Selective in vivo molecular and cellular biocompatibility of black peppercorns by piperine-protein intrinsic atomic interaction with elicited oxidative stress and apoptosis in zebrafish eleuthero embryos.

Day to day consumption of black pepper raise concern about the detailed information about their medicinal, pharmaceutical values and knowledge about the biocompatibility with respect to ecosystem. This study investigates the in vivo selective molecular biocompatibility of its seed cover (SC) and seed core (SP) powder extract using embryonic zebrafish model. Gas chromatography mass spectrometry (GCMS) analysis of the extract prepared by grinding showed presence of different components with "piperine" as principle component. Biocompatibility analysis showed dose and time dependent selective effect of SC and SP with LC50 of 30.4 µg/ml and 35.6 µg/ml, respectively on survivability, hatching and heartbeat rate in embryonic zebrafish. Mechanistic investigation elucidated it as effect of accumulation and internalization of black pepper leading to their influence on structure and function of cellular proteins hatching enzyme (he1a), superoxide dismutase (sod1) and tumor protein (tp53) responsible for delayed hatching, oxidative stress induction and apoptosis. The study provided insight to selective biocompatibility of black pepper expedient to produce higher quality spices with respect to pharmaceutical, clinical and environmental aspects.

Quality variation and standardization of black pepper (Piper nigrum): A comparative geographical evaluation based on instrumental and metabolomics analysis.

Black pepper (Piper nigrum; BP), known as the 'king of spices', imported from various countries is widely available in Saudi Arabian markets, as its demand as a food as well as a medicine for minor ailments is increasing in the country. However, there is a lack of appropriate information regarding these samples in terms of quality variation and standardization. We thus aimed to evaluate the quality and standardize the BP sample with respect to its physicochemical characters, active principle variation [i.e. piperine (PPN)], toxicity, and biological activity. The main focus is to validate whether any difference exists in the quality and quantity of active principle in these samples. For this purpose, physicochemical (chemical tests and ash values) and instrumental analyses [accelerated solvent extraction (ASE), ultra-high-pressure liquid chromatography (UHPLC)-diode array detector, infrared (IR), nuclear magnetic resonance (NMR), and inductively coupled plasma-MS (ICP-MS)] and biological evaluation {in vitro antioxidant activity [2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] and cytotoxicity assay} were performed. An extract yield (g) with %recovery of 2.26 ± 4.24 (11.3) was obtained for the Vietnamese sample, using a fast and rapid method of extraction (ASE). These values were 1.22 ± 2.64 (6.1) and 0.75 ± 1.69 (3.75) for the Pakistani and Indian samples. Physicochemical tests revealed the presence of flavonoids and phenolic compounds in all samples; however, in the Vietnamese sample a low amount of total, acid-insoluble, and high water-soluble ash value was noted. IR and NMR was applied to further standardize the samples. Results of ICP-MS analysis showed a high amount of macronutrients and micronutrients in the samples tested while UHPLC analysis revealed a high amount of PPN (ng/mL) in the Pakistani sample (1,362,614.09); these values were 1,051,848.04 and 768,512.81 for the Vietnamese and Indian samples, respectively. In vitro antioxidant and cytotoxicity activities revealed higher potential for the Vietnamese sample. The samples were properly standardized and effectively differentiated in terms of quality and biological activities using a fast and reliable method, however it certainly does not mean that a particular geographical region is more better or productive in terms of herbal products.

Toxicity and Detoxification Mechanism of Black Pepper and Its Major Constituent in Controlling Rhynchophorus ferrugineus Olivier (Curculionidae: Coleoptera).

The survival, feeding response, and detoxification mechanism of Rhynchophorus ferrugineus Olivier, a key pest responsible for destruction of date palm, was examined with different extracts of Piper nigrum and its major constituent (piperine) identified by GC-MS. In the present study, toxicity of different extracts of black pepper was evaluated by incorporating diffferent doses of extracts into the artificial diet of red palm weevil larvae. All extracts showed dose-dependent insecticidal activity to the tested eighth-instar red palm weevil larvae. Among all the extracts, maximum larvicidal activity was exhibited by chloroform (LD50 = 342.62 mg/l), followed by dichloromethane (LD50 = 357.78 mg/l), acetone (LD50 = 372.57 mg/l), and ethanol (LD50 = 408.88 mg/l). However, piperine, a major constituent of all black pepper extracts identified by GC-MS in the present work, was found to be the most potent treatment exhibiting the least LD50 (219.88 mg/l). In addition, nutritional indices evaluated by calculating the efficiency of the conversion of ingested food (ECI) and digested food (ECD) at the same dose (219.88 mg/l) showed that there was maximum reduction in the ECI (49.90%) and ECD (62.21%) index of larvae fed diets incorporated with piperine. Larvae that were fed diets incorporated with different black pepper extracts experienced increases in the expression of detoxification genes (glutathione S-transferase and cytochrome P450), and this upregulation in detoxification genes (glutathione S-transferase, cytochrome P450 and esterase) was tremendously high in larvae fed diets incorporated with piperine. Results suggest that piperine is a promising bio-pesticide agent for the control of R. ferrugineus Olivier.

The larvicidal effects of black pepper (Piper nigrum L.) and piperine against insecticide resistant and susceptible strains of Anopheles malaria vector mosquitoes.

BACKGROUND: Insecticide resistance carries the potential to undermine the efficacy of insecticide based malaria vector control strategies. Therefore, there is an urgent need for new insecticidal compounds. Black pepper (dried fruit from the vine, Piper nigrum), used as a food additive and spice, and its principal alkaloid piperine, have previously been shown to have larvicidal properties. The aim of this study was to investigate the larvicidal effects of ground black pepper and piperine against third and fourth instar Anopheles larvae drawn from several laboratory-reared insecticide resistant and susceptible strains of Anopheles arabiensis, An. coluzzii, An. gambiae, An. quadriannulatus and An. funestus. METHODS: Larvae were fed with mixtures of standard larval food and either ground black pepper or piperine in different proportions. Mortality was recorded 24 h after black pepper and 48 h after piperine were applied to the larval bowls. RESULTS: Black pepper and piperine mixtures caused high mortality in the An. gambiae complex strains, with black pepper proving significantly more toxic than piperine. The An. funestus strains were substantially less sensitive to black pepper and piperine which may reflect a marked difference in the feeding habits of this species compared to that of the Gambiae complex or a difference in food metabolism as a consequence of differences in breeding habitat between species. CONCLUSIONS: Insecticide resistant and susceptible strains by species proved equally susceptible to black pepper and piperine. It is concluded that black pepper shows potential as a larvicide for the control of certain malaria vector species.

Toxicidade de extratos de Piper nigrum, piperina e piperamidas para o diplópodo Orthoporus fuscipes em condições de laboratório / Toxicity of extracts from Piper nigrum, piperine and piperamides to the millipede Orthoporus fuscipes under laboratory conditions

The toxicity of an ethanolic extract of black pepper (Piper nigrum), of piperine and of the synthetic amides adamantylpiperamide, sopentylpiperamide and diisopropylpiperamide was evaluated using the millipede Orthoporus fuscipes. For the experiments, the test organism was exposed to a diet of wheat bran and sugar (9:1) supplemented with the test substance in solution and mortality was monitored over a period of 17 days. Mortality was 100 percent for 0.3 g of the ethanolic extract of black pepper fruits and for diisopropylpiperamide after 4 and 14 days of exposure, respectively. Piperine at a concentration of 0.3 g resulted in 70 percent mortality after 4 days and remained at this rate until the end of the exposure period. Thus, among the compounds tested the ethanolic extract of black pepper fruit was the most effective and most promising for the control of Orthoporus fuscipes populations since it promoted a higher rate of mortality of the test organism within a shorter period of exposure.

A toxicidade do extrato etanólico da pimenta-do-reino (Piper nigrum), da piperina e amidas sintéticas: adamantilpiperamida, isopentilpiperamida e diisopropilpiperamida foi avaliada para o diplópodo Orthoporus fuscipes. Os experimentos consistiram na exposição dos organismos-teste a uma dieta de farelo de trigo e açúcar (9:1) a qual foi adicionada a substância teste em solução observando-se a mortalidade por um período de 17 dias. Verificou-se na dose contendo 0,3 g do extrato etanólico de frutos da pimenta-do-reino e da diisopropilpiperamida, 100 por cento de mortalidade após 04 e 14 dias de exposição, respectivamente. A piperina na concentração de 0,3 g causou 70 por cento de mortalidade após 4 dias, mantendo-se até o final do período de exposição. Dessa forma, dentre os compostos testados, o extrato etanólico do fruto da pimenta-do-reino foi considerado o mais eficiente e promissor no controle de populações de Orthoporus fuscipes, pois foi o que promoveu maior porcentagem de exposição.