Sains Malaysiana 50(2)(2021): 449-460

http://dx.doi.org/10.17576/jsm-2021-5002-16

Polarity Difference and the Presence of Phytoestrogen Compounds Affecting Estrogenic Activity of Peperomia pellucida Extracts

(Perbezaan Kekutuban dan Kehadiran Sebatian Fitoestrogen yang Mempengaruhi Aktiviti Estrogen Ekstrak Peperomia pellucida)

I GUSTI AGUNG AYU KARTIKA¹, MUHAMAD INSANU¹, CATUR RIANI¹, KYU HYUCK CHUNG², I KETUT ADNYANA¹*

¹School of Pharmacy, Bandung Institute of Technology, 40132, Bandung, Indonesia

²School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea

Received: 16 November 2019/Accepted: 6 July 2020

ABSTRACT

Peperomia pellucida (L.) Kunth has been studied as an anti-osteoporotic agent. However, there is no report about its estrogenic activity, which is important for its anti-osteoporotic activity. Thus, the aim of this research was to study the estrogenic potency of P. pellucida extract. The estrogenic activity of P. pellucida extracts (n-hexane, ethyl acetate, ethanol, and water extracts) was studied using E-screen assay and confirmed with a molecular docking simulations. Further, the presence of phytoestrogen compounds was identified using thin layer chromatography (TLC), TLC densitometry, and high-performance liquid chromatography. The n-hexane, ethyl acetate, and ethanol extracts at a concentration of 0.1 µg mL^-1 exhibited a partial agonist effect, whereas the water extract showed full agonist effect at the similar concentration. This activity was produced through a classical ligand-dependent mechanism similar to estradiol. All of the extracts also showed antiestrogenic activity. The TLC chromatogram evidently depicted the presence of quercetin and stigmasterol in the n-hexane and ethyl acetate extracts. Apigenin and apigetrin at concentrations of 0.239±0.076 and 1.063±0.156 µg mg^-1 extract, respectively, were present in the water extract. A docking study on estrogen receptors confirmed that apigetrin prefer to produce estrogenic activity, whereas the other compounds can produce both estrogenic and antiestrogenic activity. Hence, we suggest that the bioactive compounds in the water extract are flavonoids, such as apigenin and apigetrin. In summary, the water extract is recommended to be used as an estrogenic agent.

Keywords: Apigenin; apigetrin; docking; estrogenic; extract; Peperomia pellucida

ABSTRAK

Peperomia pellucida (L.) Kunth telah dikaji sebagai agen anti-osteoporosis. Walau bagaimanapun, tiada laporan mengenai aktiviti estrogennya yang penting untuk aktiviti anti-osteoporosisnya. Oleh itu, tujuan penyelidikan ini adalah untuk mengkaji potensi estrogen ekstrak P. pellucida. Aktiviti estrogen ekstrak P. pellucida (n-heksana, etil asetat, etanol dan ekstrak air) telah dikaji dengan menggunakan ujian E-screen dan disahkan dengan simulasi dok pengimejan. Selanjutnya, sebatian fitoestrogen telah dikenal pasti menggunakan kromatografi lapisan tipis (KLT), KLT densitometri dan kromatografi cecair prestasi tinggi. Ekstrak n-heksana, etil asetat dan etanol pada kepekatan 0.1 μg mL^-1 menunjukkan kesan agonis separa, manakala ekstrak air menunjukkan kesan agonis penuh pada kepekatan yang sama. Aktiviti ini dihasilkan melalui mekanisme ligan klasik yang sama seperti estradiol. Semua ekstrak juga menunjukkan aktiviti antiestrogenik. Kromatogram KLT jelas menggambarkan kehadiran quersetin dan stigmasterol dalam ekstrak n-heksana dan etil asetat. Apigenin dan apigetrin masing-masing pada kepekatan 0.239±0.076 dan 1.063±0.156 μg mg^-1 ekstrak, hadir dalam ekstrak air. Kajian dok mengenai reseptor estrogen mengesahkan bahawa apigenin dan apigetrin lebih suka menghasilkan aktiviti estrogenik, sedangkan quersetin dan stigmasterol dapat menghasilkan kedua-dua aktiviti estrogenik dan antiestrogenik. Oleh itu, kami mencadangkan bahawa sebatian bioaktif dalam ekstrak air adalah flavonoid, seperti apigenin dan apigetrin. Ringkasnya, ekstrak air disyorkan untuk digunakan sebagai agen estrogen.

Kata kunci: Apigenin; apigetrin; dok; ekstrak; estrogen; Peperomia pellucida

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*Corresponding authors; email: ketut@fa.itb.ac.id