Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum induces non-selective cytotoxicity and P-glycoprotein inhibition (original) (raw)
Related papers
Journal of Natural Medicines, 2013
Natural products are some of the important sources of new anticancer drugs. The Brazilian flora is considered one of the most diverse in the word, although not many large-scale pharmacological and phytochemical studies have been conducted to date. With this in mind, in the present study we evaluated the antiproliferative activity of Solanum lycocarpum fruit glycoalkaloid extract (SL) and its major compounds, solamargine (SM) and solasonine (SS), against different tumor cell lines: murine melanoma (B16F10), human colon carcinoma (HT29), human breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), human hepatocellular liver carcinoma (HepG2) and human glioblastoma (MO59J, U343 and U251). The antiproliferative activity was evaluated using XTT assay and results were expressed as IC 50. The most pronounced antiproliferative activity was observed for SM, with IC 50 values ranging from 4.58 to 18.23 lg/mL. The lowest IC 50 values were observed against HepG2, being 9.60 lg/mL for SL, 4.58 lg/mL for SM and 6.01 lg/mL for SS. Thus, SL, SM and SS demonstrated antiproliferative activity against the tumor cell lines tested, and were most effective against the HepG2 cell line.
Anticancer agents from Solanum Surattense
2020
Two steroids glycosides solamargine (1) and dioscine (2) were isolated from methanolic extract of Solanum surattense and evaluated for their anticancer activity. The structure of the isolated compounds was identified through 1D and 2D NMR techniques, mass spectrometry and in comparison, with the literature values of their spectroscopic data. Both compounds showed the excellent anticancer activity against NIH-3T3 fibroblast cancer cell line with IC50 value of 7.55±1.5 and 3.3±1.9μg/ml respectively which were comparable with control Cyclohexamide which showed the IC50 value of 0.8± 0.2 μg/ml. A R T I C L E H I S T O R Y Received: October 15, 2019 Accepted: January 13, 2020
Impact of certain Solanum species' natural products as potent cytotoxic and anti-Inflammatory agents
The present study was conducted to evaluate both the cytotoxic and anti-inflammatory activities of ethanol extracts (T), and both n-butanol (B) and total glyco-alkaloid fractions (TGA) of Solanum seaforthianum Andr. (SS) and Solanum macrocarpon L. (SM) growing in Egypt. Cytotoxic activity was measured using sulforhodamine B (SRB) assay on prostate cancer cell line (PC-3), breast cancer cell line (MCF7), liver cancer cell line (HepG2) and human fibroblast cell line (HFB4) while anti-inflammatory activity was measured using formalin induced paw edema method. The highest cytotoxic potentiality was indicated for those of TGA fraction of S. seaforthianum Andr. on PC-3 cell line (IC 50 = 0.28µg/ml ± 0.01) followed by its activity on MCF-7 cell line (IC 50 = 2.84 µg/ml±0.20). On the other hand, the potency of TGA fractions of both species showed higher potency followed by n-butanol fractions where ethanol extracts showed lowest potency which is emphasizing the cytotoxic potentiality of the glyco-alkaloids. Based on the IC50s indicated for the different extracts and fractions on normal fibroblast cell line, considerable safety was indicated against prostate carcinoma rather than breast or hepatic carcinoma. TGA fraction of S. macrocarpon L. and of S. seaforthianum Andr. showed the highest anti-inflammatory activity with efficacy of 159 and 156%, respectively as compared to standard indomethacin. That's why the TGA fraction of S. seaforthianum Andr. was subjected for isolation of individual alkaloids using different chromatographic techniques and identified using 1 H and 13-CNMR spectroscopy beside Co-chromatography with authentic samples as solamargine (A 1), solasonine (A 2) and solasodine (A 3) which are firstly isolated from S. seaforthianum Andr. growing in Egypt.
Journal of Applied Biology & Biotechnology
Solasodine is a steroid glycoalkaloid (aglycone) found in the genus Solanum (family Solanaceae). Solanum is widely used as a traditional medicinal herb, and solasodine is documented for various pharmacological properties like antioxidant, hepatoprotective, neuroprotective, and anticancer activities. In the present study, the cytotoxic effects of solasodine extracts of in vitro cultured four Solanum species, namely, S. surattense, S. villosum, S. nigrum, and S. incanum has been assessed on two cancer lines, including Human Colorectal Adenocarcinoma cell line (HT-29), Osteosarcoma cell line (MG-63), and also on normal (Normal fibroblast L-929) cell lines in vitro. Results revealed significant cytotoxic effect on both HT-29 and MG-63 cancer cell lines, whereas very less cytotoxicity for the normal cells which indicate the major targeting of extracted solasodine on cancer cells only. Moreover, S. surattense extract found to have greater cytotoxic effect on HT-29 cells and S. nigrum extract on MG-63 cells. The results exhibited an active anti-proliferative role of solasodine extracts on colon and bone cancer cell lines which suggests the usage of these extracts as novel targeted therapy in colon and bone cancers.
2020
The current investigation was focused on the assessment of antiproliferative effects of the Solanum macranthum aqueous fruits extract against the human breast cancer cell line MDA-MB-231 in vitro. Phytochemical analysis of the S. macranthum aqueous fruits extract was performed and the phytoconstituents found positive for alkaloids, phenols, and saponins. Quantitative analysis of the total alkaloid and phenol was determined using gravimetric analysis and folins-phenols reagent method, respectively. The total alkaloid present was estimated to be 7.58% and total phenol of 158.774 mg/Gallic Acid Equivalent. The cytotoxicity of S. macranthum aqueous fruits extract was screened using 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay and camptothecin was used as standard reference drug. At the concentration of 500 μg/ml, the aqueous extract potentially inhibited the growth of the MDA-MB-231 cell line in vitro reaching 19%, and the IC50 value was calculated to be 525...
Journal of The Brazilian Chemical Society, 2002
Steroidal alkaloids, flavonoids and their glycosides occurring in numerous species of Solanum genus are known to possess a variety of biological activities. The flavonoid tiriloside (1), a rich in glycoalkaloids total fraction named GB and the glycoalkaloid solasonine (2) isolated from thricomes of young branches and fruits from Solanum crinitum Lam, and the aglycone solasodine (3) isolated from Solanum jabrense Agra & M. Nee, were assayed against murine Ehrlich carcinoma and human K562 leukaemia cultured cells. The exposure in vitro of these cancer cells to these products resulted in a dose-dependent growth inhibition evaluated by the MTT method. The results indicated significant cytotoxic activities with IC 50 = 69.50 µM, 19.5 µg mL -1 , and 74.20 µM for 1, GB and 2, respectively, against Ehrlich carcinoma, and IC 50 = 186.50 µM, 13.65 µg mL -1 and 76.92 µM, for 1, GB, 2 and 2a, respectively, against K562 leukaemia cells. The low activity of the aglycone 3 indicates that the role of the sugar moiety is very important in the cytotoxic activity of glycoalkaloid solsonine. The cytotoxic activity revealed by the GB fraction may be attributed to the presence of 2. Additionally, these results show the viability of the MTT assay for monitoring phytochemical bioactive compounds.
A novel glycosidic steroidal alkaloid from Solanum aculeastrum
Bulletin of the Chemical Society of Ethiopia, 2003
The root bark of Solanum aculeastrum Dunal yielded a new steroidal alkaloid glycoside characterised as (25R)-3β-{O-α-L-rhamnopyranosyl-(1→2)-[O-β-D-glucopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranosyl}-22α-N-spirosol-5-ene. The structure was established by spectroscopic analysis and comparison with published data of similar compounds reported in literature.
International Journal of Pharmacy and Pharmaceutical Sciences, 2020
Objective: The present study was aimed to determine the cytotoxicity concentration (CTC50) of different extracts made from the leaf and stem bark of an ethno botanically selected S. pubescens against Human liver carcinoma (Hep G2), Human colon carcinoma (CaCo2 Methods: Ethnobotanical survey was done through interviewing traditional medicinal practitioners then a potential herbal plant was selected after a thorough literature survey and its identity was confirmed. The soxhlet extraction method was adopted using five different solvents from leaf and stem bark powders of the study plant and the CTC) and Human breast cancer (T-47 D) cell lines. 50 Results: Among the different extracts, CTC of all the extracts were determined by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay method. 50 Conclusion: The major findings of the present study clearly provides evidence that the leaf and stem bark of S. pubescens possesses the potential anticancer bioactive compound solasodine. values were significant for stem bark extracts made from methanol (24.51±0.08 µg/ml) against Hep G2, while leaf chloroform extract was promising (57.15±1.75 µg/ml) against CaCo2 and n-hexane extract of leaf exhibited significant value (20.27±1.52 µg/ml) against T-47 D cancer cell lines.
Chemistry & Biodiversity, 2013
Leishmaniasis is an infection caused by a protozoan parasite of the genus Leishmania and is the second most prevalent parasitic protozoal disease after malaria in the world. We report the in vitro leishmanicidal activity on promastigote forms of Leishmania amazonensis and cytotoxicity, using LLCMK 2 cells, of the glycoalkaloids from the fruits of Solanum lycocarpum, determined by colorimetric methods. The alkaloidic extract was obtained by acid-base extraction; solamargine and solasonine were isolated by silica-gel chromatography, followed by reversed-phase HPLC final purification. The alkaloidic extract, solamargine, solasonine, as well as the equimolar mixture of the glycoalkaloids solamargine and solasonine displayed leishmanicidal activity against promastigote forms of L. amazonensis, whereas the aglycone solasodine was inactive. After 24 and 72 h of incubation, most of the samples showed lower cytotoxicities (IC 50 6.5 to 124 mm) as compared to leishmanicidal activity (IC 50 1.1 to 23.6 mm). The equimolar mixture solamargine/solasonine was the most active with an IC 50 value of 1.1 mm, after 72 h. Likewise, solamargine was the most active after 24 h with an IC 50 value of 14.4 mm, both in comparison with the positive control amphotericin B.
Cytotoxicity of Solanum nigrumL green fruits on breast (MCF-7) and liver (HepG-2) cancer cell lines
Medicinal plants have been used for decades for the treatment of different diseases. Solanum nigrumL is an important medicinal plant in many traditional health care systems. It has been used for the management of liver disorders, diabetes, infections, cancer, inflammations and peptic ulcer. In the present study, we screened the green unripe S. nigrumL fruits and leaves for their cytotoxic activity. The ethanolic extract of green fruits revealed a marked cytotoxicity against breast (MCF-7) and liver (HepG-2) cancer cell lines with IC50of 12.7 and 16.6 µg/mL, respectively. This activity is related to the high content of steroidal glycoalkaloids in S. nigrumL unripe green fruits.