Bioactive Compounds, Antioxidant, Anti-Inflammatory, Anti-Cancer, and Toxicity Assessment of Tribulus terrestris—In Vitro and In Vivo Studies

Abstract

Tribulus terrestris L. belongs to the family Zygophyllaceae and integral part of various ancient medicinal systems including Chinese, Indian, and European to combat various health ailments. The aim of the present study was to assess the phytochemical constituents, in vitro antioxidant activity using DPPH, FRAP, and H2O2 assays, in vitro anticancer activity using MTT assay, and in vitro and in vivo anti-inflammatory properties of T. terrestris. The acute and sub-acute toxicity of extracts exhibiting most biological potential was examined using murine models. Liquid–liquid partitioning followed by RP–HPLC sub-fraction of crude extract was performed. After that, ESI-MS/MS analysis was done for the timid identification of bioactive metabolites responsible for bioactivities of sub-fractions and HPLC analysis to quantify the compounds using external standards. Among all extracts, T. terrestris methanol extract was noted to hold maximum phenolic (341.3 mg GAE/g) and flavonoid (209 mg QE/g) contents, antioxidant activity in DPPH (IC50 71.4 µg/mL), FRAP (35.3 mmol/g), and H2O2 (65.3% inhibition) assays, anti-inflammatory activities in vitro at 400 µg/mL (heat-induced hemolysis, % inhibition 68.5; egg albumin denaturation, % inhibition 75.6%; serum albumin denaturation, % inhibition 80.2), and in vivo at 200 mg/kg (carrageenan-induced paw edema, % inhibition 69.3%; formaldehyde-induced paw edema, % inhibition 71.3%) and anticancer activity against breast cancer cell (MCF-7) proliferation (IC50 74.1 µg/mL). Acute and sub-acute toxicity studies recorded with no change in body weight, behavior, hematological, serum, and histopathological parameters in treated rats with T. terrestris methanol extracts when compared to control group. Fraction B obtained through liquid–liquid partitioning resulted in more bioactive potential as compared to the parent methanol extract. RP–HPLC analysis of fraction B resulted with four sub-fractions (TBTMF1-TBTMF4), wherein TBTMF3 delineated notable bioactive capabilities as compared to other fractions and parent methanol extract. ESI-MS/MS analysis of TBTMF3 resulted with tentative identification of myricetin, rutin, liquitrigenin, physcion, and protodioscin. It can be stated that T. terrestris is a potential bearing herb and findings of current study further verify the claims made in ancient medicinal systems. However, after investigation of each identified compound, it must be considered for drug discovery.

The Potential Effects of Tribulus Terrestris L. On Cellular Parameters and Steroidogenesis in Vitro

“…A varied representation of detected phenolic compounds confers certain characteristics to Tribulus. The specific content of our sample could be related to its antioxidant activity, which was discussed in a previous study (Abbas et al 2022. ) Our study evaluated antioxidant activity by DPPH scavenging method.…”

Tiliroside suppresses triple-negative breast cancer as a multifunctional CAXII inhibitor

“…Tribulus terrestris L. (TT), a plant in many regions of Asia and Africa, has been used in traditional Chinese medicine as an herb to treat breast diseases for thousands of years by the formation of oral administration decoction [ 11 ]. Nowadays, evidence has proven that the extracts of TT has many medical effects such as antihypertension, diuretic effect and cancer suppression [ 12 ].…”

“…Nowadays, evidence has proven that the extracts of TT has many medical effects such as antihypertension, diuretic effect and cancer suppression [ 12 ]. TT extracts have been found to regulate the apoptosis and metastasis of cancer cells by regulating NF-κB signaling [ 11 ]. Tiliroside ( TS , C 30 H 26 O 13 ), as a major active ingredient of TT, has been further found to possess anti-inflammatory, anticholinesterase and antioxidant activities [ 13 ].…”

Tiliroside suppresses Triple-negative breast cancer as a multifunctional CAXII inhibitor

“…Chinese Medicine as an herb to treat breast diseases for thousands of years [10]. Nowadays, evidence has proved that the extracts of TT has many medical qualities such as antihypertension, diuretic effect and cancer suppression [11].…”

“…Nowadays, evidence has proved that the extracts of TT has many medical qualities such as antihypertension, diuretic effect and cancer suppression [11]. TT extracts have been found to regulate the apoptosis and metastasis of cancer cells by regulating NF-κB signaling [10]. Tiliroside (C 30 H 26 O 13 ), as a major active ingredient of TT, has further been found to possess anti-in ammatory, anticholinesterase and antioxidant activities [12].…”