ABSTRACT
Ruta chalepensis is an herb used to treat various ailments, and its potential cytotoxic effects on different tumor cell lines have been extensively studied. The present study aimed to evaluate the cytotoxic activity of R. chalepensis methanol extract (RCME), sub-partitions obtained from solvents of increasing polarity, and major compounds, as well as their hemolytic, anti-hemolytic, and antioxidant potential. The in vitro cytotoxic activity against the human hepatocarcinoma (HEP-G2) and the murine lymphoma cell line (L5178Y-R) was evaluated using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay, whereas selectivity indices (SIs) were determined by comparing cytotoxicity against normal African green monkey kidney cells (VERO) and human peripheral blood mononuclear cells (PBMC). Hemolytic and anti-hemolytic activities were evaluated on human erythrocytes. The most effective cytotoxic treatment was evaluated for nitric oxide release by J774A.1 macrophages. Antioxidant activity of R. chalepensis material was also determined. Results showed that RCME produced significant (p < 0.05) cytotoxicity in HEP-G2 (IC50 = 1.79 µg/mL) and L5178Y-R (IC50 = 1.60 µg/mL) cells and exhibited high SIs (291.50 and 114.80, respectively). In addition, the n-hexane fraction (RCHF) showed an IC50 of 18.31 µg/mL in HEP-G2 cells and an SI of 9.48 in VERO cells, whereas the chloroform fraction (RCCF) evidenced an IC50 of 1.60 µg/mL in L5178Y-R cells and an SI of 34.27 in PBMC cells. Chalepensin (CHL), rutamarin (RTM), and graveolin (GRV), which are major components of R. chalepensis, showed high activity against L5178Y-R cells, with IC50 of 9.15, 15.13 and SI of 45.08 µg/mL, respectively. In addition, CHL, RTM, and GRV showed SIs of 24.76, 9.98, and 3.52, respectively, when compared with PBMC cells. RCME at concentrations of 125 µg/mL and 250 µg/mL, significantly (p < 0.05) decreased nitrite production in J774A.1 cells, when exposed to lipopolysaccharide. This study demonstrated that RCME showed significant cytotoxic activity against HEP-G2 and L5178Y-R cells, without affecting normal VERO, PBMC, and J774A.1 cells.
ABSTRACT
Cancer is a major health problem with significant morbidity and mortality. In addition, plants are a source of metabolites with diverse biological properties, including antitumor potential. In this study, we investigated the in vitro murine lymphoma L5178Y-R cell growth inhibition, human peripheral blood mononuclear cells (PBMC) toxicity and proliferation, and antioxidant, hemolytic, and anti-hemolytic activities of methanol extracts from 15 plants of traditional use in Mexico. Justicia spicigera caused the highest tumor cell growth inhibition with a half maximal inhibitory concentration (IC50) of 29.10 µg/mL and a selectivity index >34.36 compared with those of PBMC, whereas Mimosa tenuiflora showed the highest lymphoproliferative activity from 200 µg/mL compared with that induced by concanavalin A. In addition, M. tenuiflora showed an antioxidant effect (IC50 = 2.86 µg/mL) higher than that of ascorbic acid. Regarding the hemolytic and anti-hemolytic activity, all extracts presented significant anti-hemolytic activity. The extract of J. spicigera is emerging as a possible source of effective antineoplastic compounds.
ABSTRACT
Medicinal plants are traditionally used in Mexico to treat diseases such as cancer. The present study aimed to evaluate the cytotoxic, antioxidant, and anti-hemolytic activity of 15 plants of ethnopharmacological use in Mexico. For this, plant methanol extracts were prepared by the Soxhlet method, after which their cytotoxic activity was evaluated against human hepatocellular carcinoma (HEP-G2) and monkey kidney epithelial (Vero) cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction colorimetric assay. The selectivity index (SI) of each extract was then determined by the IC50 ratio of normal to tumor cells. We showed that Ruta chalepensis extract possessed an IC50 of 1.79 µg/mL and 522.08 µg/mL against HEP-G2 and Vero cells, respectively, resulting in an SI of 291.50. Furthermore, antioxidant activity was evaluated by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging technique, where the best antioxidant potential was shown by the Heterotheca inuloides extract (IC50 = 19.24 µg/mL). Furthermore, the hemolytic potential was determined against human erythrocytes, which showed that the extracts with the highest anti-hemolytic activity were Smilax aspera (IC50 = 4.41 µg/mL) and Amphipterygium adstringens (IC50 = 5.35 µg/mL). In conclusion, we observed that R. chalepensis methanol extract possesses cytotoxic activity against HEP-G2 cells, without affecting non-tumorigenic Vero cells. Our results indicated the antitumor potential of medicinal plants used in Mexico.
