Potential cytotoxic effects of Heliotropium hirsutissimum Weber in breast cancer


Gökkaya İ., Aykaç O., Özsoy C., Çiçek Polat D., Renda G.

7th International Symposium on Advances in Pharmaceutical Analysis (APA 2025) , Ankara, Türkiye, 24 Ağustos - 27 Eylül 2025, ss.103, (Özet Bildiri)

  • Yayın Türü: Bildiri / Özet Bildiri
  • Basıldığı Şehir: Ankara
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.103
  • Karadeniz Teknik Üniversitesi Adresli: Evet

Özet

Breast cancer is among the most common causes of cancer-induced mortality in women. Despite many methods of treatment, including radiation therapy, surgery, and chemotherapy, the survival rate for locally advanced and metastatic breast cancer remains low [1]. Natural products have been used for years as an essential source of raw materials in the development of safe and effective anticancer drugs with little toxicity [2].The genus Heliotropium L. (Boraginaceae) comprises about 250 species distributed in both hemispheres. The flora of Türkiye is characterized by 14 species, two of which are endemic [3]. Species of Heliotropium are documented for their application in traditional medicine for treating asthma, bronchitis, sunburn, baldness, eczema, and gastritis and as antipyretics, cholagogues, wound healers, and antiulcer agents [4]. Pyrrolizidine alkaloids, flavonoids, terpenoids, and geranyl aromatic compounds have been isolated from different parts of Heliotropium plants [3]. Previous studies have demonstrated that Heliotropium species and isolated secondary metabolites exhibit significant cytotoxic effects against several cancer cell lines. This study assessed the possible cytotoxic effect of Heliotropium hirsutissimum Weber on breast cancer for the first time.

The aerial parts of H. hirsutissimum were collected during the flowering period (Tlos Ancient City, Yakaköy, Saklikent Road,Fethiye/Muğla), and voucher specimens were prepared (Herbarium Registration number: AEF31056). The powdered aerial parts were macerated in a methanol:water mixture (70:30) for 8 hours at room temperature. The methanol extract was evaporated using a rotary evaporator at a temperature not exceeding 40 °C and under reduced pressure. The crude methanol extract (HH-M) was fractionated with n-hexane (HH-H), ethyl acetate (HH-EA), and n-butanol (HH-B), respectively. The n-hexane, ethyl acetate, and n-butanol sub-extracts and the remaining water extract (HH-W) were concentrated to dryness at 40°C. The potential cytotoxicity of crude methanol extract and its sub-extracts on estrogenreceptor-positive MCF-7 (ATCC® HTB-22TM) cells was evaluated using the MTT (3-(4.5-dimethylthiazol-2-yl)-2.5-diphenyltetrazolium bromide) assay. Healthy mouse fibroblast L929 (ATCC® CCL-1) cells were used to evaluate the selective toxic effect. Following an incubation period of 24 hours, the IC50 values for HH-M, HH-H, HH-EA, HH-B, and HH-W extracts against the MCF-7 cell line were found to be 12.25±0.02, 15.25±0.13, 22.02±0.16, 18.60±0.17, and 19.30±0.06 μg/ml, respectively. All tested extracts exhibited remarkable cytotoxic activity in estrogen receptor-positive MCF-7 cells. The crude methanol extract demonstrated the highest efficacy, with a selectivity index of 5.33. The previous research indicated that the methanol extract of Heliotropium bacciferum Moc. & Sessé ex DC. inhibited cell proliferation in the MCF-7 cell line by 55% and 50% at doses of 100 and 150 μg/mL, respectively, as determined by the MTT assay [5]. The methanol extract of Heliotropium ramosissimum Sieber ex DC. flowering aerial parts induced apoptosis and necrosis in the Colo-205 cell line, with an IC50 value of 18.60 μg/mL [6]. Similar to previous studies, this study revealed that H.hirsutissimum exhibited a cytotoxic effect. Based on the findings, investigations may be designed to clarify the mechanism of cytotoxic action of H. hirsutissimum and to isolate the compounds responsible for this activity.