Antimalarial compounds against polycystic ovary syndrome?

Polycystic ovary syndrome is one of the most common endocrine disorders affecting women of reproductive age. It is characterized by elevated levels of androgens (hyperandrogenemia) and is associated with a wide range of health impacts, including metabolic dysfunction, impaired ovulation, and often infertility.

However, despite the high prevalence of the syndrome, the mechanistic basis of PCOS has been poorly understood and pharmacological treatments often focus only on specific symptoms with limited effectiveness.

Since hyperandrogenemia is the main feature and the cause of most of the symptoms and comorbidities associated with PCOS, treatments aimed at suppressing androgen production could be beneficial for its treatment.

A team led by Yang Liu of Fudan University in Shanghai, China, evaluated the effect of artemisinin and its derivatives on the development of polycystic ovary syndrome.

Although artemisinin and its derivatives are best known for their antimalarial effects, these compounds have also been shown to have beneficial metabolic effects.

In rodent models, Liu and colleagues found that artemether (ATM), an artemisinin derivative isolated from the plant genus Artemisia, reduces ovarian androgen synthesis by targeting CYP11A1, a crucial enzyme in androgen production. ATM induces the degradation of CYP11A1 by increasing its interaction with the LONP1 protease.

Furthermore, the study authors found that overexpression of LONP1 suppresses ovarian androgen production.

Finding additional uses for medications that have already been approved to treat other health problems is a faster way to introduce a new treatment into healthcare than the typical way of creating a completely new drug and having to subject it to countless tests to prove that its consumption is safe for humans. (Photo: Amazings/NCYT)

In a pilot clinical trial with 19 women with polycystic ovary syndrome, Liu and colleagues further demonstrated the therapeutic potential of artemisinin. A 12-week regimen of dihydroartemisinin, a drug used to treat malaria, in these women substantially reduced key biomarkers of PCOS and led to more regular menstrual cycles without side effects.

The study is titled “Artemisinins ameliorate polycystic ovarian syndrome by mediating LONP1-CYP11A1 interaction.” And it has been published in the academic journal Science. (Source: AAAS)