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Nutraceuticals for Hypertension Control
Published in Nilanjana Maulik, Personalized Nutrition as Medical Therapy for High-Risk Diseases, 2020
Balázs Varga, Mariann Bombicz, Andrea Kurucz, Béla Juhász
Dried fruits of Piper nigrum (black pepper) are commonly used in gastrointestinal disorders. Its principal alkaloid, piperine is responsible for the antispasmodic effect via opioid agonist and Ca2+ antagonist activity (Mehmood and Gilani 2010). According to Taqvi, Shah et al. (2008), intravenous administration of piperine caused a dose-dependent decrease in mean arterial preassure in normotensive rats. After that, in a Langendroff’s perfused rabbit heart preparation, piperine caused partial inhibition and verapamil caused inhibition of force and rate of ventricular contraction and coronary flow. In addition, piperine inhibited high K+ precontraction and partially inhibited phenylephrine. Moreover, simirarly to verapamil, piperine caused a rightward shift in calcium-concentration-response curves. Both in rat aorta and in bovine coronary artery preparations, piperine demonstrated K+ precontraction endothelium-independent vasorelaxation. Based on these data, piperine exerts its blood pressure lowering effect via the blockage of Ca2+ channels (Taqvi, Shah et al. 2008).
Indian Diet and Cancer Prevention
Published in Sheeba Varghese Gupta, Yashwant V. Pathak, Advances in Nutraceutical Applications in Cancer, 2019
Vasudha Pritipaul, Asra Sami, Sheeba Varghese Gupta
Piper nigrum or black pepper is a spice that originated in Kerala, a region in India. Over time, black pepper became accessible to the rest of the world through trade [44]. It remains a staple ingredient in the Indian diet.
Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Piper nigrum or, more commonly, black pepper is a member of the genus Piper native to India and Southeast Asia. It has been used for thousands of years as a flavoring in food, preservative, and medicine, particularly by the Ayurvedic physicians of India. It contains a wide range of phytochemicals, including phenolics, lignans, terpenes, chalcones, flavonoids, alkaloids, and steroids.1 Piperine, pipene, piperamides, and piperamine are seen as most active with the highest potential various biological activities. The biological effects are reported to include antibacterial, analgesic, antioxidative (which has made it valuable as a spice and food preservative) antispasmodic, hepatoprotective, and antidepressant.2
Topical creams of piperine loaded lipid nanocarriers for management of atopic dermatitis: development, characterization, and in vivo investigation using BALB/c mice model
Published in Journal of Liposome Research, 2022
Pravin Kumar, Dinesh Kumar Sharma, Mahendra Singh Ashawat
In the traditional system of medicine, that is, Chinese, Korean, Japanese, and Iranian several phytoconstituents or a mixture of phytoconstituents have been reported for the treatment of AD (Kumar, Sharma, et al.2020). A common possible mechanism of action of herbal medicines is by regulating the expression of Th1 and Th2 cell, thus reducing the levels of IgE and eosinophils with improved lesions in atopic skin. Piperine a major alkaloid of black pepper (piper nigrum) and long pepper (piper longum) has been used traditionally in folk medicines for the treatment of seizures, asthma, and chronic bronchitis. The different pharmacological investigations have reported the anti-inflammatory activity for piperine (Leila et al.2017). Piperine given orally showed inhibitory action on eosinophils, IgE antibodies, and Th2 cytokines in allergic skin conditions (Jung et al. 2015). Forty-seven to sixty-four percent of piperine given orally is subjected to the first-pass metabolism (Bhat and Chandrasekhara 1986). Further, an oral dose of piperine 10–20 mg/Kg body weight for 30 days was reported to have toxic effects on the reproductive system and eye irritation (Priprem et al.2011, Tasleem et al.2014).
The development of novel cytochrome P450 2J2 (CYP2J2) inhibitor and the underlying interaction between inhibitor and CYP2J2
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Xiangge Tian, Meirong Zhou, Jing Ning, Xiaopeng Deng, Lei Feng, Huilian Huang, Dahong Yao, Xiaochi Ma
Nowadays, herbal medicines are increasingly employed world wide as alternative and complementary therapies. More importantly, various natural products such as vincristine, camptothecin, artemisinin and paclitaxel, had been isolated and widely used in the clinic15–18. For example, CPT-11 as the first-line chemotherapeutic agent, was designed based on the natural product camptothecin19,20. So, herbal medicines were regarded as the valuable resources of drug research and development16,21–23. In our present study, the inhibitory effect of 108 common herbal medicines towards CYP2J2 was screened using our self-developed highly selective fluorescent probe BnXPI of CYP2J224. Among them, Piper nigrum L. exhibited prominent inhibition activity and Piperine was identified as the major bioactive component of Piper nigrum L. After then, based on the chemical structure of piperine, we conducted the structure optimisation according to the interaction characteristics between Piperine and CYP2J2 catalytic cavity to further design and synthesise a series of Piperine derivatives24. Finally, compound 9k and 9l were proved to be potent inhibitors of CYP2J2 which both possessed nanomole level of IC50 values, and their inhibition kinetics were also further investigated; additionally, the underlying interactions between these potent inhibitors and CYP2J2 enzyme were illustrated by docking and molecular dynamic (MD) simulation. All of our findings would give some useful guidance for development of novel inhibitors of CYP2J2 .
In-silico, in-vitro and ex-vivo evidence of combining silymarin phytopharmaceutical with piperine, and fulvic acid for enhancing its solubility and permeability
Published in Pharmaceutical Development and Technology, 2023
Tanya Ralli, Zoya Saifi, Amita Kumari, Vidhu Aeri, Kanchan Kohli
PIP is the world’s first BA enhancer that was validated by Indian scientists at the Regional Research laboratory, Jammu (Javed, Ahsan et al. 2016). It is the major alkaloid which is extracted from the fruits of Piper nigrum belonging to Piperaceae family. They mainly act by enhancing the permeability of the drugs through intestinal mucosa (by acting at P glycoprotein (P-gp) receptor) and inhibiting the drug metabolism enzymes i.e. CYP3A4 and CYP3A5 (Singh and Deep 2011). For evaluating these mechanisms of PIP, we have performed the molecular docking studies with the enzymes involved in permeation enhancement, i.e. P-gp and metabolism inhibitors i.e. CYP3A4 and CYP3A5.