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Nanomaterials in Cardio Protection
Published in Parimelazhagan Thangaraj, Lucindo José Quintans Júnior, Nagamony Ponpandian, Nanophytomedicine, 2023
Piperine, a major alkaloid in black pepper, has shown great advantages as a loaded component in lipid-based nanoparticles with applications in neurodegenerative diseases and epilepsy. The role of this bioactive compound as a major oxidative stress reducer has been studied using in vitro spectroscopy. Such compounds are expected to be further explored in combination with therapeutic (Smilkov et al. 2019) nanoconjugates to overcome the impact of oxidative stress in cardiovascular and other diseases.
Nanophytopharmaceuticals
Published in Bhupinder Singh, Om Prakash Katare, Eliana B. Souto, NanoAgroceuticals & NanoPhytoChemicals, 2018
Alka Mukne, Swapna Nair, Misbah Momin
Polymeric nanoparticles have also been developed for co-delivery of more than one drug to achieve synergistic effect and enhance the intracellular drug concentrations. Camptothecin, an alkaloid obtained from Camptotheca acuminata, is reported to have a broad spectrum of anticancer activity. The clinical use of camptothecin is restricted due to its hydrophobicity and toxicity and is often co-administered with other natural anticancer agents such as curcumin. Xiao et al. (2015) prepared chitosan-functionalized cationic polymeric nanoparticles loaded with camptothecin and curcumin, as a combination therapy for treatment of colon cancer. The nanoparticles exhibited an initial burst release, followed by simultaneous sustained release of both the drugs up to 72 h. In vitro studies revealed that the cellular uptake and anticancer activity of both drugs were significantly higher in colon-26 cells when the drugs were formulated as polymeric nanoparticles. A similar study has been reported by Katiyar et al. (2016), where PLGA nanoparticles were prepared by nanoprecipitation method for co-delivery of rapamycin and piperine for the treatment of breast cancer. Rapamycin, a macrolide obtained from the bacterium Streptomyces hygroscopicus, is a potent anticancer agent that is in phase II clinical trials for the treatment of breast cancer. Despite its potency, clinical use of rapamycin is limited due to its poor water solubility, low oral bioavailability, dose-dependent toxicity and low tumor specificity. Rapamycin is effluxed out by P-glycoprotein and MDR-associated proteins (MRP-1, -2, and -3) that further reduce its bioavailability. Piperine (an alkaloid obtained from Piper longum) was used as a chemosensitizer in the formulation to improve the efficacy of rapamycin. Piperine itself has mild anticancer activity and is reported to act as a natural bioenhancer by improving intestinal permeability. It also acts as a P-glycoprotein inhibitor and increases clinical bioavailability of drugs due to its ability to inhibit metabolizing enzymes. The formulation showed sustained in vitro release of both phytoconstituents for two weeks, with rapamycin getting released at a slower rate compared with piperine. Evaluation of effect of P-glycoprotein efflux on drug transport using an in vitro everted gut sac method revealed that uptake of rapamycin had increased in the presence of piperine. In vivo pharmacokinetic studies showed that bioavailability of rapamycin had increased 4.8 times in the presence of piperine. Rapamycin-piperine-PLGA nanoparticles demonstrated significantly greater in vitro anticancer activity in human-derived breast cancer cell lines (MDA-MB-231) compared with free rapamycin solution.
Vitamin E modified polyamidoamine dendrimer for piperine delivery to alleviate Aβ1–42 induced neurotoxicity in Balb/c mice model
Published in Journal of Biomaterials Science, Polymer Edition, 2023
Ajit Singh, Debarati Rakshit, Ankit Kumar, Awanish Mishra, Rahul Shukla
To tackle acetylcholine (Ach) restoration and antioxidant effect phytochemicals have received more attention for the management of several neurodegenerative illnesses. Treatments for different neurodegenerative conditions have been proposed using a range of medicinal herbs. The fruit of Piper longum plant contains nitrogenous bitter alkaloid known as piperine (PIP). PIP has been shown to have a substantial impact on the CNS and enhances cognitive function in AD preclinical studies [5]. According to structure based activity of PIP showed multiple double bond system in molecular structure which functions as free radical scavenging which scavenges reactive oxygen species. Whereas tertiary nitrogen aziridinium ion in PIP structure functions as the antagonist of acetylcholine esterase (AChE) enzyme in the CNS [6]. Despite all PIP neuroprotective benefits, the physicochemical characteristics prevent oral delivery to brain and systemic circulation. PIP possesses a number of challenges in the physiochemical characteristics, including a poor water solubility of 40 µg/mL and log P value of 2.25. Due to extremely hydrophobic nature of PIP absorption to the systemic circulation and brain delivery through oral delivery [7, 8].
The protective effect of piperine on oxidative stress and hepatic damage induced by diisononyl phthalate in rat
Published in Egyptian Journal of Basic and Applied Sciences, 2021
Oluwatobi Adewumi Adeyemo, Ayokanmi Ore, Elizabeth Oyinkansola Ajisafe
Exposure to phthalates is currently a source of concern worldwide, considering the industrial importance of phthalates as well as their potential health risks [23,24]. DINP is one of the most commonly applied phthalates in wide varieties of plastic products and other household materials [25]. Studies have demonstrated the ability of DINP to induce hepatotoxicity via oxidative stress, inflammation and depletion of the hepatic antioxidant system [6,26,27]. Piperine (PIPE), an alkaloid from black pepper, has demonstrated huge potentials in the treatment of chronic diseases, mostly attributed to its antioxidant and anti-inflammatory activities [28]. This study was designed to investigate the protective effects of PIPE in DINP-induced hepatotoxicity in the rat model.
Phytotoxicity assessment of synthesized green nanosuspension on germination and growth in Vigna radiata
Published in Inorganic and Nano-Metal Chemistry, 2021
Ranjani S., Noorul Samsoon Maharifa H., Raihanathus Sahdhiyya A., Hemalatha S.
Piper nigrum of the family Piperaceae, commonly known as Black pepper is the most widely used culinary spice, also used as a medicine, preservative, and antimicrobial agent. Piperine, a major bioactive compound in pepper has been found to have antioxidant, antimicrobial, anticarcinogenic, antiasthmatic, immunomodulatory, neuroprotective, hypoglycemic, antiulcer, and anti-inflammatory properties.[20,21] Bioactive compounds of pepper such as Nerolidol and Piperamides have pesticidal and insecticidal activities.[22]