Phytotherapeutic Agents in Epilepsy
Vikas Kumar, Addepalli Veeranjaneyulu in Herbs for Diabetes and Neurological Disease Management, 2018
Piperine is a piperidine alkaloid responsible for the pungency of black pepper (P. nigrum; Fam. Piperaceae) used as an analgesic, anti-inflammatory agent and in the treatment of epilepsy in traditional system of medicine. In traditional Chinese medicine, a mixture of radish and pepper is used to treat epilepsy. Earlier studies have documented anticonvulsant effects of piperine against kainate-induced seizures.143 Piperine significantly delays the onset of PTZ-and PIC-induced seizures,144 seizures induced by PIL145 and STR.146 The studies indicate that piperine exhibits analgesic and anticonvulsant effects via opioid and GABA-ergic pathways, respectively.144,145 A recent study on anticonvulsant mechanisms of piperine has suggested that Na+ channel antagonist activity could also be a contributor to the complex anticonvulsant mechanisms of piperine.146
Curcumin and Neglected Infectious Diseases
Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay in Medicinal Chemistry of Neglected and Tropical Diseases, 2019
In the past three decades, several strategies have been adopted in order to increase curcumin (1) bioavailability, mainly by improving the solubility and stability of the compound, as well as decreasing the metabolic degradation. Initially, the co-administration with piperine (31) (Figure 8) demonstrated to limit the hepatic and intestinal metabolism of curcumin and, thus, increase its bioavailability (Shoba et al. 1998). Chemical structure of piperine (31).
Peepali
H.S. Puri in Rasayana, 2002
In Ayurveda, a composition consisting of long pepper, black pepper and ginger is very often incorporated into various formulations under the name Trikatu. In some research (Atal et al. 1981) it was found that Trikatu enhanced the bioavailability of other therapeutic agents. Zutshi and Kaul (1982) observed that individual members, as well as Trikatu collectively, increased the bioavailability of vaccines by 300 per cent when orally ingested. The same effect was seen in long and black pepper, and it was found that this activity is due to the alkaloid piperine. Lee et al. (1984) carried out a pharmacological study on piperine. Bano et al. (1987) noted that piperine altered the pharmacokinetic parameters of phenytoin. Majumdar et al. (1990) also observed that piperine makes pentabarbitone more potent and thus increases sleeping time by inhibiting liver enzymes. Annamalai and Manavalan (1990) also confirmed that Trikatu enhanced the therapeutic activity by reducing acid secretion and preventing the degradation of active medicaments by gastric acids. Majeed et al. (1996) patented the use of piperine for gastro-intestinal absorption and its systemic utilization in nutritional supplements. Shoba et al. (1998) confirmed that Trikatu enhanced the bioavailability of drugs.
Development of piperine nanoemulsions: an alternative topical application for hypopigmentation
Published in Drug Development and Industrial Pharmacy, 2022
Burcu Ozkan, Ebru Altuntas, Rabia Cakir Koc, Yasemin Budama-Kilinc
Piper longum L. (long pepper) and Piper nigrum L. (black pepper) (Piperaceae) are traditionally used in Indian medicine and are among the most widely used spices in the world. Piperine is an alkaloid derived from its oleoresin in black pepper, giving the bitter taste of P. longum L. and P. nigrum L. [13]. Recently, piperine has been found to be effective in the pigmentation mechanism as well as other biological activities [14]. A group of scientists from King's College London showed that basic alkaloid piperine and its synthetic derivatives stimulate skin pigmentation and are effective in restoring skin pigmentation [10]. In a study conducted by Soumyanath et al., piperine has been demonstrated to increase melanocyte proliferation in vitro, and act through protein kinase C stimulation [15]. In another study, it was observed that the aqueous extract of piperine (0.1 mg/ml) stimulated the growth of mouse melanocyte line culture by approximately 300% within 8 days [16]. In this content, piperine can be considered as a potential active ingredient with its biological activities on melanogenesis, providing the re-occurrence of pigmentation and these findings may lead to better outcomes in the development of potential treatments. It can also reduce the risk of skin cancer by reducing the need for UV radiation in the treatment of vitiligo.
Augmentation of therapeutic potential of curcumin using nanotechnology: current perspectives
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Pulavendran Sivasami, Thiagarajan Hemalatha
Shoba et al. have proved that stabilizing agent could improve the bioavailability of curcumin by administering piperine followed by curcumin injection in rats. The serum concentration is increased after piperine administration and the same trend is observed in healthy human volunteers [25]. However, how concomitant administration helps to improve the serum concentration and mechanistic actions over stabilization of drug in in vivo is not understood. In addition, piperine has adverse effects on the metabolism of a wide range of drugs [26,27]. Graft-vinyl acetate copolymers are synthesized by free radical polymerization and curcumin nanoparticles are prepared by ultrasonic irradiation. The nanoparticles are discrete and uniform spheres, covered with positive charges. The encapsulation efficiency of nanoparticles is up to 91.6% and a slower release rate of curcumin is achieved [28]. Because of highly hydrophobic nature, curcumin cannot be administered systemically. Liposomal encapsulation of curcumin makes this agent amenable to intravenous dosing and circumvents the problem of poor oral availability that limits the utility of free curcumin. The composition shows increased resistance to cancer cell growth; however, in vitro release is not explained [29].
Hydroxypropyl-β-cyclodextrin as an effective carrier of curcumin – piperine nutraceutical system with improved enzyme inhibition properties
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Anna Stasiłowicz, Ewa Tykarska, Kornelia Lewandowska, Maciej Kozak, Andrzej Miklaszewski, Joanna Kobus-Cisowska, Daria Szymanowska, Tomasz Plech, Jacek Jenczyk, Judyta Cielecka-Piontek
Curcumin and piperine have been shown to be able to act within the CNS44,45. As a pleiotropic effect of curcumin within the central nervous system, anti-inflammatory, antioxidant, and anti-protein-aggregate action are mentioned46. Curcumin’s profile of activity places it as an important nutraceutical candidate in the prevention of neurodegenerative diseases such as Alzheimer’s, Parkinson’s and stroke47,48. Neuroprotective effects have also been reported in piperine. S. Hua pointed out in preclinical studies on the effect of piperine on neural apoptosis in the case of brain damage in animals49. P. Shrivastava et al.50 confirmed that the anti-inflammatory effect of piperine might inhibit the development of Parkinson’s diseases. Our results confirm the possibility of curcumin (Papp 3.11 × 10−5 cm s−1) and piperine (1.19 × 10−5 cm s−1) permeability through the blood–brain barrier. Both compounds were classified as well permeable because they achieved higher Papp values than 4.0 × 10−6 cm s−128. The preparation of the curcumin and the piperine nutraceutical system with 2-hydroxypropyl-β-cyclodextrin increased their permeability through the blood–brain barrier (Papp 3.95 × 10−5 cm s−1 and 3.77 × 10−5 cm s−1, respectively).
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