Erythrina abyssinica Lam. is an important medicinal plant growing in Sudan; its seeds were investigated for the first time for their alkaloidal constituents and biological activity. The in vitro cytotoxicity of the crude alkaloidal fraction (CAF) against the cell lines HeLa, Hep-G2, HEP-2, HCT116, MCF-7 and HFB4 showed promising activity, with IC₅₀ values of 13.8, 10.1, 8.16, 13.9, 11.4 and 12.2 µg mL⁻¹, respectively. Doxorubicin (positive control) showed in vitro cytotoxic activity with IC₅₀ values 3.64, 4.57, 4.89, 3.74, 2.97 and 3.96 µg mL⁻¹, respectively. Bioassay-guided fractionation and isolation of the CAF led to the isolation of five Erythrina alkaloids, identified as erythraline, erysodine, erysotrine, 8-oxoerythraline and 11-methoxyerysodine. These were evaluated for their in vitro cytotoxic activity against Hep-G2 which resulted in IC₅₀ values 17.60, 11.80, 15.80, 3.89 and 11.40 µg mL⁻¹, respectively. Furthermore, in vitro cytotoxic activity against HEP-2 was evaluated, which resulted in IC₅₀ values 15.90, 19.90, 21.60, 18.50 and 11.50 µg mL⁻¹, respectively. The CAF caused a reduction in the viability of mock-infected MT-4 cells with a CC₅₀ of 53 µM and a 50% protection of MT-4 cells against HIV-1 induced cytopathogeneticy with a EC₅₀ of >53 µM, compared with EFV as a positive control, which had a CC₅₀ of 45 µM and an EC₅₀ of 0.003 µM. We concluded that the isolated alkaloids were responsible for the anti-carcinogenic [corrected] actions of the plant extract previously reported in the literature.
Naturally occurring anti-mutagenic principles present in plants, human diet and other sources have protective effects against mutagens. Anthraquinones (AQs) considered one of the major plant phenolic pigments that contain many members, have evidenced the capability for inhibiting the mutagenicity toward Salmonella typhimurium of a number of mutagens. Not only genotoxicity/carcinogenesis is caused by mutagens but also the inception and pathogenesis of several chronic degenerative diseases. The present review attempts to furnish a brief overview on structure-antimutagenicity relationships of natural and synthetic anthraquinones.
Leaves of Ixora undulata Roxb. were investigated phytochemically for the first time for its alkaloidal content, which resulted in the isolation of a novel unusual thiazepine alkaloid glycoside identified as 7-[(β-D-glucopyranosyl)oxy]-6-hydroxy-2-methoxy-4,5-dihydro-1,3-thiazepine and trivially named as Rubiothiazepine. Its structure was determined on the basis of 1D and 2D NMR ( 1 H-, 13 C-NMR, 1 H-1 H COSY, 1 H-13 C HETCOR, 1 H-13 C HMBC, 1 H-15 N HMBC and DIFNOE), high resolution ESI-CID-MS/MS, UV and IR spectroscopy. The isolated compound showed cytotoxic activity against EL 4 (Murine Leukemia) with IC 50 >100 µg/mL, and also showed cytotoxic and HIV-1 activity against MT-4 and HIV-1IIIB with CC 50 >100 µg/mL and EC 50 >100 µg/mL, respectively.
Background Trichinellosis is a public health threat infected both animals and humans as a result of eating undercooked meat. It caused by Trichinella spiralis that has widespread drug resistance and even developed many sophisticated strategies for their survival, this increases the demand in searching for new anthelmintic drugs from natural source. Methods Our objectives were to test the in vitro and in vivo anthelmintic activity of Bassia indica BuOH frac., and to characterize its chemical composition using UPLC-ESI–MS/MS. Besides an in silico molecular docking study with the prediction of the PreADMET properties. Results In vitro investigation of B. indica BuOH frac., showed severe destruction of the adult worm and larvae, marked cuticle swelling, areas with vesicles, blebs and loss of annulations. This was assured via in vivo study, which revealed a significant reduction (P < 0.05) in the mean adult worm count with efficacy of 47.8% along with a significant decrease (P < 0.001) in the mean larval count per gram muscle with efficacy 80.7%. Histopathological examinations of the small intestine and muscular sections showed marked improvement. In addition, immunohistochemical findings demonstrated that B. indica BuOH frac. depressed the proinflammatory cytokines expressions of TNF-α, which was obviously upregulated by T. spiralis. Precise chemical investigation of the BuOH frac. using UPLC-ESI–MS/MS resulted in the identification of 13 oleanolic type triterpenoid saponins; oleanolic acid 3-O-6´-O-methyl-β-D-glucurono-pyranoside (1), chikusetsusaponin-IVa (2) and its methyl ester (3), chikusetsusaponin IV (4) and its methyl ester (5), momordin-Ic (6) and its methyl ester (7), betavulgaroside-I (8), -II (9) -IV (10), -X (11), licorice-saponin-C2 (12) and -J2 (13). In addition, 6 more phenolics were identified as syringaresinol (14), 3,4-di-O-caffeoylquinic acid (15), 3-O-caffeoyl-4-O-dihydrocaffeoylquinic acid (16), 3,4-di-O-caffeoylquinic acid butyl ester (17), 3,5-di-O-galloyl-4-O-digalloylquinic acid (18) and quercetin 3-O-(6´´-feruloyl)-sophoroside (19). The auspicious anthelmintic activity was further ascertained using in silico molecular docking approach that targeted certain protein receptors (β-tubulin monomer, tumor necrosis factor alpha (TNF-α), cysteine protease (Ts-CF1), calreticulin protein (Ts-CRT)), all the docked compounds (1–19) fit into the binding site of the active pocket with binding affinities noteworthy than albendazole. In addition, ADMET properties, drug score and drug likeness were predicted for all compounds.
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