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1.
Drug Res (Stuttg) ; 72(3): 123-130, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34979573

RESUMEN

The 2019-nCoV (COVID-19; novel coronavirus disease-2019) outbreak is caused by the coronavirus, and its continued spread is responsible for increasing deaths, social and economic burden. COVID-19 created a chaotic situation worldwide and claimed the lives of over 5,027,183 and 248,467,363 confirmed cases have been reported so far as per the data published by WHO (World Health Organization) till 5th November 2021. Scientific communities all over the world are toiling to find a suitable therapeutic drug for this deadly disease. Although till date no promising drug has been discovered for this COVID-19. However, as per the WHO, over 102 COVID-19 vaccines are in clinical development and 185 in pre-clinical development. Naturally occurring phytoconstituents possess considerable chemical richness in the form of anti-viral and anti-parasitic potential and have been extensively exploited for the same globally. Still, phytomedicine-based therapies are considered as the best available treatment option to minimize and treat the symptoms of COVID-19 because of the least possible side effects compared to synthetic drugs recommended by the physicians/clinicians. In this review, the use of plant chemicals as a possible therapeutic agent for severe acute respiratory syndrome coronavirus 2 (SARS CoV2) is highlighted with their proposed mechanism of action, which will prove fruitful and effective in finding a cure for this deadly disease.


Asunto(s)
Tratamiento Farmacológico de COVID-19 , Antivirales/uso terapéutico , Vacunas contra la COVID-19 , Humanos , SARS-CoV-2
2.
Drug Res (Stuttg) ; 70(11): 493-502, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32707592

RESUMEN

An efficient and environmental benign solvent-free synthesis of 5-amino-3-aryl-1-(6'-chloropyridazin-3'-yl)pyrazoles (4A-E): was accomplished by grinding 3-chloro-6-hydrazinopyridazine (2): and ß-ketonitriles (3A-E): in the presence of p-toulenesulfonic acid as a catalyst. Subsequently, 6'-chloro group in 4A-E: was replaced with cyclic 2° amine derivatives viz. pyrrolidine 5A: , piperidine 5B: and morpholine 5C: to obtain 6A-E: , 7A-E: , 8A-E: respectively. The newly synthesized compounds were characterized by using IR, NMR (1H and 13C), mass spectral studies, elemental analyses. All the synthesized compounds were studied for their docking interaction with target protein 6COX and screened for their in vivo analgesic mode of action against swiss albino mice (animal model) using acetic-acid induced writhing test. Consequently, docking simulations data justifies the potential of synthesized series as an analgesic and very well correlated with in vivo study. Preliminary results revealed that most of the synthesized compounds exhibited moderate to good analgesic activity as compared to reference/standard drug (s) sodium diclofenac and candidates 4D: and 7C: protrude out as a promising lead for further investigation.


Asunto(s)
Inhibidores de la Ciclooxigenasa 2/farmacología , Diseño de Fármacos , Dolor/tratamiento farmacológico , Pirazoles/farmacología , Piridazinas/farmacología , Ácido Acético/administración & dosificación , Ácido Acético/toxicidad , Animales , Ciclooxigenasa 2/metabolismo , Ciclooxigenasa 2/ultraestructura , Inhibidores de la Ciclooxigenasa 2/síntesis química , Inhibidores de la Ciclooxigenasa 2/uso terapéutico , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Humanos , Ratones , Simulación del Acoplamiento Molecular , Dolor/inducido químicamente , Pirazoles/química , Pirazoles/uso terapéutico , Piridazinas/química , Piridazinas/uso terapéutico , Relación Estructura-Actividad
3.
Adv Bioinformatics ; 2014: 903246, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25114678

RESUMEN

The present study attempts to establish a relationship between ethnopharmacological claims and bioactive constituents present in Pinus roxburghii against all possible targets for diabetes through molecular docking and to develop a pharmacophore model for the active target. The process of molecular docking involves study of different bonding modes of one ligand with active cavities of target receptors protein tyrosine phosphatase 1-beta (PTP-1ß), dipeptidyl peptidase-IV (DPP-IV), aldose reductase (AR), and insulin receptor (IR) with help of docking software Molegro virtual docker (MVD). From the results of docking score values on different receptors for antidiabetic activity, it is observed that constituents, namely, secoisoresinol, pinoresinol, and cedeodarin, showed the best docking results on almost all the receptors, while the most significant results were observed on AR. Then, LigandScout was applied to develop a pharmacophore model for active target. LigandScout revealed that 2 hydrogen bond donors pointing towards Tyr 48 and His 110 are a major requirement of the pharmacophore generated. In our molecular docking studies, the active constituent, secoisoresinol, has also shown hydrogen bonding with His 110 residue which is a part of the pharmacophore. The docking results have given better insights into the development of better aldose reductase inhibitor so as to treat diabetes related secondary complications.

4.
J Integr Med ; 11(6): 371-6, 2013 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-24299601

RESUMEN

Traditional medicine is a blend of information gathered over generations from various communities and cultures. Pinus roxburghii Sargent (Pinaceae) commonly known as "chir pine" is widely used in traditional and folkloric systems of medicine. The all parts of the plant are believed to possess medicinal qualities in Ayurvedic and Unani systems of medicine. In these traditional systems of medicine, the plant is used to heal many diseases, including afflictions of the eyes, ears, throat, blood, and skin. The plant parts are rich in various bioactive compounds such as α-pinene, abietic acid, quercetin and xanthone. Resin acids and flavanoid form a major portion of these bioactive compounds. This review presents examples of traditional medicinal uses for P. roxburghii, and subsequently explores the current understanding of the chemical, pharmacological, and biochemical properties of the extracts and the main active constituents found in each tissue of the plant. Clinical trial information is also included where available. Careful evaluation of these data may be helpful for scientists and researchers to discover and evaluate the specific chemical entities responsible for the traditional medicinal uses of P. roxburghii.


Asunto(s)
Etnobotánica , Fitoterapia , Pinus , Animales , Humanos , Pinus/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
5.
Artículo en Inglés | WPRIM | ID: wpr-671829

RESUMEN

Traditional medicine is a blend of information gathered over generations from various communities and cultures. Pinus roxburghii Sargent (Pinaceae) commonly known as "chir pine" is widely used in traditional and folkloric systems of medicine. The all parts of the plant are believed to possess medicinal qualities in Ayurvedic and Unani systems of medicine. In these traditional systems of medicine, the plant is used to heal many diseases, including afflictions of the eyes, ears, throat, blood, and skin. The plant parts are rich in various bioactive compounds such as α-pinene, abietic acid, quercetin and xanthone. Resin acids and flavanoid form a major portion of these bioactive compounds. This review presents examples of traditional medicinal uses for P. roxburghii, and subsequently explores the current understanding of the chemical, pharmacological, and biochemical properties of the extracts and the main active constituents found in each tissue of the plant. Clinical trial information is also included where available. Careful evaluation of these data may be helpful for scientists and researchers to discover and evaluate the specific chemical entities responsible for the traditional medicinal uses of P. roxburghii.

6.
Zhong Xi Yi Jie He Xue Bao ; 10(9): 1056-60, 2012 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-22979938

RESUMEN

OBJECTIVE: To study the anticonvulsant activity of alcoholic extract of bark of Pinus roxburghii Sarg. (AEPR) used in Indian traditional medicine system in treating convulsion. METHODS: Anticonvulsant activity was evaluated by maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced seizures in Wistar albino rats. In the MES model, 150 mA current for 0.2 s was given through ear electrodes to induce convulsions in rats. The duration of tonic extension of hind limb was used as the end point, namely, prevention or decrease in the duration of hind limb extension was considered as a protective action. In the PTZ model, the anticonvulsant property of AEPR was assessed by its ability to delay the onset of myoclonic spasm and clonic convulsions produced by intraperitoneal administration of PTZ. RESULTS: In the MES-induced seizure model, AEPR in doses of 300 and 500 mg/kg body weight reduced all the phases of convulsion significantly (P<0.01). Standard drug phenytoin at a dose of 25 mg/kg significantly reduced flexion phase (P<0.01) and abolished all phases of convulsion. In the PTZ-induced seizure model, the administration of the extract at doses of 300 and 500 mg/kg 30 min prior to injection of PTZ significantly delayed the onset of clonic seizure (P<0.01). AEPR at the dose of 100 mg/kg body weight could not exert any significant protective effect on PTZ-induced convulsions. Standard drug diazepam at a dose of 4 mg/kg showed much delayed onset of clonic seizure. CONCLUSION: The study suggests that AEPR would be effective against generalized tonic-clonic and partial seizures. Thus AEPR possesses anticonvulsant property against MES- and PTZ-induced seizures in Wistar rats. However, further research is in progress to isolate the compound responsible for its activity.


Asunto(s)
Anticonvulsivantes/farmacología , Pinus/química , Extractos Vegetales/farmacología , Convulsiones/tratamiento farmacológico , Animales , Anticonvulsivantes/uso terapéutico , Femenino , Masculino , Corteza de la Planta/química , Extractos Vegetales/uso terapéutico , Ratas , Ratas Wistar
7.
Zhong Xi Yi Jie He Xue Bao ; 9(10): 1061-5, 2011 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-22015185

RESUMEN

Traditional medicine systems consist of large numbers of plants with medicinal and pharmacological importance and hence represent an invaluable reservoir of new bioactive molecules. Alpinia galanga (family Zingiberaceae) is commonly known as galangal and has been used for its emmenagogue, aphrodisiac, abortifacient, carminative, antipyretic and anti-inflammatory qualities and used in the treatment of various diseases such as bronchitis, heart diseases, chronic enteritis, renal calculus, diabetes, rheumatism and kidney disorders. It was reported to contain, among other components, essential oils, tannins, phenol, glycosides, monoterpenes and carbohydrates. In the last few years, new compounds such as gallic acid glycoside, galangoisoflavonoid,ß-sitosterol, galangin, alpinin, zerumbone and kampferide have been isolated from various parts of A. galanga. Therefore, the present review is aimed to summarize the information regarding A. galanga concerning the new phytoconstituents and pharmacological uses that have appeared in recent years.


Asunto(s)
Alpinia/química , Flavonoides/química , Flavonoides/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Rizoma/química , Sitoesteroles/farmacología
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