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. 2024 Feb 21;24(1):96.
doi: 10.1186/s12906-024-04394-5.

Chili pepper extracts, capsaicin, and dihydrocapsaicin as potential anticancer agents targeting topoisomerases

Terézia Hudáková #  1 , Martina Šemeláková #  1 , Peter Očenáš  2 , Mária Kožurková  3 , Kristína Krochtová  3 , Simona Sovová  3 , Zuzana Tóthová  1 , Zuzana Guľášová  4 , Peter Popelka  5 , Peter Solár  6
Affiliations

Chili pepper extracts, capsaicin, and dihydrocapsaicin as potential anticancer agents targeting topoisomerases

Terézia Hudáková et al. BMC Complement Med Ther. .

Abstract

DNA topoisomerases regulate conformational changes in DNA topology during normal cell growth, such as replication, transcription, recombination, and repair, and may be targeted for anticancer drugs. A DNA topology assay was used to investigate DNA-damaging/protective activities of extracts from Habanero Red (HR), Habanero Maya Red (HMR), Trinidad Moruga Scorpion (TMS), Jalapeno (J), Serrano pepper (SP), Habanero Red Savina (HRS), Bhut Jolokia (BJ), and Jamaica Rosso (JR) peppers, demonstrating their inhibitory effect on the relaxation of pBR by Topo I. DNA topoisomerase II (Topo II) is proven therapeutic target of anticancer drugs. Complete inhibition of Topo II was observed for samples TMS, HR, and HMR. Extracts J and SP had the lowest capsaicin and dihydrocapsaicin content compared to other peppers. HR, HMR, TMS, J, S, HRS, BJ, JR extracts showed the anticancer effect, examined by MTS and xCell assay on the in vitro culture of human colon carcinoma cell line HCT116.

Keywords: Capsaicin; Chili pepper extract; Dihydrocapsaicin; Topoisomerases inhibition.

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Conflict of interest statement

The authors declare no competing interests.

Figures

Fig. 1
Fig. 1
Nuclease activity. Nuclease activity of selected molecules were studied on isolated plasmid pUC19 and chili extracts in final concentration 1/10 of stock solution incubated at 37 °C for 18 hrs. Compounds of extract: HR – Habanero Red; HMR – Habanero Maya Red; TMS – Trinidad Moruga Scorpion; J – Jalapeno; SP – Serrano pepper; HRS – Habanero Red Savina; BJ – Bhut Jolokia; JR – Jamaica Rosso (final concentration 1/10 of stock solution); CAP – capsaicin (final concentration 0,05 mg/mL); DHK – dihydrocapsaicin (final concentration 0,05 mg/mL); K1 – pUC19; K2 – pUC19 + EtOH
Fig. 2
Fig. 2
Decatenation assay for topoisomerase II. Topoisomerase II decatenation assay was carried out using kinetoplast DNA (kDNA, 200 ng) in human topoisomerase IIa (hTop IIa, 1.5 U) enzyme, in 1/10 of stock solutions (3 μL from extracts, capsaicin 0.5 mg/mL and 1.0 mg/mL). Extracts: HR – Habanero Red; HMR – Habanero Maya Red; TMS – Trinidad Moruga Scorpion; J – Jalapeno; SP – Serrano pepper; HRS – Habanero Red Savina; BJ – Bhut Jolokia; JR – Jamaica Rosso (final concentration 1/10 of stock solution); CAP 1 – capsaicin (final concentration 0.05 mg/mL); CAP 2 – capsaicin (final concentration 0.1 mg/mL); DHK – dihydrocapsaicin (final concentration 0.05 mg/mL); K1 – kDNA; K2 – kDNA + Topo II (1.5 U) + EtOH
Fig. 3
Fig. 3
Relaxation assay for topoisomerase I. TMS – Trinidad Moruga Scorpion (final concentration 1/10 of stock solution); CAP – capsaicin (final concentration 0.05 mg/mL); DHK – dihydrocapsaicin (final concentration 0.05 mg/mL); K1 – pBR322; K2 – pBR322 + topo I (0.5 U); K3 – EtOH
Fig. 4
Fig. 4
Relaxation assay for topoisomerase I. HR – Habanero Red; HMR – Habanero Maya Red; TMS – Trinidad Moruga Scorpion; J – Jalapeno; SP – Serrano pepper; HRS – Habanero Red Savina; BJ – Bhut Jolokia; JR – Jamaica Rosso (final concentration 1/10 of stock solution); CAP 1 – capsaicin (final concentration 1/10 of stock solution 0.05 mg/mL); CAP 2 – capsaicin (final concentration 0.1 mg/mL); DHK – dihydrocapsaicin (final concentration 0,05 mg/mL); K1 – pBR322; K2 – pBR322 + Topo I (1.0 U); K3 – pBR322 + Topo I + EtOH
Fig. 5
Fig. 5
MTS Analysis. MTS analysis of cell viability at 48 and 72 hrs upon treatment with chili extracts (HR, HMR, TMS, J, S, HRS, BJ, JR) and capsaicin (CAP), dihydrocapsaicin (DHK) in different concentrations cultivated with HCT116 cells. The extracts of peppers HR, HMR, TMS, J, SP, HRS, BJ, JR. Control group (cells HCT116) was not affected by extracts, Cap1 - Cap6 concentrations of CAP at 10 μM, 25 μM, 50 μM, 100 μM, 150 μM, 200 μM. DHK1 - DHK6 concentrations of DHK at 10 μM, 25 μM, 50 μM, 100 μM, 150 μM, 200 μM. MTS analysis expressed as a fold of control [%] of absorbance generated in cell-mediated MTS assays to control group. Absorbance values are obtained from three independent experiments (n = 3 for each group) and values are expressed in mean ± SE. The groups treated with extracts alone were compared with control: * p < 0.05, **p < 0.01, ***p < 0.001. * vs Ctrl, ▲ vs HR and each extract mutually at both analyzed times (48 hrs, 72 hrs). Statistically insignificant [ns]: CAP1 vs DHK1, HR vs DHK3 at 48 hrs; CAP1 vs DHK1, BJ vs CAP3, HR vs DHK3, HRS vs JR at 72 hrs
Fig. 6
Fig. 6
xCell proliferation. HCT116 cells (Ctrl) seeded in plates (RTCA E-Plates 96) were treated with 100 μM chilli extracts 24 hrs after seeding. The cell adhesion and spread were monitored over 90 hrs using the ×CELLigence RTCA system (Agilent). HRS and JR extracts (CAP content (362.57 and 343.40 μg/ml) increased cell proliferation during 30-50 hrs of culture
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