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1.
Pak J Pharm Sci ; 36(5): 1467-1481, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37869923

RESUMEN

Ficus religiosa L., a member of the Moraceae family, is a medicinal plant having a number of pharmacological properties. The anti-inflammatory and analgesic actions of an ethanolic extract of F. religiosa bark FRE (at 100 and 200mg/kg dosages) and the biomarker component quercetin QC (at 5 and 10mg/kg doses) were investigated. The estimate of quercetin was carried by using an HPTLC analysis of FRE. Additionally, qualitative and quantitative screening for key important phytocomponents was done using dried, ground plant stem barks. By using molecular docking, the molecular interaction profile with several anti-inflammatory drug targets was examined. Both the FRE as well as QC showed a substantial decline in paw volume when compared with the relevant control groups (p<0.01 & p<0.001). Following the administration of acetic acid to mice, the FRE and QC both demonstrate a substantial lengthening of the paw licking or leaping towards Eddy's hot plate as well as a decrease in the number of writhes (p<0.01 & p<0.001). This study supports the use of these herbs in conventional medicine to treat pain and inflammation by through similar mechanism as compound quercetin (QC).


Asunto(s)
Ficus , Ratones , Animales , Factor de Necrosis Tumoral alfa , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Quercetina/farmacología , Analgésicos/farmacología , Analgésicos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios no Esteroideos , Fitoquímicos/farmacología
2.
Molecules ; 27(13)2022 Jun 21.
Artículo en Inglés | MEDLINE | ID: mdl-35807236

RESUMEN

For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor-acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemical pathways and enzymes or stimulate/block the receptors in the biological systems. Therefore, medicinal chemists have been focusing their efforts on thiazole-bearing compounds in order to develop novel therapeutic agents for a variety of pathological conditions. This review attempts to inform the readers on three major classes of thiazole-bearing molecules: Thiazoles as treatment drugs, thiazoles in clinical trials, and thiazoles in preclinical and developmental stages. A compilation of preclinical and developmental thiazole-bearing molecules is presented, focusing on their brief synthetic description and preclinical studies relating to structure-based activity analysis. The authors expect that the current review may succeed in drawing the attention of medicinal chemists to finding new leads, which may later be translated into new drugs.


Asunto(s)
Tiazoles , Tiazoles/química
3.
J Pharm Bioallied Sci ; 16(1): 31-37, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38694964

RESUMEN

Background: In India, the cosmetics industry has expanded significantly because of changing lifestyles and increased awareness. In terms of earning the most money from the personal care and cosmetics industry in 2021, India is ranked fourth globally. Many cosmetics sold in India include ingredients that cannot be used on humans. Objective: To assess knowledge, attitudes, and practice toward the uses of cosmetics and cosmetovigilance in India. Methods: A cross-sectional study was conducted, from April to May 2022, among the general population living in the Delhi NCR region, India. Study questionnaires (printed and survey link) were distributed in public as well as at workplaces for the survey. Results: Around 268 (54.78%) females and 223 (45.21%) males participated in the survey. Amongst the total respondents - 407 (83%) agreed that they are using cosmetic products on a daily basis, females 229 (85.44%), being the majority users compared to males 178 (80%), with a significant P value = 0.011. Most of the people reported side effects of shampoos - 7.13% (hair fall, hair thinning, dryness of the scalp, itching), followed by allergic reactions to moisturizers - 5.70%. Conclusion: Because of the right safety and effectiveness mentorship of cosmetics, regulatory agencies and stakeholders should adopt this broadly. Cosmetovigilance needs to be put into practice.

4.
Expert Opin Drug Deliv ; 19(7): 771-793, 2022 07.
Artículo en Inglés | MEDLINE | ID: mdl-35695697

RESUMEN

INTRODUCTION: Diabetes mellitus (DM) is the most common metabolic disease and multifactorial, harming patients worldwide. Extensive research has been carried out in the search for novel drug delivery systems offering reliable control of glucose levels for diabetics, aiming at efficient management of DM. AREAS COVERED: Polymeric micelles (PMs) as smart drug delivery nanocarriers are discussed, focusing on oral drug delivery applications for the management of hyperglycemia. The most recent approaches used for the preparation of smart PMs employ molecular features of amphiphilic block copolymers (ABCs), such as stimulus sensitivity, ligand conjugation, and as a more specific example the ability to inhibit islet amyloidosis. EXPERT OPINION: PMs provide a unique platform for self-regulated or spatiotemporal drug delivery, mimicking the working mode of pancreatic islets to maintain glucose homeostasis for prolonged periods. This unique characteristic is achieved by tailoring the functional chemistry of ABCs considering the physicochemical traits of PMs, including sensing capabilities, hydrophobicity, etc. In addition, the application of ABCs for the inhibition of conformational changes in islet amyloid polypeptide garnered attention as one of the root causes of DM. However, research in this field is limited and further studies at the clinical level are required.


Asunto(s)
Diabetes Mellitus , Micelas , Diabetes Mellitus/tratamiento farmacológico , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Glucosa , Humanos , Polímeros/química
5.
Chem Biol Interact ; 361: 109960, 2022 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-35533733

RESUMEN

In recent years, unique physicochemical properties of amphiphilic block copolymers have been utilized to design the polymeric micelles for brain-specific delivery of drugs, proteins, peptides and genes. Their unique properties such as nano-size, charge-switching ability, stimuli-responsive cargo release, flexible structure, and self-assembly enable them to overcome limitations of conventional dosage forms that include rapid drug release, drug efflux, and poor brain bioavailability, and poor stability. These limitations hinder their therapeutic efficacy in treating brain diseases. Their ease of functionalization and enhanced penetration and retention effect make them suitable nanocarriers for the diagnosis of various brain diseases. In this context, the present manuscript provides an insight into the progress made in the functionalization of micelles such as the incorporation of stimuli-sensitive moieties in copolymers, conjugation of cargo molecules with the core-forming block via responsive smart linkers, and conjugation of active ligands and imaging moieties with the corona forming block for brain targeting and imaging. Further, the review also expounds on the role of polymeric micelles in delivering neurotherapeutic to the brain. Some patents related to polymeric micelles formulated for brain delivery are also enlisted.


Asunto(s)
Encefalopatías , Micelas , Encéfalo , Encefalopatías/tratamiento farmacológico , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Humanos , Polímeros/química
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