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solasodine Glycosides: A Topical Therapy for Actinic Keratosis. A Single-Blind, Randomized, Placebo-Controlled, Parallel Group Study with CuradermBEC5

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Journal of Cancer Therapy 2013年第2期4卷 588-596页

作者： Bill E. Cham Australasian Institute of Medical Research Brisbane Australia.

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 ***: 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.

关键词： solasodine Glycosides Solamargine Solasonine Actinic Keratosis Apoptosis Skin Cancer Clinical Trial CuradermBEC5

solasodine Glycosides from the Eggplant in a Topical Cream PsorendBECAre Effective against Psoriasis

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International Journal of Clinical Medicine 2019年第3期10卷 174-182页

作者： Tania R. Chase Kai E. Cham Bill E. Cham Australasian Medical Research Port Vila Republic of Vanuatu

Background: Psoriasis is a chronic disease that can have significant effects on quality of life. Aim: To test whether the antineoplastic, antipathogenic plant derived secondary metabolites, solasodine glycosides, can treat psoriasis. Case Presentation: We report a case of a 54-year-old French-Vietnamese male who presented with diagnosed erythematous scaly annular recalcitrant psoriasis scattered throughout his body. Method: After failing conventional treatment regimens for over 10 years the patient received a trial with a topical cream formulation PsorendBEC, containing solasodine glycosides, for his psoriasis. Result: Topical applications of PsorendBEC twice daily resulted in complete resolution of cutaneous lesions after 4 weeks of treatment with no recurrence post 1 year after therapy. Conclusion: Topical PsorendBEC therapy rapidly removes recalcitrant psoriasis with no apparent side effects.

关键词： Psoriasis BEC solasodine Glycosides PsorendBEC Eggplant Devil’s Apple Black Nightshade

Treatment of Skin Cancer with a Selective Apoptotic-Inducing CuradermBEC5Topical Cream Containing solasodine Rhamnosides

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International Journal of Clinical Medicine 2015年第5期6卷 326-333页

作者： Aruba Cham Bill Cham Australasian Medical Research Port Vila Republic of Vanuatu

solasodine rhamnosides produced in plants as secondary metabolites, are safe and effective when treating a variety of cancers, including non-melanoma skin cancers. They are cytotoxic against multi-drug resistant tumor cells, stimulate lasting immunity against cancer, are not mutagenic and display anti-mutagenic properties. These antineoplastics, through cellular specific receptor-mediated actions, directly induce apoptosis by triggering extrinsic and intrinsic apoptotic pathways in cancer cells but not normal cells. CuradermBEC5 contains solasodine rhamnosides and is a topical formulation for the treatment of keratoses and non-melanoma skin cancers. The mode of action, together with the selectivity towards cancer cells, with CuradermBEC5 therapy, results in outstanding beneficial outcomes. This study shows graphically and pictorially that CuradermBEC5 seeks and destroys basal cell carcinoma whilst normal skin cells replace the dead cancer cells during therapy, emanating into impressive cosmetic end results. The clinical observations with CuradermBEC5 therapy reveal that initially the lesion size increases over four-fold due to the interaction of CuradermBEC5 with deeper and more lateral tumor cells, followed by a decrease in size, ultimately, resulting in complete elimination of the basal cell carcinoma.

关键词： Skin Cancer BEC Solamargine Curaderm Apoptosis solasodine Rhamnosides

solasodine induces apoptosis and inhibits metastasis on ovarian cancer HEY cells

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中国药理学通报 2015年第B11期31卷 240-240页

作者： XUXiao-huang ZHANGLe-le WUGuo-zheng LuJin-jian StateKeyLaboratoryofQualityResearchinChineseMedicine InstituteofChineseMedicalSciencesUniversityofMacauMacao

Aim solasodine, a steroidal alkaloid isolated from solanaceous species, has been reported to exhibit anticancer activity on several cell lines. The aim of this study is to explore the antitumor potential of solasodine on ovarian cancer HEY cells. Methods MTT assay, Hoechst 33342 staining, JC-1 mitochondrial membrane potential assay, and LDH release assay were used to study the anti-proliferative and apoptosis-inducing effects of solasodine. MDC staining was to label the acidic puncta in the cells. Meanwhile, wound healing assay and transwell assay were performed to determine whether solasodine exhibits anti-metastasis effect on HEY cells. Gelatin zymography assay was used to determine the activities of MMP-2 and MMP-9 and Western blot was used to examine the expression of the relevant proteins. Results solasodine inhibited the cell viability on HEY cells in time- and dose-dependent manners, causing shrinking of nuclei, damage of cell membrane, and appealing apoptotic body on high dosage and reducing cell mitochondrial membrane potential. It also inhibited autophagic flux that interfere autolysosome degra- dation. Furthermore, solasodine suppressed the migration and invasion abilities of HEY cells ascribable to down- regulating the expression and attenuating the activities of MMP-2 and MMP-9. Conclusion The inducing apoptosis and anti-metastasis activity of solasodine on HEY cells suggest it appears certain potential on ovarian cancer treat- ment.

关键词： ovarian cancer solasodine apoptosis autophagy migration invasion

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

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Modern Chemotherapy 2013年第2期2卷 33-49页

作者： Bill E. Cham Australasian Institute of Medical Research Brisbane Australia

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.

关键词： Cancer Skin Cancer Solamargine Solasonine BEC solasodine Rhamnosyl Glycosides CuradermBEC5 Apoptosis Antineoplastic Targeted Therapy

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

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International Journal of Clinical Medicine 2011年第4期2卷 473-477页

作者： Bill E. Cham 不详

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.

关键词： Nonmelanoma Skin Cancers solasodine Rhamnosyl Glycosides Curaderm Solamargine Solasonine

具有抗肿瘤活性的solasodine结构修饰研究

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具有抗肿瘤活性的Solasodine结构修饰研究

作者：况丽琴华东理工大学

学位级别：硕士

甾体皂甙具有多种生理活性,有研究表明,solasodine皂甙对多种人体癌细胞都有一定的抑制活性。因此,本论文对具有抗肿瘤活性的solasodine结构修饰进行了一定的研究,分为两部分：第一部分是solasodine糖甙化的研究。以D-葡萄糖、D-半乳糖... 详细信息

甾体皂甙具有多种生理活性,有研究表明,solasodine皂甙对多种人体癌细胞都有一定的抑制活性。因此,本论文对具有抗肿瘤活性的solasodine结构修饰进行了一定的研究,分为两部分：第一部分是solasodine糖甙化的研究。以D-葡萄糖、D-半乳糖、L-鼠李糖为原料,经过全苯甲酰化保护、溴代制得溴代糖基给体2、4、6,及购买的乙酰溴-α-D-葡萄糖,再与solasodine在AgSO3CF3催化下得到目标化合物7、8、10、12,收率在85%以上,然后水解得到化合物9、11、13。对化合物7-13进行活性检测,结果表明化合物8、9、11、13对A549(人肺癌细胞)、Colo205(人肠癌细胞)、MDA-MB-435(人乳腺癌细胞)、QGY7703(人肝癌细胞)、HL-60(人白血病细胞)都具有一定的体外抗肿瘤活性。第二部分是3,16-二羟基-孕甾-5-烯-22-醛的合成研究。本论文设计以去氢表雄酮和孕甾双烯醇酮为原料,与乙基三苯基溴化磷、(α-溴丙醛缩乙二醇)三苯基溴化磷、(α-溴丙酸乙酯)三苯基溴化磷和(甲氧基甲基)三苯基氯化磷四种不同的季膦盐通过Wittig反应来合成该化合物。在合成的过程中并没有得到设计的目标化合物,因此,以酮为原料通过Wittig反应进行合成的方法并不是特别的理想,但还是合成得到了与目标化合物结构较接近的化合物17。

关键词： solasodine 糖苷化 wittig反应抗肿瘤活性

An alternative total synthesis of solamargine

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Science China Chemistry 2012年第7期55卷 1247-1251页

作者： WEI GuoHua WEI DongBin DU YuGuo State Key Laboratory of Environmental Chemistry and Ecotoxicology Research Center for Eco-Environmental Sciences(CAS)Beijing 100085China

Solamargine, （25R）-3β-（O-a-L-rhamnopyranosyl-（1--2）-[O-a-L-rhamnopyranosyl-（1--4）]-β-D-glucopyranosloxy}-22a-N- spirosol-5-ene, isolated from the berries of solanum aculeastrum, has been synthesized in 26.8% overall yield. First glycosylation before N-cyclization significantly facilitated synthesis of the desired molecule. We anticipate that this work will provide a new approach to access solamargine and its diversified analogues.

关键词： solasodine natural products solamargine glycosides

CuradermBEC5for Skin Cancers, Is It? An Overview

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Journal of Cancer Therapy 2011年第5期2卷 728-745页

作者： Tania Robyn Chase 不详

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.

关键词： Nonmelanoma Skin Cancers solasodine Rhamnosyl Glycosides Curaderm Solamargine Solasonine