin class phytochemical found in the Angelica dahurica. Alloimperatorin revealed significant therapeutic potential in medicine mainly due to its anti-oxidative, anti-inflammatory, anti-apoptotic potential, however its biological potential in breast cancer and their photosensitization effect were also discussed in the present work. Analytical data signified the presence of alloimperatorin in different medicinal plants.
ConclusionPresent work signified the biological importance and therapeutic potential of alloimperatorin in medicine.
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Extraction Fuel During Hydro-distillation Modifies Eucalyptus Essential Oil Yield, Phytochemical Quality, and Capital Cost
Authors: Arun Dev Sharma and Inderjeet KaurIntroductionPlant-based essential oils are usually extracted using the hydro-distillation process. During this process type of fuel is a major factor that regulates yield, aromatic quality, and capital cost. AIM: This study aimed to examine the distillation of eucalyptus essential oil using Fire word (FW), Liquefied Petroleum Gas (LPG), and Electric Filament (EF) derived energy as fuels. Eucalyptus fresh leaves were used to extract the essential oil.
MethodsSeveral parameters were examined, including the yield of oil, total phenolic content and total antioxidant activity, and total capital cost of each procedure. The results revealed that EF-based hydro-distillation reduced the cost of essential oil production many times compared to FW and LPG-based fuels.
ResultsUsing EF, essential oil quality also increased considerably in terms of total phenolic content (1.49 mg GAE/ml) and total antioxidant activity (4.2 mg AE/ml). GC-FID analysis discovered the occurrence of 1,8 cineole as a major component in eucalyptus essential oil.
ConclusionTo conclude, EF-based fuel offers significant advantages over traditionally used fuels to hydro-distill eucalyptus essential oil in cosmetic and pharma-based industries.
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Phytochemical, Medicinal, and Green Approaches of Allamanda cathartica L.: A Mini Review
Authors: Acharya Balkrishna, Akansha Saini, Rachna Bhandari, Vedpriya Arya and Ishwar Prakash SharmaAllamanda cathartica L. belongs to the family Apocynaceae and is a traditionally valuable medicinal plant that has been commonly used in the traditional medicinal system and contributes to the native healthcare system in various parts of the world. This plant is renowned for its antibacterial and anticancer effects and its usage in the treatment of jaundice, diabetes, hypertension, and polio. All of the economically and medicinally essential plant parts of this species are used in the preparation of a potent cathartic. This review focused on and intended to highlight the most current knowledge about A. cathartica, including its important ethnomedicinal, modern medicinal, and phytochemical potential along with its green approaches. This plant has been extensively used in herbal medicine and has various important phytopharmacological properties. The modern green technological approaches of this plant enhance agricultural productivity when its various nanoparticles are applied in fields that perform antimicrobial, antipathogenic activities. Nanoparticles serve as carriers for the delivery of drugs and as disease targets in contemporary medicine. This plant has recently been involved in modern medicine as a threat to cancer, which is a significant accomplishment for modern medical science. Hence, A. cathartica is an important plant that can be useful to cure various ailments and could be useful in modern science with its green approaches. We must further investigate this plant's bioactivities to determine the mode of action.
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Exploring Human 5HT1A/2A Receptor Through Homology Modeling and Flexible Docking Studies for the Binding Hotspot of Substituted 2,4-imidazolidinedione and Oxazolidinedione Derivatives
Authors: Meenakshi Dhanawat, Sumeet Gupta and Somdutt MujwarIntroductionTo obtain the binding site of a model of the human 5-HT1A/2A receptor, a series of substituted 2,4-imidazolidinediones and oxazolidinediones were subjected to flexible docking using GLIDE.
MethodsThe docking scores that were generated are correlated with the in-vivo affinity data that had already been collected.
ResultsWhen combined with a homology model of 5HT1A/2A, the GLIDE docking approach was based on a template for 2-adrenergic receptors.
ConclusionA model for ligand binding in the hydrophobic portion of the binding site was proposed after discussing the impact of the structure and hydrophobic characteristics of the aryl moiety on binding affinities.
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Organoselenium Compounds as Potential Therapeutic Agents for Treating Brain Disorders
Authors: Varsha Sarode, Lata Kothapalli, Asha Thomas and Ritesh BholeAmong the inorganic elements, selenium is one of the essential entities required in trace amounts. Selenium (Se) has a vital role to play in brain physiology. It is well demonstrated that an abnormal level of selenium is the cause of the pathogenesis of various neurodegenerative diseases. As selenium levels are age-dependent, deficiency of Se is well correlated with cognitive disability with aging, which further correlates with Alzheimer’s disease. Organoselenium compounds are considered an essential therapeutic class of compounds as they have gained a wide spectrum of applications in biotransformation and are well-studied by several researchers. In recent years, a detailed analysis of the effectiveness of organoselenium compounds in attenuating disease are done. A literature search on PubMed, Embase, and Scopus databases was done using the keywords “organoselenium compounds, brain disorder, Alzheimer's, Parkinson's' disease, and neurodegenerative disorders. The introduction of selenium as a functional group in aryl and heteroaryl compounds has given the lead for treating various brain ailments including Alzheimer's disease, depression, anxiety, Parkinson’s disease, etc. The organoselenium compounds are also potent antioxidants and are promising chemical entities for further studies.
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Theoretical Investigation on the Mechanistic Pathways of Cp*Cobalt(III)-Catalyzed Transformation of N-Substituted Carbamoyl Indoles to Pyrroloindolone Derivatives
Authors: Rohini Saha, Saptarshi Saha and Gourab Kanti DasAimA theoretical study on the Cp*cobalt(III) catalyzed C-H functionalization transformation of N-substituted carbamoyl indoles with alkyne derivatives to pyrroloindoline derivatives has been performed using the DFT method.
BackgroundThe indole skeleton is important for developing regioselective C-H bond functionalisation reactions. Pyrrolo[1,2-a]indole bearing a 6-5-5 tricyclic skeleton (Scheme-1) is an important structural component found in many biologically active natural products and pharmaceuticals (such as antitumor mitomycin C, antimalarial flinderole B etc.).Thus C−H activation process has great demand methods for efficiently synthesizing a pyrrolo[1,2-a]indole unit from readily available starting materials. Matsunaga & Kanai et al. published one such attractive report, which shows pyrroloindoline derivatives can be synthesized (Scheme-2) through Cp*Co(III) catalysed C-H alkenylation and annulations from N-substituted carbamoyl indoles.
ObjectiveOur current project deals with determining the rate step of the reaction for the energetically favourable pathway and investigating the actual reason behind the regioselectivity of the products, whether it is steric or electronic effects of the substituents.
MethodsThe geometry optimization and energy calculations of all the systems were carried out with the Gaussian 09 software. Construction of trial geometries, monitoring of the progress of calculations and visualization of the final output was done by several graphical user interface software like Gauss View, Molden etc. Geometry optimization of all species is performed using M06-2X functional in DFT method as a method for performing optimization of structures. 6-31G (d, p) basis set was employed for all non-metal atoms, and the LANL2DZ basis set was employed for cobalt. The relaxed scan method was used to determine the geometries of several transition structures on the reaction pathway's potential energy surface (PES).
ResultsDFT study on a reaction of carbamoyl indoles with alkyne derivatives by activating Co(III)Cp* catalytic condition is done here. The targeting scheme followed the energetics of two possible pathways. The initial step of the reaction is the alkyne insertion step which needs 21.27 kcal mol-1 energy. In the first case, the final annulated product has been generated through a carbon-carbon bond formation, proton transfer and demetallation processes in path-a. The global activation barrier is quite high (30.17 kcal mol-1). However, the study of the second pathway, which generated the simple alkenylated product through the proto-demethylation process in path-b, reveals a more reliable activation barrier (21.27 kcal mol-1).
ConclusionA comparison of the energy requirement reveals that the formation of the final product should go through a favourable simple alkenylation process that is path-b for dimethyl amine. Due to the lower energy barrier, the simple alkenylation pathway (i.e., Path-b) is a more favourable one. The initial alkyne addition step is the rate-determining step. The regioselectivity of the alkyne addition is purely governed by the steric crowding around the substrate. Thus the favourable mode of alkyne addition has a lower energy barrier due to lesser steric interactions. This theoretical investigation may guide future researchers in developing another economical route for generating similar derivatives.
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Quinazolinone: Pharmacophore with Endless Pharmacological Actions
Authors: Meenakshi Dhanawat, Sumeet Gupta and Somdutt MujwarDue to its extensive applications in the field of pharmaceutical chemistry and its potent biological and pharmacological activities, including analgesic, antioxidant, antimicrobial, anticancer, ant-inflammatory, anti-tubercular, antihyperlipidemic, antihistamine, antiviral, anticonvulsant and antiparkinsonian, the heterocyclic molecule occupies a distinct place in the scientific community. The discovery that many synthetic quinazolinone derivatives exhibit a wide range of biological functions has sparked interest in this area of study.
The purpose of this review is to collate literature work reported by researchers on quinazolinone and its derivatives for their various pharmacological activities.
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- Materials Science and Nanotechnology, Nanotechnology
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Chronic Inflammatory Pain Modulating Potential of Rubiadin: In-vivo, In-vitro and In-silico Investigations
Authors: Atul R. Chopade, Suraj N. Mali, Vijay R. Salunkhe, Madhav R. Burade and Prakash M. SomadeBackgroundThe study model of chronic musculoskeletal inflammatory pain, Rubiadin [1,3-dihydroxy-2-methylanthracene-9,10-dione] choice of a drug, aimed to evaluate the anti-hyperalgesic effects.
ObjectiveTo induce gastrocnemius muscle-stimulated hyperalgesia, 3% carrageenan was injected intraperitoneally.
MethodsThe response to heat and mechanical stimuli was monitored for 9 days. The effect of 1st dose of rubiadin started monitoring after the 14th day of carrageenan injection and continued monitoring until the 22nd day. After the administration of rubiadin intraperitoneally, antihyperanalgesic activity was observed.
ResultsFurthermore, increasing the temperature and mechanical threshold supports histopathological observations with extreme reduction in prostaglandin E2 (PGE2) level.
ConclusionThe objective is to observe anti-inflammatory and anti-hyperalgesic activity of rubiadin in a pain model that is initiated via supraspinal or spinal neuronal mechanisms, predominantly by inhibition of PEG2. Rubiadin provides a wide range of activities in the treatment of chronic muscle pain and chronic muscular inflammation.
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Platinum(II) Complexes of 3-Hydroxypyridine-2-Carboxaldehyde, N(4)-Methyl and N(4)-Pyrrolidinyl Thiosemicarbazones: Synthesis, Characterization, and Primary Anticancer Screening against HeLa Cells, and Molecular Docking
Authors: Paras Nath Yadav, Shivani Sharma, Motee Lal Sharma, Abdur Rauf, Umer Rahid and Yuba Raj PokharelBackgroundThiosemicarbazones are an important class of synthetic organic compounds exhibiting promising biological activities, including antiviral, antibacterial, antitubercular, antiprotozoal, antimalarial, antifungal, enzyme inhibitory, and antitumor. Different α-(N)-heterocyclic thiosemicarbazones are potent inhibitors of ribonucleotide reductase enzyme that play a critical role in the DNA synthesis; moreover, some have been found 1000-fold more potent than the clinical drug hydroxyl urea.
ObjectiveDifferent coordination complexes have been assessed for their efficacy to target MDR and surpass side effects associated with platinum drugs. In this work, we have prepared and investigated the anticancer potential of new platinum compounds of 3- hydroxy-2-formylpyridine thiosemicarbazones.
MethodsNovel Pt(II) complexes were synthesized and characterized by elemental analyses, FT-IR, 1H-NMR, UV-visible spectroscopy, and mass spectrometry. The in vitro anticancer activity of the synthesized compounds against HeLa cells by MTT assay was assessed. Protein-fixed and ligand-flexible docking studies were carried out using the Lamarckian genetic algorithm and Autodock 4.2 software.
ResultsThe IC50 values of compounds (3) and (4) through MTT screening against HeLa cells were found to be 107.16 µM and 132.13 µM, respectively. The binding energy value for the complex [Pt(HyPyMe)Cl] was -6.49 kcal/mol. While for complex, [Pt(HyPyPyrd)Cl] was found to have a binding energy value of -6.83 kcal/mol.
ConclusionThe spectroscopic and analytical data showed the mononuclear structures and square planar geometry of the Pt(II) complexes. The compounds exhibited moderate antineoplastic activity, and N(4)-methyl-substituted compound exhibited better anticancer activity. [Pt(HyPyMe)Cl] complex formed hydrogen bond interactions with guanine-6, guanine-7 and thiamine-8. While, [Pt(HyPyPyrd)Cl] interacted with guanine-7 and guanine-16 via hydrogen bond interaction.
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Mitochondrial Dysfunction in Neurodevelopmental Disorders: A Systematic Review on Pathways and Mechanisms
BackgroundNeurodevelopmental disorders (NDDs) are types of disorders that are marked by a wide range of genetic and clinical mutability which will affect the development and function of the brain. Mitochondria are increasingly associated with various neurodevelopmental disorders and it is found because of mutation of mitochondrial genes, which leads to mitochondrial dysfunction.
ObjectiveUnderstanding the pathways and mechanisms of mitochondrial dysfunction related to neurodevelopmental disorders such as ADHD, Pelizaeus-Merzbacher Disease (PMD), mental retardation, Autism spectrum disorder, Rett's syndrome, and Fragile X syndrome is important. In this review, we discussed the possible factors associated with mitochondria that influence the clinical presentation of NDDs, better understanding of the mechanisms behind these pathways will hopefully be helpful for the diagnosis and treatment approaches.
ConclusionMitochondria are simply another subcellular victim of various neurodegenerative pathways, or are they a common denominator on the path to neurodegeneration? A better understanding of functional and molecular mechanistic pathways can lead to the identification of potential targets, thereby opening perspectives for future treatment.
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A State-of-the-Art Review on Opioids Induced Constipation and its Management
Authors: Suraj Longare, Dhwani Rana, Sagar Salave and Derajram BenivalBackgroundPain is a complex physiological and psychological response to a noxious stimulus, sometimes deteriorating a patient’s quality of life. Opioids remain the mainstay treatment modality for chronic pain. Several concerns are raised regarding the long-term use of opioids and the risks associated with their usage. Findings advocate that the longstanding practice of opioid consumption manifests in adverse effects.
ObjectiveDue to the physiological changes opioids instigate in the gastrointestinal tract, opioid-induced constipation remains a common complication pragmatic in patients undergoing opioid medications. Several therapeutic interventions are made available, and the review describes the overall medications with practical examples, aiding in selecting a treatment plan.
MethodsThe method comprises data collection from various search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding pain management, opioids, opioid-induced constipation, and its pharmacological interventions.
ResultsThe thoughtful custom of exploring several options to manage opioid-induced constipation must allow patients to benefit from opioid analgesia.
ConclusionThis paper reviews the role of opioids in pain management, the underlying mechanisms of their action, opioid-induced constipation, and pharmacological therapies, with experimental studies aiding clinicians to optimise treatment plans.
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