The Potential Function of Kisspeptin-10

According to research and studies, Kisspeptin is a naturally occurring protein known as metastin that plays a vital role in reproduction and puberty hormone secretion. Kisspeptin-10 peptide regulates testosterone levels and sex-related behaviors like arousal, drive, and motivation, earning it the moniker “Love Hormone.” The peptide also influences mood and behavior, regulates kidney function, and promotes angiogenesis.

Kisspeptin-10 has also show to potentially inhibit tumor growth and metastasis in the brain. The peptide is under study for its ability to modulate gonadotropin-releasing hormone (GnRH)^[1].

How Kisspeptin-10 Increases Testosterone Secretion

• Kisspeptin-10 may affect and influence testosterone levels by modulating FSH and LH levels in the circulatory system, which is sex-specific. Kisspeptin-10 can increase testosterone levels in men but has no effect on testosterone levels in women.
• Kisspeptin-10 peptide analogs influence the pulse frequency of LH in men, implying that Kisspeptin-10 can possibly fine-tune the regular pulsatile release of sex hormones.
• Clinical trials with Kisspeptin-10 in healthy men show a dose-dependent and rapid increase in serum LH and testosterone levels. Kisspeptin-10 accomplishes this by increasing the pulsatile release of LH. High doses of Kisspeptin-10 peptide can cause rapid pulsation, resulting in continuous LH release.

The Impact of Kisspeptin-10 Peptide on Increasing Gonadotropin-Releasing Hormone

GnRH neurons in the hypothalamus synthesize and release gonadotropin-releasing hormone (GnRH). The first hypothalamic-pituitary-gonadal hormonal release influences the anterior pituitary gland to release FSH and luteinizing hormone (LH). The primary hormone for puberty and the control of gamete maturation in the genitals is GnRH. Kisspeptin-10 can change menstruation in certain conditions, treat precocious puberty, and provide continuous infusion in some cancers by increasing GnRH release. 

The Function of Kisspeptin-10 in Energy Balance

• Kisspeptin-10 neurons are energy status sensitive: undernutrition and overnutrition inhibit Kisspeptin-10 neurons’ ability to induce GnRH release^[3]. Infertility can occur in men and women under extreme energy balance conditions, mediated by the kisspeptin-10 peptide. As a result, Kisspeptin-10 synthesis and release are energy balance sensitive. However, the findings suggest that Kisspeptin-10 may be the sole regulator of energy balance.
• Clinical studies in mice samples depleted of the Kisspeptin-10 receptor (Kiss1r) via genetic manipulation reveal an increase in adiposity and a decrease in energy expenditure. Clinical studies show that Kisspeptin-10 receptors exist in adipose (fat) and brown adipose tissues. Kisspeptin-10 peptide may also help to explain the neurochemical modulation that results in energy-modulating behavior concerning reproduction.

Potential Efects on Mood

A study of 29 healthy heterosexual men who were given Kisspeptin-10, or a placebo found that those who received Kisspeptin increased limbic brain activity^[4]. There is an increase in drive, reward-seeking behavior, and overall improved mood. Kisspeptin-10 peptide appears to accomplish this by integrating the emotional brain and the sexual process through the overall reproduction process. 

The Functions of Kisspeptin-10 in the Heart and Kidney

• Kisspeptin-10 and its receptors are found in numerous locations throughout the kidney and play an essential role in stimulating kidney functions, according to the findings. Clinical studies in mice lacking the Kiss1 receptor show that the peptide is critical for maintaining glomerular development during development, though whether this action is direct or indirect is unknown.
• Although the function of Kisspeptin-10 in the kidney is unknown, the peptide influences vascular development and injury responses. Kisspeptin-10 studies in mice with cardiovascular disease suggest that the peptide can act in the vascular beds, controlling vasoconstriction.
• The effects of Kisspeptin-10 on angiogenesis and vascular function can significantly impact the kidney and cardiovascular system.

The Roles of Kisspeptin-10 Peptide in Memory Enhancement

Clinical studies in mice show that Kisspeptin analogs can reverse the navigational and learning impairment caused by ethanol intoxication. Kisspeptin-10 and its analogs play an essential role in neurons encoding information and compensating for learning defects in certain genetic and chronic disease conditions. 

Kisspeptin-10 and Cancer

• Kisspeptin-10 was discovered about 20 years ago to suppress melanoma metastasis, a skin cancer, by approximately 95%, indicating that the peptide has this effect by reducing cancer cell spread. The evaluation of various metastatic cancers shows that Kisspeptin-10 levels decrease in the bladder, GI, breast, pancreatic, ovarian, thyroid, skin, and prostate, proving that the peptide plays an essential role in cancer spread.
• In 2020, an experiment on kisspeptin-10 levels under daylight exposure established a link between melatonin, kisspeptin-10, and cancer^[5]. Findings in mice models exposed to daylight confirmed high levels of Kisspeptin and low melatonin levels, and vice versa in the dark. In daylight mice, there is no increase in tumor growth rates, metastasis, or volume. Kisspeptin-10 and melatonin are implicated in tumor suppression because one influences the actions of the other, though the precise relationship is unknown.

Conclusion

Research shows that Kisspeptin-10 offers excellent subcutaneous bioavailability, and low oral bioavailability with a number of potential uses.

Disclaimer: The products mentioned are not intended for human or animal consumption. Research chemicals are intended solely for laboratory experimentation and/or in-vitro testing. Bodily introduction of any sort is strictly prohibited by law. All purchases are limited to licensed researchers and/or qualified professionals. All information shared in this article is for educational purposes only.

References

1. Jayasena CN, Nijher GM, Comninos AN, Abbara A, Januszewki A, Vaal ML, Sriskandarajah L, Murphy KG, Farzad Z, Ghatei MA, Bloom SR, Dhillo WS. The effects of kisspeptin-10 on reproductive hormone release show sexual dimorphism in humans. J Clin Endocrinol Metab. 2011 Dec;96(12):E1963-72. doi: 10.1210/jc.2011-1408. Epub 2011 Oct 5. PMID: 21976724; PMCID: PMC3232613.
2. George JT, Veldhuis JD, Roseweir AK, Newton CL, Faccenda E, Millar RP, Anderson RA. Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. J Clin Endocrinol Metab. 2011 Aug;96(8):E1228-36. doi: 10.1210/jc.2011-0089. Epub 2011 Jun 1. PMID: 21632807; PMCID: PMC3380939.
3. Navarro VM. Metabolic regulation of kisspeptin – the link between energy balance and reproduction. Nat Rev Endocrinol. 2020 Aug;16(8):407-420. doi: 10.1038/s41574-020-0363-7. Epub 2020 May 19. PMID: 32427949; PMCID: PMC8852368.
4. Comninos AN, Wall MB, Demetriou L, Shah AJ, Clarke SA, Narayanaswamy S, Nesbitt A, Izzi-Engbeaya C, Prague JK, Abbara A, Ratnasabapathy R, Salem V, Nijher GM, Jayasena CN, Tanner M, Bassett P, Mehta A, Rabiner EA, Hönigsperger C, Silva MR, Brandtzaeg OK, Lundanes E, Wilson SR, Brown RC, Thomas SA, Bloom SR, Dhillo WS. Kisspeptin modulates sexual and emotional brain processing in humans. J Clin Invest. 2017 Feb 1;127(2):709-719. doi: 10.1172/JCI89519. Epub 2017 Jan 23. PMID: 28112678; PMCID: PMC5272173.
5. Pazarci P, Kaplan H, Alptekin D, Yilmaz M, Lüleyap U, Singirik E, Pelit A, Kasap H, Yegani A. The effects of daylight exposure on melatonin levels, Kiss1 expression, and melanoma formation in mice. Croat Med J. 2020 Feb 29;61(1):55-61. doi: 10.3325/cmj.2020.61.55. PMID: 32118379; PMCID: PMC7063558.