Synthesis of glycosides bearing the disaccharide of OSW-1 or its 1→4-linked analogue and their antitumor activities

Ma, Xingquan; Yu, Biao; Hui, Yongzheng; Dong, Xiaoming; Ding, Jian

doi:10.1016/s0008-6215(00)00225-1

Cited by 45 publications

(38 citation statements)

References 8 publications

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“…Several studies of OSW-1 have focused on its isolation, cytotoxic tests, chemical synthesis, and preparation of synthetic analogues to understand the structure-activity relationships (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18). However, the mechanism by which OSW-1 exerts antitumor activity is not well delineated.…”

Section: ␤16␤17␣-trihydroxycholest-5-en-22-one 16-o-(2-o-4-methoxymentioning

confidence: 99%

Effective Killing of Leukemia Cells by the Natural Product OSW-1 through Disruption of Cellular Calcium Homeostasis

Garcı́a-Prieto

Ahmed

Zhao

et al. 2013

Journal of Biological Chemistry

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Background:The mechanistic action of antitumor agent OSW-1 is not clearly understood. Results: OSW-1 triggers a calcium-dependent cell death through inhibition of sodium-calcium exchanger 1 (NCX1) and mitochondrial calcium overload. Conclusion: Potency and efficacy of OSW-1 in eliminating leukemia cells are dependent on homeostatic calcium disruption. Significance: New insights on the role of calcium in the mechanism of OSW-1 reveal potential in therapeutics.

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Section: ␤16␤17␣-trihydroxycholest-5-en-22-one 16-o-(2-o-4-methoxymentioning

confidence: 99%

Effective Killing of Leukemia Cells by the Natural Product OSW-1 through Disruption of Cellular Calcium Homeostasis

Garcı́a-Prieto

Ahmed

Zhao

et al. 2013

Journal of Biological Chemistry

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“…Several studies have suggested that OSW-1 has a potent anti-proliferative effect against a variety of tumor cell lines, such as leukemia, pancreatic cancer, malignant brain tumor, and hepatocellular carcinoma cells, but is less toxic to non-malignant cells in vitro (5,6); however, it is so difficult to isolate the compound in certain stages that the application is restricted to research. Recent studies have shown that the synthesis of OSW-1 and its derivatives has gradually improved; however, this finding provides the premise for a possible therapeutic application for OSW-1 in the future (7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24). We determined whether the anti-proliferative effect of OSW-1, Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo the mechanism of which is not completely understood, can be extrapolated to colon cancer cells.…”

Section: Introductionmentioning

confidence: 99%

Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo

et al. 2017

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Abstract. As a natural compound, Ornithogalum caudatumAit is primarily used as an anti-inflammatory and antitumor agent in Chinese folk medicine. In 1992, OSW-1 was isolated from this compound, which is a new member of cholestane saponin family. In numerous recent studies, OSW-1 has been shown to have powerful cytotoxic anticancer effects against various malignant cells. However, the therapeutic efficacy of OSW-1 on colon cancer and the underlying mechanism are not understood. To explore the mechanism underlying OSW-1 in antitumor therapy, a therapeutic function analysis of OSW-1 on colon cancer was performed in vitro and in vivo. It was shown that with low toxicity on normal colonic cells, OSW-1 suppresses colon cancer cells in vitro and this inhibition was via the intrinsic apoptotic pathway, which increased cellular calcium, changed mitochondrial membrane potential, disrupted mitochondrial morphology, and led to the release of cytochrome c and the activation of caspase-3. Furthermore, in a nude mouse model, OSW-1 had a powerful effect on suppressing colon tumor proliferation without significant side effects through the apoptosis pathway. Taken together, these results demonstrate that OSW-1 is a potential drug for colon cancer treatment.

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“…8,9) Recent studies have shown that they have cytotoxic properties against several strains of human cancer cells. [10][11][12][13][14] Dioscin [15][16][17] and trillin 18) are the best known diosgenyl saponins with these properties (Fig. 1).…”

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confidence: 99%

The Mitotic-Arresting and Apoptosis-Inducing Effects of Diosgenyl Saponins on Human Leukemia Cell Lines

Liu

Wang

et al. 2004

Biological & Pharmaceutical Bulletin

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Diosgenyl saponins are the most abundant steroid saponins, and exert a large variety of biological functions. In a previous report, we showed that dioscin was able to induce cytotoxicity and apoptosis in human myeloblast leukemia HL-60 cells. This study further investigated the action mechanisms underlying this effect. The activation of caspase-9 and -3, but not caspase-8, together with the down-regulation of anti-apoptotic Bcl-2 protein, demonstrated that the apoptotic signaling triggered by dioscin was mediated through the intrinsic mitochondriadependent pathway. We also investigated its anti-proliferative effect on human chronic myelogenous leukemia K562 cells. Flow cytometry analysis showed that dioscin treatment induced the accumulation of cells in the G 2 /M phase. Cytomorphology with DAPI and Wright-Giemsa staining demonstrated the enlargement of cell volume and multinucleation in the treated cells. Subsequent apoptosis was delineated with phosphatidylserine externalization and DNA hypodiploidy. Trillin was one of the hydrolysates of dioscin. We demonstrated that it could induce multinucleation in HL-60, K562 and human promyelocytic leukemia NB 4 cells, suggesting its extensive mitotic-arresting effects. As the diosgenyl sapogenin, diosgenin was also shown to be able to induce multinucleation and apoptosis in K562 cells in a similar manner to dioscin. These findings suggest that diosgenyl saponins have the properties to induce mitotic arrest and apoptosis, suggesting that they may be a new kind of antimitotic agent.

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Synthesis of glycosides bearing the disaccharide of OSW-1 or its 1→4-linked analogue and their antitumor activities

Cited by 45 publications

References 8 publications

Effective Killing of Leukemia Cells by the Natural Product OSW-1 through Disruption of Cellular Calcium Homeostasis

Effective Killing of Leukemia Cells by the Natural Product OSW-1 through Disruption of Cellular Calcium Homeostasis

Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo

The Mitotic-Arresting and Apoptosis-Inducing Effects of Diosgenyl Saponins on Human Leukemia Cell Lines

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