Actamide - Black pepper [Piper nigrum] fruit 95% piperine powder extract

Actamide Key Facts

Actamide® is a premium quality black pepper extract standardised to 95% piperine

Actamide® is manufactured using proprietary process of extraction of naturally grown handpicked black pepper (Piper nigrum)

---

Background

Black pepper (Piper nigrum) is one of the most widely used spices and belongs to the Piperaceae family. Along with its use as a spice, black pepper has been used as a preservative, an insecticide and as an ingredient in herbal medicine (Takooree et al., 2019). Piperine is commonly touted as a digestive aid, an anti-inflammatory and as an antioxidant. However, piperine is widely used for its bioavailability enhancing effects.

---

At present, we have the following variants of Actamide

Actamide - Black pepper [Piper nigrum] fruit 95% piperine powder extract

Actamide Organic - Black pepper [Piper nigrum] fruit 95% piperine powder extract [Certified Organic]

---

Chemistry

Piperine, an alkaloid, is the major active principle of black pepper. Actamide is standardised to contain no less than 95% piperine.

Piperine

CAS - 94-62-2
Molecular Formula - C17H19NO3
Molecular Weight - 285.34
IUPAC - (2E,4E)-5-(1,3-benzodioxol-5-yl)-1-piperidin-1-ylpenta-2,4-dien-1-one

---

Piperine and Health

Research has found that piperine presents a wide spectrum of biological activities including stimulating digestive enzymes, inhibiting oxidation reactions, enhancing the bioavailability of a number of drugs and other nutrients as well as exhibiting anti-inflammatory effects (Derosa et al., 2016).

Digestion

Piperine is reported to acts as a digestive tract stimulant and interacts with the digestive system in a number of different ways. Piperine can potentially increase bile acid secretion and it can also inhibit bile acid metabolism. Piperine has been found to potentially increase pancreatic lipase, pancreatic amylase, chymotrypsin and trypsin activity (Srinivasan, 2007). Piperine may also enhance the activity of intestinal lipase and intestinal amylase (Platel & Srinivasan, 1996).

Bioavailability Enhancement

Piperine is of major importance to both the supplement industry and pharmaceutical industry due to its actions as a bioenhancer for numerous drugs and nutrients. For this reason, piperine is included in the formulations of many supplements. Piperine enhances the bioavailability of other substances through several different mechanisms. One such mechanism is through its ability to enhance bile acid secretion and inhibit bile acid metabolism. Bile acids aid in the formation of micelle, which is required for the absorption of both lipids and lipid soluble drugs. Therefore, piperine can enhance both the solubility and the absorption of these drugs (Mhaske et al., 2018). Piperine has also been found to interact with intestinal epithelial cells, stimulating gamma-glutamyl transpeptidase activity and therefore increasing amino acid uptake by epithelial cells (Johri et al., 1992).
Efflux pumps are transport proteins that play a vital role in how many drugs work. Research has also found that piperine increases the duration of a drug at the active site by inhibiting human p-glycoprotein, which is a major efflux pump (Bharadwaj et al., 2002). Also, an enzyme, CYP3A4, is a major metabolising enzyme responsible for the first pass metabolism of drugs. This enzyme has been shown to be inhibited by piperine, therefore enhancing the bioavailability of some drugs.
One such ingredient that is commonly paired with piperine is curcumin (CurQreal). Curcumin has a vast array of health benefits but unfortunately possess very poor bioavailability. When curcumin is co-ingested with piperine, curcumin has been found to become 2000% more bioavailable and therefore can be more beneficial to health (Han, 2011). Piperine has also been shown to improve the bioavailability of other substances such as gallic acid and coenzyme Q10 (Bang et al., 2009).
Due to its interaction with numerous drugs, it is vital that individuals who are on medication consult with their doctor before using piperine.

Antioxidant

Oxygen radical injury and lipid peroxidation have been found to contribute to numerous health conditions such as atherosclerosis, cancer and aging. Reactive oxygen species have also been found to play a role in cell damage and the initiation and progression of carcinogenesis. Piperine has been found to suppress the accumulation of lipid peroxidation products, enhance the activity of antioxidant enzymes as well as eliminate the accumulation and activation of polymorphonuclear cells (Derosa et al., 2016). The antioxidant effects of piperine have proven to protect against arthritis thanks to the suppression of lipid peroxidation and boosting the anti-oxidant defence system by shifting the balance of cytokines towards a bone protecting pattern.

Anti-inflammatory

Piperine has shown to be effective at reducing the levels of pro-inflammatory mediators such as interleukin-1β, tumour necrosis factor-α, and prostaglandin-2, and increases levels of the anti-inflammatory mediator interleukin-10 (Derosa et al., 2016). Piperine has also shown to exhibit antirheumatic effects and therefore could be beneficial for the treatment of rheumatoid arthritis (Bang et al., 2009).

Cancer

Piperine has demonstrated antitumour activities in a variety of cancers. Piperine has shown to inhibit proliferation, induce apoptosis in breast cancer and prostate cancer cells (Do et al., 2013; Samykutty et al., 2013; Ouyang et al., 2013). Piperine has also shown to exhibit a cytostatic effect on colorectal cancer cells (Yaffe et al., 2013). As well as this, piperine has also shown promise as a therapeutic agent in the treatment of osteosarcoma and melanoma (Zhang et al., 2015; Fofaria et al., 2014).

---

Trademark

Actamide is a trademark of Vita Actives, EU trademark number 013810981

---

References

1. Bang, J., Oh, D., Choi, H., Sur, B., Lim, S., Kim, J., Yang, H., Yoo, M., Hahm, D. and Kim, K., 2009. Anti-inflammatory and antiarthritic effects of piperine in human interleukin 1β-stimulated fibroblast-like synoviocytes and in rat arthritis models. Arthritis Research & Therapy, 11(2), p.R49.
2. Bhardwaj, R., Glaeser, H., Becquemont, L., Klotz, U., Gupta, S. and Fromm, M., 2002. Piperine, a Major Constituent of Black Pepper, Inhibits Human P-glycoprotein and CYP3A4. Journal of Pharmacology and Experimental Therapeutics, 302(2), pp.645-650.
3. Derosa, G., Maffioli, P. and Sahebkar, A., 2016. Piperine and Its Role in Chronic Diseases. Advances in Experimental Medicine and Biology, pp.173-184.
4. Do, M., Kim, H., Choi, J., Khanal, T., Park, B., Tran, T., Jeong, T. and Jeong, H., 2013. Antitumor efficacy of piperine in the treatment of human HER2-overexpressing breast cancer cells. Food Chemistry, 141(3), pp.2591-2599.
5. Fofaria, N., Kim, S. and Srivastava, S., 2014. Piperine Causes G1 Phase Cell Cycle Arrest and Apoptosis in Melanoma Cells through Checkpoint Kinase-1 Activation. PLoS ONE, 9(5), p.e94298.
6. Han, H., 2011. The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs. Expert Opinion on Drug Metabolism & Toxicology, 7(6), pp.721-729.
7. Johri, R., Thusu, N., Khajuria, A. and Zutshi, U., 1992. Piperine-mediated changes in the permeability of rat intestinal epithelial cells. Biochemical Pharmacology, 43(7), pp.1401-1407.
8. Mhaske, D., Sreedharan, S. and Mahadik, K., 2018. Role of Piperine as an Effective Bioenhancer in Drug Absorption. Pharmaceutica Analytica Acta, 09(07).
9. Ouyang, D., Zeng, L., Pan, H., Xu, L., Wang, Y., Liu, K. and He, X., 2013. Piperine inhibits the proliferation of human prostate cancer cells via induction of cell cycle arrest and autophagy. Food and Chemical Toxicology, 60, pp.424-430.
10. Platel, K. and Srinivasan, K., 1996. Influence of dietary spices or their active principles on digestive enzymes of small intestinal mucosa in rats. International Journal of Food Sciences and Nutrition, 47(1), pp.55-59.
11. Samykutty, A., Shetty, A., Dakshinamoorthy, G., Bartik, M., Johnson, G., Webb, B., Zheng, G., Chen, A., Kalyanasundaram, R. and Munirathinam, G., 2013. Piperine, a Bioactive Component of Pepper Spice Exerts Therapeutic Effects on Androgen Dependent and Androgen Independent Prostate Cancer Cells. PLoS ONE, 8(6), p.e65889.
12. Srinivasan, K., 2007. Black Pepper and its Pungent Principle-Piperine: A Review of Diverse Physiological Effects. Critical Reviews in Food Science and Nutrition, 47(8), pp.735-748.
13. Takooree, H., Aumeeruddy, M., Rengasamy, K., Venugopala, K., Jeewon, R., Zengin, G. and Mahomoodally, M., 2019. A systematic review on black pepper (Piper nigrum L.): from folk uses to pharmacological applications. Critical Reviews in Food Science and Nutrition, 59(sup1), pp.S210-S243.
14. Yaffe, P., Doucette, C., Walsh, M. and Hoskin, D., 2013. Piperine impairs cell cycle progression and causes reactive oxygen species-dependent apoptosis in rectal cancer cells. Experimental and Molecular Pathology, 94(1), pp.109-114.
15. Zhang, J., Zhu, X., Li, H., Li, B., Sun, L., Xie, T., Zhu, T., Zhou, H. and Ye, Z., 2015. Piperine inhibits proliferation of human osteosarcoma cells via G2/M phase arrest and metastasis by suppressing MMP-2/-9 expression. International Immunopharmacology, 24(1), pp.50-58.