Background: Coumarin is an oxygen-containing compound in medicinal chemistry. Coumarin plays an important role in both natural systems like plants and also in synthetic medicinal applications as drug molecules. Many structurally different coumarin compounds were found to show a big range of similarity with the vital molecular targets for their pharmacological action and small modifications in their structures resulted insignificant changes in their biological activities. Objective: This review gives detailed information about the studies of the recent advances in various pharmacological aspects of coumarins. Method: Various oxygen-containing heterocyclic compounds represented remarkable biological significances. The fused aromatic oxygen-heterocyclic nucleus is able to change its electron density; thus changing the chemical, physical and biological properties respectively due to its multiple binding modes with the receptors, which play crucial role in pharmacological screening of drugs. A number of heterocyclic compounds have been synthesized which have their nucleus derived from various plants and animals. In coumarins, benzene ring is fused with pyrone nucleus which provides stability to the nucleus. Coumarins have shown a wide range of pharmacological activities such as anti-tumour, anti-coagulant, anti-inflammatory, anti-oxidant, antiviral, anti-malarial, anti-HIV and antimicrobial activity etc. Results: Reactive oxygen species like superoxide anion, hydroxyl radical and hydrogen peroxide are a type of unstable molecule that contains oxygen, which reacts with other molecules in the cell during the metabolism process but it may produce cytotoxicity when reactive oxygen species increase in number, by the damage of biological macromolecules. Hydroxyl radical (˙OH), is a strong oxidizing agent and it is responsible for the cytotoxicity by oxygen in different plants, animals and other microbes. coumarin is the oldest and effective compound having antimicrobial activity, anti-inflammatory, antioxidant, antidepressant activity, analgesic, anticonvulsant activity, etc. Naturally existing coumarin compounds act against SARS-CoV-2 by preventing viral replication through the targeting on active site against the Mpro target protein. Conclusion: This review highlights the different biological activities of coumarin derivatives. In this review we provide an updated summary of the researches which are related to recent advances in biological activities of coumarins analogue and their most recent activities against COVID -19. Natural compounds act as a rich resource for novel drug development against various SARS-CoV-2 viral strains including viruses like herpes simplex virus, influenza virus, human immunodeficiency virus, hepatitis B and C viruses, middle east respiratory syndrome and severe acute respiratory syndrome.
: The aim of the present study was to review the streptozotocin-nicotinamide (STZ-NA) diabetes model. Type 2 diabetes is more prevalent (90-95%) in adults than type 1. Experimentally-induced diabetes models may be established by chemicals, viral agents, insulin antibodies, surgery, etc. The most advisable and prompt method to induce diabetes is using chemicals, and STZ and alloxan are widely used chemicals. STZ has proven to be a better diabetogenic agent than alloxan because alloxan has many drawbacks, as it induces only type 1 diabetes, has a high mortality rate in rats, and causes ketosis in animals. Moreover, it has lesser selectivity towards β-cells, and the diabetes-induced is reversible. STZ can be used to induce both type 1 and type 2 diabetes. It is noted that the genotoxic behavior of STZ in animals is accomplished through a reduction of nicotinamide adenine dinucleotide (NAD+) in pancreatic β-cells via the GLUT2 (Glucose transporter 2), which can cause cellular damage by DNA (Deoxyribonucleic acid) strand breaks that lead to cell death. NA is a biochemical precursor of NAD+, and it is a poly-ADP-ribose-polymerase-1 (PARP-1) inhibitor. NAD+ is an important redox reaction co-enzyme for the production of adenosine triphosphate (ATP) and many other metabolic pathways. Extreme DNA damage contributes to the over-activation of PARP-1, loss of cellular resources, and necrotic cells death. Some studies have expressed that NA can protect pancreatic β-cells against the severe cytotoxicity of STZ. The review concluded that the STZ-NA model is dependent on the competency of NA to attain partial protection against the β-cytotoxic essence of STZ to induce type-2 diabetes.
Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.
Introduction: Diabetes mellitus (DM) and steroid medication, coincided with coronavirus disease 2019 (COVID-19), results in a weakened immune system, allowing some commonly found pathogens to become more harmful. Mucormycosis (black fungus) is such a type of opportunistic infection caused by fungi belonging to the Mucorales family. DM is the most prominent risk factor for mucormycosis. Excessive blood sugar and decreased insulin levels lead to diabetic ketoacidosis (DKA), a devastating complication of DM that can be fatal if left untreated. Methods: Diabetic ketoacidosis is more common in type 1 diabetic patients, although it can also be fall in type 2 diabetic patients. DKA occurs when the body lacks enough insulin to allow blood sugar to enter the cells and is used for energy. Instead, the liver breaks down fat for fuel producing chemicals known as ketones in the process. Results: When too many ketones are created too quickly, they can reach dangerously high levels in the body. Mucormycosis is a rare but serious infectious disease that requires medication or surgical removal. Conclusion: The confluence of diabetes and COVID-19 makes managing mucormycosis a serious and dead issue. Although the effectiveness of prophylactic antifungal therapy has yet to be demonstrated, hyperglycemia control appears to be the most important step in managing mucormycosis in DKA patients.
Background: Diabetes mellitus is a class of metabolic disorder which results high level of sugar due to inadequacy in insulin secretion. High Sugar level in diabetes is linked with the impairment and dysfunction of eyes, kidneys, blood vessels, nerves and heart. In current research there is extended interest in herbal medicines because of the side effects noticed with oral hypoglycemic for therapy of hyperglycemia. Herbal medicines could play a dominant role in the control of diabetes mellitus. Methods: Methanolic extracts of seeds of Psoralea corylifolia L & Psoralea esculenta L has been screened for both in-vitro and in-vivo antihyperglycemic role using streptozotocin induced diabetic rats. The methanolic extract of both plants were evaluated for pancreatic tissue studies. Results: According to the outcomes, a stunning blood glucose level decrement was observed in the diabetic groups treated by methanolic extracts of Psoralea corylifolia L. seeds. Conclusion: In this study, the methanolic extract of Psoralea corylifolia L. seeds used to evaluate antihyperglycemic potential showed appreciably notable and astonishing results, when compared with the Glibenclamide. Methanolic extract of Psoralea corylifolia L. seeds have potential to regulate hyperglycemia in the In-vivo model. Hence Psoralea corylifolia L. methanolic seeds extract may be selected for its antihyperglycemic activity.
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