Solasodine 11 is a steroidal alkaloid with various biological activities.Herein,8 novel solasodine derivatives were synthesized and their effect on prostate cancer cell proliferation was assessed in vitro.Significant ...Solasodine 11 is a steroidal alkaloid with various biological activities.Herein,8 novel solasodine derivatives were synthesized and their effect on prostate cancer cell proliferation was assessed in vitro.Significant improvement in antiproliferative activity was achieved among some of the synthetic analogs.In particular,19 exhibited the most potent inhibitory effect against the proliferation of PC-3 cell line（IC50= 3.91μmol/L）.展开更多
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 communicatio...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.展开更多
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. Pre...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.展开更多
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...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.展开更多
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...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.展开更多
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 ...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.展开更多
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 comb...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.展开更多
The incidences of nonmelanoma skin cancer are increasing worldwide, and the ongoing war on its treatment necessitates the development of effective and non-invasive methods. Through basic and clinical research, non-inv...The incidences of nonmelanoma skin cancer are increasing worldwide, and the ongoing war on its treatment necessitates the development of effective and non-invasive methods. Through basic and clinical research, non-invasive treatments like Curaderm have been developed, leading to improved quality of life for patients. Excipients, previously considered inactive ingredients, play a crucial role in enhancing the performance of topical formulations. The development of Curaderm emphasizes the importance of understanding the interactions between active ingredients, excipients, and the biological system to create effective and affordable pharmaceutical formulations. The systematic approach taken in the development of Curaderm, starting from the observation of the anticancer activity of natural solasodine glycosides and progressing through toxicological and efficacy studies in cell culture, animals, and humans, has provided insights into the pharmacokinetics and pharmacodynamics of solasodine glycosides. It is crucial to determine these pharmacological parameters within the skin’s biological system for maximal effectiveness and cost-effectiveness of a skin cancer treatment. Curaderm, as a topical treatment for nonmelanoma skin cancer, offers benefits beyond those obtained from other topical treatments, providing hope for improved quality of life for patients.展开更多
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 incr...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.展开更多
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% ...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.展开更多
文摘Solasodine 11 is a steroidal alkaloid with various biological activities.Herein,8 novel solasodine derivatives were synthesized and their effect on prostate cancer cell proliferation was assessed in vitro.Significant improvement in antiproliferative activity was achieved among some of the synthetic analogs.In particular,19 exhibited the most potent inhibitory effect against the proliferation of PC-3 cell line（IC50= 3.91μmol/L）.
文摘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.
文摘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.
文摘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.
文摘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.
文摘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.
文摘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.
文摘The incidences of nonmelanoma skin cancer are increasing worldwide, and the ongoing war on its treatment necessitates the development of effective and non-invasive methods. Through basic and clinical research, non-invasive treatments like Curaderm have been developed, leading to improved quality of life for patients. Excipients, previously considered inactive ingredients, play a crucial role in enhancing the performance of topical formulations. The development of Curaderm emphasizes the importance of understanding the interactions between active ingredients, excipients, and the biological system to create effective and affordable pharmaceutical formulations. The systematic approach taken in the development of Curaderm, starting from the observation of the anticancer activity of natural solasodine glycosides and progressing through toxicological and efficacy studies in cell culture, animals, and humans, has provided insights into the pharmacokinetics and pharmacodynamics of solasodine glycosides. It is crucial to determine these pharmacological parameters within the skin’s biological system for maximal effectiveness and cost-effectiveness of a skin cancer treatment. Curaderm, as a topical treatment for nonmelanoma skin cancer, offers benefits beyond those obtained from other topical treatments, providing hope for improved quality of life for patients.
文摘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.
基金supported partially by the National Basic Research Program of China (2011CB936001)National Natural Science Foundation of China (20732001,20872172,21072217)
文摘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.
