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Molecules ; 26(16)2021 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-34443598


Apocynin (APO) is a known multi-enzymatic complexed compound, employed as a viable NADPH oxidase (NOX) inhibitor, extensively used in both traditional and modern-day therapeutic strategies to combat neuronal disorders. However, its therapeutic efficacy is limited by lower solubility and lesser bioavailability; thus, a suitable nanocarrier system to overcome such limitations is needed. The present study is designed to fabricate APO-loaded polymeric nanoparticles (APO-NPs) to enhance its therapeutic efficacy and sustainability in the biological system. The optimized APO NPs in the study exhibited 103.6 ± 6.8 nm and -13.7 ± 0.43 mV of particle size and zeta potential, respectively, along with further confirmation by TEM. In addition, the antioxidant (AO) abilities quantified by DPPH and nitric oxide scavenging assays exhibited comparatively higher AO potential of APO-NPs than APO alone. An in-vitro release profile displayed a linear diffusion pattern of zero order kinetics for APO from the NPs, followed by its cytotoxicity evaluation on the PC12 cell line, which revealed minimal toxicity with higher cell viability, even after treatment with a stress inducer (H2O2). The stability of APO-NPs after six months showed minimal AO decline in comparison to APO only, indicating that the designed nano-formulation enhanced therapeutic efficacy for modulating NOX-mediated ROS generation.

Acetofenonas/química , Acetofenonas/farmacologia , Peróxido de Hidrogênio/farmacologia , NADPH Oxidases/metabolismo , Nanopartículas/química , Neurônios/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Animais , Sobrevivência Celular/efeitos dos fármacos , Neurônios/citologia , Neurônios/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Células PC12 , Ratos
J Pharmacopuncture ; 23(2): 54-61, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32685233


Inflammation is an immune response of the human body but excessive inflammation is taken as a major factor in the development of many diseases including autoimmune disorders, cancer and nerve disorders etc. In this regards the need is to suppress the inflammatory response. Suppression of extra or imperfect inflammatory response is not a big deal provided there is an exact knowledge of particular target in the body. Recent advancements in Pharmacological aspect made the therapy with improved outcomes in number of patients. Anticytokine therapy might be one of the important and novel approaches for inflammation and Arthritis. This can be achieved only when we go through the pathophysiology of expression and identification of mediators. Let's take an example of cytokine like interleukins (IL), chemokines, interferons (INF), tumor necrosis factors (TNF-α), growth factors, and colony stimulating factors) release pathway which is a major signalling protein in inflammatory response. In the present study we have reviewed the recent pharmacological therapeutic advancement, inflammatory mediators, receptors, and major signalling pathways. Such information will not only provide the idea about the mechanism of action of Pharmaceuticals and molecular targets but also it provides a new aspect for drug designing and new corrective approaches in existing clinical medicines. This study will be a source of good information for the researchers working in the area of drug designing and molecular Pharmacology especially in anti-inflammatory and anti arthritic medicines for target based therapy.

J Pharmacopuncture ; 23(1): 1-7, 2020 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-32322429


Nicotine, primary component of tobaco produces craving and withdrawal effect both in humans and animals. Nicotine shows a close resemblance to other addictive drugs in molecular, neuroanatomical and pharmacological, particularly the drugs which enhances the cognitive functions. Nicotine mainly shows its action through specific nicotinic acetylcholine receptors located in brain. It stimulates presynaptic acetylcholine receptors thereby enhancing Ach release and metabolism. Dopaminergic system is also stimulated by it, thus increasing the concentration of dopamine in nuclear accumbens. This property of nicotine according to various researchers is responsible for reinforcing behavioral change and dependence of nicotine. Various researchers have also depicted that some non dopaminergic systems are also involved for rewarding effect of nicotinic withdrawal. Neurological systems such as GABAergic, serotonergic, noradrenergic, and brain stem cholinergic may also be involved to mediate the actions of nicotine. Further, the neurobiological pathway to nicotine dependence might perhaps be appropriate to the attachment of nicotine to nicotinic acetylcholine receptors, peruse by stimulation of dopaminergic system and activation of general pharmacological changes that might be responsible for nicotine addiction. It is also suggested that MAO A and B both are restrained by nicotine. This enzyme helps in degradation dopamine, which is mainly responsible for nicotinic actions and dependence. Various questions remain uninsurable to nicotine mechanism and require more research. Also, various genetic methods united with modern instrumental analysis might result for more authentic information for nicotine addiction.

Adv Pharmacol Sci ; 2019: 6908716, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30755770


Nutraceuticals are the pharmaceutically blended products that possess both nutritional as well as the medicinal value. Such a product is designed to improve the physical health, fight against day-to-day challenges such as stress, increase longevity, etc. Nowadays, emphasis is given to those herbs which are used as food and medicine due to its greater acceptance. Due to dynamic action, the popularity of nutraceuticals among people as well as healthcare providers has been increased over medicines and health supplements. This review documents herbs with a wide variety of therapeutic values such as immunity booster, antidiabetic, anticancer, antimicrobial, and gastroprotective. These herbs could be better options to formulate as nutraceuticals. Several nutraceuticals are described based on their availability as food, chemical nature, and mechanism of action.

BMC Complement Altern Med ; 15: 304, 2015 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-26335308


BACKGROUND: The objective of the present study is to evaluate the gastroprotective activity of Paederia foetida L. leaf for gastric ulcer. METHODS: The methanol extract of P. foetida L. leaves at two different dose levels was investigated for gastroprotective potential by using Indomethacin-pylorus ligation, alcohol induced and water immersion stress induced model in rats. In vitro DPPH* radical scavenging activity and western blot analysis of stomach tissue from pylorus ligatures rats were also carried out. HPTLC analysis was done to understand the phyto-pharmacological relationship. RESULTS: Methanol extract at a dose level of 100 mg/kg and 200 mg/kg body weight showed 72 and 78% ulcer protection when compared to negative control whereas reference drug shown 82% protection in Indomethacin-pylorus ligation model. Further, methanol extract also showed protective effect against 70% v/v ethanol and stress induced gastric ulcer model. About 84% protection as compared to cimetidine (85%) was seen in western blot analysis of stomach tissue from pylorus ligatures rats. HPTLC analysis of methanol extract of P. foetida L. confirmed the presence of ß-sitosterol. In DPPH* radical scavenging activity, the IC50 value was observed to be 43.52 µg/ml. CONCLUSIONS: These observations established the traditional claim and thus Paederia foetida could be a potent gastroprotective agent for use in future. The gastroprotective activity might be mediated by the Nrf2 mediated antioxidant and anti secretory effects.

Antiulcerosos , Extratos Vegetais , Rubiaceae/química , Úlcera Gástrica , Animais , Antiulcerosos/farmacologia , Antiulcerosos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Plantas Comestíveis/química , Ratos , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle