ABSTRACT
Coronavirus disease 2019 (COVID-19), named by WHO, is a real public health disaster of the third millennium. This highly contagious viral disease has infected the world population and is now a global pandemic. This acute respiratory distress syndrome (ARDS) has severe complica-tions like pneumonitis, respiratory failure, shock, multiorgan failure, and death. Well-defined FDA-approved synthetic is not yet available. Case management strategies like lockdown, use of masks and sanitizers, social distancing, and repurposing of antiviral drugs were initially undertaken to cope with this pandemic. Different broad-spectrum antiviral drugs are being repurposed as one of the treatment modalities. The global vaccination programme with the newly launched COVID-19 vac-cines, Covishield, covaxin, sputnik V, etc., is an ongoing process. Simultaneously, significant research is being carried out in search of natural antivirals and evaluating the potency of food bioac-tives to aid naturistic protection against the coronavirus. This mini-review has compiled the latest updates on the screening and evidence-based mechanistic evaluation of phytochemicals and food bioactives as non-pharmacological adjuvant aid in COVID pandemics.Copyright © 2023 Bentham Science Publishers.
ABSTRACT
The jelly from achenes of Ficus pumila var. awkeotsang (FPAA) is a famous beverage ingredient in Taiwan. In this work, ficumarin (1), a new compound was obtained from its twigs (FPAT) and elucidated with comprehensive spectroscopic data. The biosynthetic origin was proposed from the p-coumaroyl-CoA pathway. Alloxanthoxyletin, betulinic acid, and catechin were identified as the major and active constituents responsible for relieving neutrophilic inflammation by FPAT. Among them, the most potent alloxanthoxyletin was found to interact with PRO350 and GLU377 of human INOSOX. Further, Nrf2 activating capacity of the FPAT fraction and its coumarins was confirmed. With the analysis of LC-MS/MS data and feature-based molecular networking, coumarins were found as the dominant and responsible components. Notably, alloxanthoxyletin increased Nrf2 expression by up to 816.8 +/- 58% due to the interacting with the VAL561, THR560 and VAL420 residues of 5FNQ protein. COVID-19 Docking Server simulation indicated that pyranocoumarins would promisingly interfere with the life cycle of SARS-CoV-2. FPAT was proven to exert. Copyright © 2022 Taiwan Food and Drug Administration.
ABSTRACT
Introduction: Low molecular weight heparins are used extensively in anticoagulant therapy, due to their safer profile, in comparison to other anticoagulants. Direct Oral AntiCogulants (DOACs) have been initiated in anticoagulant therapy as a safer treatment choice than coumarin derivatives. Objectives: The aim of this study was to investigate the use of oral and injectable anticoagulants, and especially the place of DOACs in anticoagulant treatment, in a tertiary Hospital of Thessaloniki, Greece. Methods: The data were collected by investigating prescriptions from the Hospital Pharmacy of a tertiary Hospital in Thessaloniki, Greece. Prescriptions of oral and injectable anticoagulants for hospitalized patients were collected during the period from June to September 2021. The consumption of the following oral and injectable anticoagulants was recorded in DDDs: acenocumarol, rivaroxaban, apixaban, dabigatran, heparin, enoxaparin, tinzaparin, bemiparin and fondaparinux. Results: The total amount of anticoagulants used was 53,041 DDDs, of which 97,9% were injectable anticoagulants whereas 2,1% were oral anticoagulants. DOACs represented the 1,8% of the anticoagulants used. The consumption of injectable anticoagulants for the hospitalized patients was 51,936 DDDs, of which 63.5% was enoxaparin, 18.5% was tinzaparin, 6.3% was heparin, 6.1% was bemiparin, and 5.6% was fondaparinux. The consumption of acenocumarol was 176 DDDs and the consumption of DOACs was 929 DDDs, with the percentage of rivaroxaban, apixaban, and dabigatran being 46%, 45% and 9% respectively. Indications with the highest prevalence for patients on enoxaparin was COVID 19, heart failure, stroke, angina pectoris, malignancy. Indications with the highest prevalence for patients on tinzaparin was COVID 19, malignancy, stroke. Indications with the highest prevalence for patients on bemiparin was malignancy, COVID 19, aortic valve disease, stroke. Heart failure, stroke and atrial fibrillation were the indications with highest prevalence in patients on DOACs. Acenocumarol was used mainly for heart failure, stroke and aortic valve stenosis. Conclusion: Injectable anticoagulants, and mainly low molecular weight heparins were the treatment of choice in hospitalized patients. Oral anticoagulants represented only a very small proportion (2,1%) of the anticoagulants used. DOACs have replaced coumarin derivatives, representing the 86% of oral anticoagulants in clinical use. Nevertheless, the percentage of DOACs was very low (1.8%) in the total consumption of anticoagulants, with rivaroxaban and apixaban being the most commonly used DOACs. Injectable anticoagulants, especially enoxaparin, are preferred by the clinicians as a safer choice for managing high risk thrombosis in hospitalized patients. DOACs, Direct Oral AntiCogulants, anticoagulants, NOACs.
ABSTRACT
Ayurveda and Siddha systems are the two ancient medical systems originated in India more than 4000 years ago had given many formulary and treatment methods against influenza like infections. Kabasura churan from Siddha system and Maha sudharshan churan from the Ayurvedic system are the two major formulations along with many other individual herbs mentioned in the texts to treat Influenza like infections. Kabasura churan and Maha Sudarshan churan both have antipyretic, analgesic and anti-inflammatory effects. Both formulations were prepared according to Siddha and Ayurvedic texts. Herbs mentioned in both formulations like Turmeric, Tulsi (Basil), Kalmegh (Andrographis), Black Pepper, Liquorice (Mulethi), and Dronapushpi (Leucas) etc., had direct antiviral effect. Herbs like Aswagandha, Ginger, Guduchi (Tinospora), Kulanjan (Galangal) etc., had immunomodulatory and anti-inflammatory effect. Active compounds from different herbs were selected to study their antiviral activity through molecular docking algorithm. Application of modern of tools like Bioinformatics and Highthroughput screening methods can predict the efficacy of the ancient documented formulations and can be compared as per their literature. Compounds like curcumin, Glycyrrhizin, Ursolic acid, Quercetin, Andrographolide, Coumarins etc. were showed polyspecific activity like inhibition of Spike protein, Furin, Main Protease (Mpro) and Papain like Proteases (PLpro). Thus we propose use of Kabasura churan and Maha Sudharshan churan as alternative complementary medicine as a palliative treatment against COVID-19 caused by SARS-CoV-2 by conducting proper Randomized Clinical Trials.
ABSTRACT
In recent years, it has been reported that many herbal plants contain antiviral agents which combat a human disease that is caused by pathogenic viruses. The natural products which are obtained from plants as antiviral agents against viruses have gone through researches to check the efficacy and potentials of the herbal products in the prevention of viral disorders. On the basis of randomized controlled studies and in-vivo studies, and in-vitro studies, some agents are utilized all across the globe. Progressively numerous studies on therapy of antivirals have been increased. Though, efficacy remains disputable for antiviral drugs that are employed for viral disorders. The viral diseases are challenging for the health of people around the world cause significant increase in mortality and enhance crises. There are many synthetic antiviral drugs that have a large number of side effects and have narrow therapeutic window range, while in the other hand herbal formulations have minimized side effects. The advantages of herbal formulation over synthetic drugs encourage us to devise and expand new herbal moieties against the emerging viral infections. The medicinal plants contain phytochemicals that have antiviral properties. In this paper, the activity of antiviral agents from medicinal plants which have importance in Ayurveda, are discussed along with their source.
ABSTRACT
Currently, Covid-19 pandemic infects staggering number of people around the globe and causes a high rate of mortality. In order to fight this disease, a new coumarin derivative ligand (4-[(pyridin-3-ylmethyl) amino]-2H-chromen-2-one) (LTA) has been synthesized and characterized by single-crystal X-ray diffraction, NMR, ATR, UV-Visible and cyclic voltammetry. Chemical reactivity, kinetic and thermodynamic studies were investigated using DFT method. The possible binding mode between LTA and Main protease (Mpro) of SARS-CoV-2 and their reactivity were studied using molecular docking simulation. Single crystal X-ray diffraction showed that LTA crystallizes in a monoclinic system with P2 1 space group. The reactivity descriptors such as nucleophilic index confirm that LTA is more nucleophile, inducing complexation with binding species like biomolecules. The kinetic and thermodynamic parameters showed that the mechanism of crystal formation is moderately exothermic. The binding energy of the SARS-CoV-2/Mpro-LTA complex and the calculated inhibition constant using docking simulation showed that the active LTA molecule has the ability to inhibit SARS-CoV-2.