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Geraniol

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Geraniol is a monoterpenol from rose and citronella essential oils with noteworthy endocrine actions. Assessment of its estrogenic activity has demonstrated that it has binding affinity for isolated α‐ and β‐human estrogen receptors, and can compete directly with 17β‐estradiol. However, the compound has no significant estrogenic effects, suggesting an antagonistic role and potentially making it a viable anti-estrogen in estrogen responsive tissues (1). This is further suggested in research demonstrating that geraniol is able to inhibit the inflammatory, alveoli disrupting, pulmonary vessel damaging/congesting and collagen depositing effects of the common environmental estrogenic pollutant bisphenol A (BPA) on lung tissue (2). Normal lung structure was maintained when sufficient geraniol was coadministered with BPA (2).

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Geraniol is also anti-proliferative in breast tissue (3), further exemplifying the aforementioned mechanisms, along with inhibiting proliferation in liver tissue while protecting against DNA damage (4). Geraniol has been demonstrated to target at least 38 genes affecting 'inflammatory immunoreactions and other physiological processes' (5), and has shown promise in protecting liver tissue (6) and as an anti-inflammatory and anti-pain agent (7).

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Geraniol has also been suggested to prevent the cardiovascular system by reducing serum cholesterol and triglyceride levels as well as hepatic fatty acid biosynthesis (8).

 Key references:

  • Reduced negative effects of estrogen (1,2)

  • Breast and liver protective (3,4)

  • Anti-proliferative, protects against DNA damage (4)

  • Anti-inflammatory (5,6,7)

  • Cardiovascular protection via reduced serum cholesterol and triglycerides (8)

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1 - Howes, M. J., Houghton, P. J., Barlow, D. J., Pocock, V. J., & Milligan, S. R. (2002). Assessment of estrogenic activity in some common essential oil constituents. Journal of pharmacy and pharmacology, 54(11), 1521-1528.

2 - Kattaia, A. A., & Baset, S. A. A. (2014). Effect of bisphenol A on the lung of adult male albino rats and the possible protective role of geraniol: a histological and immunohistochemical study. Egyptian Journal of Histology, 37(1), 24-35.

3 - Duncan, R. E., Lau, D., El-Sohemy, A., & Archer, M. C. (2004). Geraniol and β-ionone inhibit proliferation, cell cycle progression, and cyclin-dependent kinase 2 activity in MCF-7 breast cancer cells independent of effects on HMG-CoA reductase activity. Biochemical pharmacology, 68(9), 1739-1747.

4 - Ong, T. P., Heidor, R., de Conti, A., Dagli, M. L. Z., & Moreno, F. S. (2006). Farnesol and geraniol chemopreventive activities during the initial phases of hepatocarcinogenesis involve similar actions on cell proliferation and DNA damage, but distinct actions on apoptosis, plasma cholesterol and HMGCoA reductase. Carcinogenesis, 27(6), 1194-1203.

5 - Zhang, Y. F., Huang, Y., Ni, Y. H., & Xu, Z. M. (2019). Systematic elucidation of the mechanism of geraniol via network pharmacology. Drug design, development and therapy, 13, 1069.

6 - Jayachandran, M., Chandrasekaran, B., & Namasivayam, N. (2015). Geraniol attenuates fibrosis and exerts anti-inflammatory effects on diet induced atherogenesis by NF-κB signaling pathway. European journal of pharmacology, 762, 102-111.

7 - Murbach Teles Andrade, B. F., Conti, B. J., Santiago, K. B., Fernandes, A., & Sforcin, J. M. (2014). C ymbopogon martinii essential oil and geraniol at noncytotoxic concentrations exerted immunomodulatory/anti‐inflammatory effects in human monocytes. Journal of Pharmacy and Pharmacology, 66(10), 1491-1496.

8 - Galle, M., Kladniew, B. R., Castro, M. A., Villegas, S. M., Lacunza, E., Polo, M., & Crespo, R. (2015). Modulation by geraniol of gene expression involved in lipid metabolism leading to a reduction of serum-cholesterol and triglyceride levels. Phytomedicine, 22(7-8), 696-704.

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