Induction of Solasonine on Apoptosis of Human Breast Cancer Bcap-37 Cells through Mitochondria-Mediated Pathway

Objective To study the in vitro antiproliferative effect and probable mechanism of solasonine on human breast cancer Bcap-37 cells, meanwhile, make comparison with solamargine. Methods The cytotoxicity was evaluated by MTT assay. The cell damage and type of cell death were examined through Hoechst33342/PI and Annexin V/PI staining, respectively. Mitochondrial membrane potential was detected by JC-1 staining. The expression of Bcl-2, Bcl-x L, Bax, and cytochrome c was determined by immunoblot method, and the activation of caspase-3 was analyzed by immunocytochemistry method. Results Solasonine showed the different extents of cytotoxicity on eight human tumor cell lines as well as four human normal cell lines, and the IC50 values of solasonine ranged from 12.73 to 37.15 μmol/L. Cell apoptosis and mitochondria depolarization were observed in Bcap-37 cells after treatment with solasonine for 24 h, respectively. In immunoblot and immunocytochemistry analysis, solasonine obviously induced the up-regulation of Bax and down-regulation of Bcl-2 and Bcl-x L, caused the release of cytochrome c from mitochondria into cytosol, and increased the expression of both pro- and cleaved caspase-3. Solamargine exhibited stronger antipoliferative activity than solasonine, but the similar mechanism in Bcap-37 cells in this study. Conclusion Solasonine possesses the antiproliferative effect on tumor cells. Regulation of the levels of Bcl-2, Bcl-x L, Bax, and activation of mitochondria cytochrome c-dependent apoptosis pathway might be one of its main antitumor mechanisms against breast cancer cells. In view of the cytotoxic effect of solasonine and solamargine also shown on normal cells, the safety needs concern when the antitumor activity is studied.

Modification of Sugar Chains in Glycoalkaloids and Variation of Anticancer Activity

To study the effect of the sugar chains in glycoalkaloids against cancer cells, 6-0-sulfated solamargine and acidcatalyzed hydrolytic products of α-solamargine and α-solasonine were prepared. The sulfation at 0-6 of solamargine was proceeded in five steps. The 6-OH group was first selectively protected with DMT-Cl, and then the secondary hydroxyl groups on the sugar ring were acetylated. After the protective group DMTr was removed, the free 6-OH group was sulfated. Finally, the acetyl groups were removed to give 6-0-sulfated solamargine in a good yield. The hydrolyses of solamargine and solasonine were performed in diluted hydrogen chlorede. Three and two hydrolyzed products were obtained from solamargine and solasonine, respectively. The antiproliferative activities against HCT-8 tumor cells of two glycoalkaloids and their derivaties were examined via a MTT assay. The results show that α-solamargine and α-solasonine exhibit strong cytotoxic activities with an IC50 of 10. 63 and 11.97 μmol/L, respectively, wheras their derivaties seem to be less activities.

Solasodine Glycosides: A Topical Therapy for Actinic Keratosis. A Single-Blind, Randomized, Placebo-Controlled, Parallel Group Study with Curaderm^BEC5

Background: Untreated actinic keratosis can advance to squamous cell carcinoma, which in turn is associated with a risk of metastasis. Current treatments for actinic keratosis have many shortcomings. This communication describes the efficacy and safety of a topical cream therapy, CuradermBEC5, containing solasodine glycosides (0.005%) for actinic keratosis.Methods: Randomly assigned patients with actinic keratosis on the face, trunk or extremities received so-lasodine glycosides cream (CuradermBEC5) or placebo (vehicle) that was self-applied to the lesions and covered with an occlusive dressing (micropore) twice daily for 3 consecutive days. Complete clearance and local reactions were as-sessed at 56 days with follow-up periods of 6 months and 1 year. Results: The rate of complete clearance at day 56 was higher with solasodine glycosides than with placebo (92% vs. 38%, P 0.001). The absolute success rates after 1 year follow-up were 82% for solasodine glycosides and 18% for placebo. No differences in local reactions were obtained when solasodine glycosides and placebo were compared. Local reactions in both groups peaked at days 2 and 3 with local pain as the major event. The pain associated with treatments lasted approximately 10 minutes after application of solasodine glycosides and placebo. Complete reepithelialization occurred two weeks after treatment. Adverse events were generally mild to moderate in intensity and resolved without sequelae. Conclusions: Solasodine glycosides cream applied topically twice daily with a dressing for 3 days is effective for the treatment of actinic keratoses.

Topical Solasodine Rhamnosyl Glycosides Derived From the Eggplant Treats Large Skin Cancers: Two Case Reports

Solasodine rhamnosyl glycosides (BEC) are a new class of antineoplastics that show superior efficacy than many established anticancer drugs as shown by intravenous, intraperitoneal and intralesion administrations. Previous studies have described the efficacy of BEC on nonmelanoma skin cancers by topical application. Two cases are now reported which show that BEC in a cream formulation Curaderm is very effective for the treatment of large nonmelanoma skin cancers that are considered difficult to treat by existing modalities. Moreover, the cosmetic outcomes are very impressive.

Curaderm^BEC5for Skin Cancers, Is It? An Overview

Skin cancer incidence is increasing at alarming rates and is considered by some as an epidemic. Its incidence is higher than all other cancers combined. The developments of new treatments have not parallelled the increased incidences of this disease. A variety of treatments are available with differing outcomes. More recently a novel topical treatment, consisting of the antineoplastic compounds solasodine rhamnosyl glycosides, solamargine and solasonine, which are derived from plant material, has been described that claims to have many advantages over the currently used skin cancer therapies. This review investigates such claims.

Drug therapy: Solamargine and other solasodine rhamnosyl glycosides as anticancer agents

In the last century, the discovery of cytotoxic agents was revolutionary for anticancer therapy. These therapies have resulted in better understanding of cancer in general. However, the development of agents that combine efficacy, safety and convenience remains a great challenge. The narrow, if not adverse, therapeutic index of most drugs, the damage not only to cancer cells, but also to normal and healthy tissue and the occurrence of resistance have limited anticancer efficacy. This review presents the development of promising novel cytotoxic solasodine rhamnosyl glycoside drugs that offer not only gains in specificity and efficacy, but also in safety, tolerability, non-resistance and convenience in the treatment of patients with cancer.