RESUMEN
BACKGROUND: An ulcer is a condition characterized by inflammation, irritation, or erosion in the mucosal lining of the stomach or duodenum. Hence, peptic ulcer is the ulcer of both the stomach and the duodenum. 10% of the world's population is affected by chronic peptic ulcers. The formation of peptic ulcers depends on gastric juice pH and the decrease in mucosal defenses. Nonsteroidal antiinflammatory drugs (NSAIDs) and Helicobacter pylori (H. pylori) infection are the two significant factors disrupting mucosal resistance to injury. Indian herbal plants are exceptional for their ethnic, ethnobotanical, and ethno-pharmaceutical use. In this review, attempts have been made to gain information regarding some plants that may be used to treat or prevent peptic ulcers. The ultimate goal of peptic ulcer disease treatment is to reduce pain, cure ulcers, and prevent recurrence. OBJECTIVE: The aim of the study was to gain knowledge about several common medicinal plants employed in Ayurveda or contemporary science for the treatment or prevention of peptic ulcers and some natural and simple approaches to cure ulcers using readily available herbs. METHODS: The literature search was carried out using search engines, like Google Scholar, Scopus, PubMed, Medline, Springer, etc. Results: The extensive literature search showed natural herbs to have potential anti-ulcer activity, including cabbage, bananas, liquorice, fenugreek, garlic, Terminalia chebula, Acacia arabica, Aegle marmelos, Aloe vera, Allium sativum, Plantago ispagula, Mimosa pudica, Annona squamosa, Azadirachta indica, and Galega purpurea. CONCLUSION: This study concluded several medicinal plants to effectively prevent or cure peptic ulcers caused by a variety of factors, including H. pylori, aspirin, indomethacin, alcohol, and others.
Asunto(s)
Infecciones por Helicobacter , Úlcera Péptica , Plantas Medicinales , Humanos , Úlcera Péptica/tratamiento farmacológico , Úlcera Péptica/epidemiología , Úlcera Péptica/etiología , Aspirina , Antiinflamatorios no Esteroideos/uso terapéutico , Infecciones por Helicobacter/complicaciones , Infecciones por Helicobacter/tratamiento farmacológico , Inflamación/tratamiento farmacológicoRESUMEN
BACKGROUND: Malaria is caused by different species of Plasmodium; among which P. falciparum is the most severe. Coptis teeta is an ethnomedicinal plant of enormous importance for tribes of northeast India. OBJECTIVE: In this study, the antimalarial activity of the methanol extracts of Coptis teeta was evaluated in vitro and lead identification was carried out via in silico study. METHODS: On the basis of the in vitro results, in silico analysis by application of different modules of Discovery Studio 2018 was performed on multiple targets of P. falciparum taking into consideration some of the compounds reported from C. teeta. RESULTS: The IC50 of the methanol extract of Coptis teeta was reported to be 0.08 µg/ml in 3D7 strain and 0.7 µg/ml in Dd2 strain of P. falciparum. From the docking study, noroxyhydrastatine was observed to have better binding affinity in comparison to chloroquine. The binding of noroxyhydrastinine with dihydroorotate dehydrogenase was further validated by molecular dynamics simulation and was observed to be significantly stable in comparison to the co-crystal inhibitor. During simulations, it was observed that noroxyhydrastinine retained the interactions, giving strong indications of its effectiveness against the P. falciparum proteins and stability in the binding pocket. From the Density-functional theory analysis, the bandgap energy of noroxyhydrastinine was found to be 0.186 Ha, indicating a favorable interaction. CONCLUSION: The in silico analysis as an addition to the in vitro results provides strong evidence of noroxyhydrastinine as an antimalarial agent.
Asunto(s)
Antimaláricos , Coptis , Antimaláricos/química , Antimaláricos/farmacología , Coptis/química , Simulación de Dinámica Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plasmodium falciparumRESUMEN
The present manuscript deals with the development of novel p-aminobenzoic acid (PABA) associated 1,3,5-triazine derivatives as antimalarial agents. The molecules were developed via microwave-assisted synthesis and structures of compounds were ascertained via numerous analytical and spectroscopic techniques. The synthesized compounds were also subjected to ADMET analysis. In a docking analysis, the title compounds showed high and diverse binding affinities towards wild (-162.45 to -369.38 kcal/mol) and quadruple mutant (-165.36 to -209.47 kcal/mol) Pf-DHFR-TS via interacting with Phe58, Arg59, Ser111, Ile112, Phe116. The in vitro antimalarial activity suggested that compounds 4e, 4b, and 4h showed IC50 ranging from 4.18 to 8.66 µg/ml against the chloroquine-sensitive (3D7) strain of Plasmodium falciparum. Moreover, compounds 4g, 4b, 4e, and 4c showed IC50 ranging from 8.12 to 12.09 µg/ml against chloroquine-resistant (Dd2) strain. In conclusion, our study demonstrated the development of hybrid PABA substituted 1,3,5-triazines as a novel class of Pf-DHFR inhibitor for antimalarial drug discovery.
Asunto(s)
Antimaláricos , Microondas , Plasmodium falciparum/crecimiento & desarrollo , Triazinas , Antimaláricos/síntesis química , Antimaláricos/química , Antimaláricos/farmacología , Humanos , Triazinas/síntesis química , Triazinas/química , Triazinas/farmacologíaRESUMEN
OBJECTIVE: Ischaemia/reperfusion (I/R) injury is defined as the damage to the tissue which is caused when blood supply returns to tissue after ischaemia. To protect the ischaemic tissue from irreversible injury, various protective agents have been studied but the benefits have not been clinically applicable due to monotargeting, low potency, late delivery or poor tolerability. KEY FINDINGS: Strategies involving preconditioning or postconditioning can address the issues related to the failure of protective therapies. In principle, postconditioning (PoCo) is clinically more applicable in the conditions in which there is unannounced ischaemic event. Moreover, PoCo is an attractive beneficial strategy as it can be induced rapidly at the onset of reperfusion via series of brief I/R cycles following a major ischaemic event or it can be induced in a delayed manner. Various pharmacological postconditioning (pPoCo) mechanisms have been investigated systematically. Using different animal models, most of the studies on pPoCo have been carried out preclinically. SUMMARY: However, there is a need for the optimization of the clinical protocols to quicken pPoCo clinical translation for future studies. This review summarizes the involvement of various receptors and signalling pathways in the protective mechanisms of pPoCo.
Asunto(s)
Poscondicionamiento Isquémico/métodos , Sustancias Protectoras/administración & dosificación , Daño por Reperfusión/tratamiento farmacológico , Animales , Humanos , Precondicionamiento Isquémico/métodos , Sustancias Protectoras/efectos adversos , Sustancias Protectoras/farmacología , Daño por Reperfusión/fisiopatología , Transducción de Señal/efectos de los fármacos , Factores de TiempoRESUMEN
BACKGROUND: Thiazole is one of the leading heterocyclic five-member ring compounds that contain nitrogen and sulphur atom. Many natural and/or synthetic compounds contain thiazole as an essential moiety and possess diverse therapeutic activities. The thiazole ring was modified at different positions to generate new molecules with potent antibacterial activities. Thus, the present review enumerates the antibacterial importance of thiazole and its derivatives. METHOD: The mining of literature has been performed using different database which includes only peer-reviewed journals. The quality of retrieved papers was appraised using standard tools. Moreover, the significant papers were described in detail to focus on thiazole derivatives showing considerable antibacterial activity. RESULT: The present review describes the chemistry, SAR (Structure Activity Relationship) studies and antibacterial importance of thiazole with different synthetic procedures. CONCLUSION: This particular study certainly benefits the researchers interested in exploiting the antibacterial activity of thiazoles in search of novel agents.