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. 2022 Sep 18;27(18):6101.
doi: 10.3390/molecules27186101.

Bioactive Potential: A Pharmacognostic Definition through the Screening of Four Hypericum Species from the Canary Islands

Rodney Lacret  1   2 , Adrián Puerta  1 , Sebastian Granica  3 , Aday González-Bakker  1 , Danela Hevia  1 , Yiling Teng  1 , Candelaria C Sánchez-Mateo  2 , Pedro Luis Pérez de Paz  4 , José M Padrón  1
Affiliations

Bioactive Potential: A Pharmacognostic Definition through the Screening of Four Hypericum Species from the Canary Islands

Rodney Lacret et al. Molecules. .

Abstract

In this work, we propose a general methodology to assess the bioactive potential (BP) of extracts in the quest of vegetable-based drugs. To exemplify the method, we studied the anticancer potential (AP) of four endemic species of genus Hypericum (Hypericum canariense L, Hypericum glandulosum Aiton, Hypericum grandifolium Choisy and Hypericum reflexum L.f) from the Canary Islands. Microextracts were obtained from the aerial parts of these species and were tested against six human tumor cell lines, A549 (non-small-cell lung), HBL-100 (breast), HeLa (cervix), SW1573 (non-small-cell lung), T-47D (breast) and WiDr (colon). The methanol-water microextracts were evaluated further for cell migration, autophagy and cell death. The most promising bioactive polar microextracts were analyzed by UHPLC-DAD-MS. The extraction yield, the bioactivity evaluation and the chemical profiling by LC-MS suggested that H. grandifolium was the species with the highest AP. Label-free live-cell imaging studies on HeLa cells exposed to the methanol-water microextract of H. grandifolium enabled observing cell death and several apoptotic hallmarks. Overall, this study allows us to select Hypericum grandifolium Choisy as a source of new chemical entities with a potential interest for cancer treatment.

Keywords: Hypericum canariense; Hypericum glandulosum; Hypericum grandifolium; Hypericum reflexum; anticancer potential; bioactive potential; screening; total activity.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Workflow procedure for the preparation of microextracts from aerial parts of Hypericum species from the Canary Islands.
Figure 2
Figure 2
Antiproliferative activity (GI50) of microextracts from Hypericum species. MW = methanol–water; MM = methanol; DM = dichloromethane–methanol.
Figure 3
Figure 3
Total activity (GI50) of microextracts from Hypericum species.
Figure 4
Figure 4
Wound closure assay results on A549 cells when using 100 µg/mL (a) and 50 µg/mL (b) of MW microextracts. Wound closure percentage with respect to time = 0 is given on the right top corner of each image.
Figure 5
Figure 5
(a) Relative fluorescence units (RFU) compared to control. HeLa cells were treated for 24 h with 100 µg/mL of each extract. (b–d). Representative images of fluorescence microscopy after 24 h of incubation with 10 µM of TAM and 100 µg/mL of GMW. Captured images in green and red were merged using ImageJ.
Figure 6
Figure 6
Anticancer potential of MW microextracts from Hypericum species.
Figure 7
Figure 7
Live-cell imaging study on HeLa cells. (a) Representative images of the experiments for untreated (control) cells and cells exposed to 10 µM TAM or 100 µg/mL GMW. (b) Images of cell vacuolization after treatment with GMW for 5 h. Yellow arrows indicate cytoplasmic vacuoles observed. (c) Confluency, Mean Cell Area and Average Dry Mass Density obtained with STEVE software based on refractive indices resulting from CX-A observation over time. Green: untreated cells. Yellow: TAM (10 µM). Blue: GMW (100 µg/mL).
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