Biological Activity Evaluation and In Silico Studies of Polyprenylated Benzophenones from Garcinia celebica

Abstract

This study aimed to isolate polyprenylated benzophenones from the rootbark of Garcinia celebica and assess their activities in vitro and in silico. The antioxidant activity was evaluated by the DPPH, ABTS, and FRAP methods. The cytotoxicity was evaluated against HeLa, MCF-7, A549, and B16 cancer cell lines. The antiplasmodial activity was performed against the chloroquine-sensitive Plasmodium falciparum strain 3D7. Molecular docking was analyzed on alpha-estrogen receptor (3ERT) and P. falciparum lactate dehydrogenase enzyme (1CET). The prediction of ADMET for the compounds was also studied. For the first time, (-)-cycloxanthochymol, isoxanthochymol, and xanthochymol were isolated from the root bark of Garcinia celebica. The antioxidant and cytotoxicity evaluation showed that all benzophenones exhibited antioxidant activity compared to gallic acid and quercetin as positive controls and also exhibited strong activity against HeLa, MCF-7, A549, and B16 cell lines compared to cisplatin as the positive control. The antiplasmodial evaluation showed that isoxanthochymol exhibited activity against the chloroquine-sensitive P. falciparum strain 3D7. In addition, the in silico molecular docking study supported in vitro activities. The ADMET analysis also indicated the isolated benzophenones are potential oral drug candidates.

Guttiferone BL from the Fruits of Allanblackia gabonensis Induces Mitochondrial‐Dependent Apoptosis in PA‐1 Ovarian Cancer Cells

“…Moreover, GBL was nontoxic towards normal ovarian epithelial cells indicating that it exhibits some cytotoxic specificity. Some previous studies revealed that several polyprenylated benzophenones found in the Clusiaceae family have potent biological activities, especially cytotoxicity against cancer cell lines [ 32 , 33 ].…”

“…Benzophenones were reported to inhibit cancer cell lines through various mechanisms of action, including apoptosis, cell cycle arrest, and endoplasmic reticulum response [ 32 ]. For instance, guttiferone E, xanthochymol, and guttiferone H isolated from Garcinia xanthochymus have shown to induce the cell cycle arrest, caspase activation associated with interference of the mitochondrial membrane potential, and the activation of the endoplasmic reticulum stress [ 34 ].…”

“…BioMed Research International studies revealed that several polyprenylated benzophenones found in the Clusiaceae family have potent biological activities, especially cytotoxicity against cancer cell lines [32,33].…”

Antidiabetic, cytotoxic and antioxidant activities of Rhodomyrtus tomentosa leaf extracts

“…DPPH (1,1-diphenyl-2-picrylhydrazyl) radicals scavenging activity was determined as previously described. 4 33.3 μL of each extract at different concentrations (159.73–4.99 μg mL −1 ) was added to 1 mL of DPPH 6.0 × 10 −5 M and the mixture were incubated at 37 °C for 20 minutes in dark room. The absorbance was measured at 517 nm using UV-visible Spectrophotometer (Thermo Fisher Scientific, USA) with three replications.…”

“…Meanwhile, cancer is one of the main causes of death in the world with about 9.6 million deaths were recorded in 2018. 4 Cancer is caused by abnormal growth of cells due to various gene mutations and unstoppable cell division. An effort in searching of effective cancer drugs becomes main research focus, as the number of new cancer cases increases per year.…”