Antitumor activity of extracts and compounds from the skin of the toad Bufo bufo gargarizans Cantor

Qi, Fanghua; Li, Anyuan; Inagaki, Yoshiaki; Kokudo, Norihiro; Tamura, Sumihito; Nakata, Munehiro; Tang, Wei

doi:10.1016/j.intimp.2010.12.007

Cited by 219 publications

(176 citation statements)

References 48 publications

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“…Cardiac glycosides including bufalin, resibufogenin, and cinobufagin are the three major active constituents to which the antitumor activity of Huachansu injection may be attributed. Huachansu injection exhibited significant effects on inhibition cell proliferation, induction of cell differentiation and apoptosis, disruption of the cell cycle, inhibition of cancer angiogenesis, reversal of multi-drug resistance, and regulation of the immune response in cancer cells (75,76). It also could effectively 25 [81][82][83] enhance physical immunity and improve the quality of life with little toxicity in cancer patients.…”

Section: Huachansu Injectionmentioning

confidence: 99%

The advantages of using traditional Chinese medicine as an adjunctive therapy in the whole course of cancer treatment instead of only terminal stage of cancer

Zhao

Zhou

et al. 2015

BST

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364

268

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Section: Huachansu Injectionmentioning

confidence: 99%

The advantages of using traditional Chinese medicine as an adjunctive therapy in the whole course of cancer treatment instead of only terminal stage of cancer

Zhao

Zhou

et al. 2015

BST

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364

268

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“…Cinobufacini (Huachansu), a Chinese medicine prepared from dried toad skin, has been widely used for the treatment of various types of cancer in China (25). Bufalin, which is the main active component of cinobufacini, has attracted much attention from researchers since the 1990's (2). Experiments have demonstrated that it is capable of inducing apoptosis in a variety of types of tumor cell, including leukemia cells such as U937, HL-60, ML1 and THP1 (5,6,(9)(10)(11)26).…”

Section: Discussionmentioning

confidence: 99%

“…Experiments have demonstrated that it is capable of inducing apoptosis in a variety of types of tumor cell, including leukemia cells such as U937, HL-60, ML1 and THP1 (5,6,(9)(10)(11)26). The mechanisms by which bufalin induces apoptosis are complex and involve a diverse range of cell signals (2,3). Data suggest that activation of the MAPK signaling pathway is one of the most important signal transduction pathways for the induction of apoptosis by bufalin (2).…”

Section: Discussionmentioning

confidence: 99%

“…It is a cardioactive C-24 steroid, with the molecular formula C 24 H 34 O 4 and a relative molecular weight of 386.5. Bufalin exhibits a variety of biological activities, such as cardiotonic, anesthetic, blood pressure stimulatory, respiratory and antineoplastic effects (2). In terms of its antitumor activity, bufalin has been demonstrated to inhibit the growth of gastric, colon, breast, prostate, gynecological, hepatocellular and bladder tumors (3).…”

Section: Introductionmentioning

confidence: 99%

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BMI-1 is important in bufalin-induced apoptosis of K562 cells

Lian

Wang

Wei

et al. 2014

Molecular Medicine Reports

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Abstract. The purpose of this study was to analyze the effects of bufalin on the gene expression of K562 cells and on the expression of BMI-1 pathway constituents in K562 cell apoptosis. K562 cells were treated with bufalin, and the inhibition rate and apoptosis were detected by an MTT assay, flow cytometry and a microarray assay. BMI-1, p16 INK4a and p14 ARF were examined by quantitative polymerase chain reaction (qPCR). Bufalin induced significant changes in the gene expression of the K562 cells; 4296 genes were differentially expressed, 2185 were upregulated and 2111 were downregulated. The most upregulated genes were associated with transcription regulation, while the most downregulated genes were associated with the non-coding RNA metabolic processes and DNA repair. qPCR analysis demonstrated that BMI-1 was overexpressed in the K562 cells. Bufalin is able to downregulate BMI-1 expression levels in K562 cells prematurely and cause an increase in the expression levels of p16 INK4a and p14 ARF . Moreover, bufalin downregulated BCR/ABL expression levels in a time-dependent manner, and the expression of BCR/ABL was not associated with the upregulation or downregulation of BMI-1 expression. Bufalin may induce K562 cell apoptosis by downregulating BMI-1 expression levels and accordingly upregulating the expression levels of p16 INK4a and p14 ARF . Bufalin may also induce K562 cell apoptosis via downregulating BCR/ABL expression levels, and this pathway may be independent of the BMI-1 pathway.

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“…ChanSu has been used for centuries to treat arrhythmia, inflammation and cancer in China and other Asian countries based on its cardiotonic, anti-inflammatory and anti-cancer effects [3] . Medicines containing ChanSu, such as Huachansu injection, are still widely used in the clinical setting to treat various cancers, including lung cancer [4,5] . BF211 is a derivative of bufalin, and the synthesis and therapeutic use of BF211 as an anti-cancer agent was granted patent protection rights in China (Authorized Announcement No CN 102532235B).…”

Section: Introductionmentioning

confidence: 99%

Bufalin derivative BF211 inhibits proteasome activity in human lung cancer cells in vitro by inhibiting β1 subunit expression and disrupting proteasome assembly

et al. 2016

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Aim: Bufalin is one of the active components in the traditional Chinese medicine ChanSu that is used to treat arrhythmia, inflammation and cancer. BF211 is a bufalin derivative with stronger cytotoxic activity in cancer cells. The aim of this study was to identify the putative target proteins of BF211 and the signaling pathways in cancer cells. Methods: A549 human lung cancer cells were treated with BF211. A SILAC-based proteomic analysis was used to detect the protein expression profiles of BF211-treated A549 cells. Cellular proteasome activities were examined using fluorogenic peptide substrates, and the binding affinities of BF211 to recombinant proteasome subunit proteins were evaluated using the Biacore assay. The expression levels of proteasome subunits were determined using RT-PCR and Western blotting, and the levels of the integral 26S proteasome were evaluated using native PAGE analysis. Results: The proteomic analysis revealed that 1282 proteins were differentially expressed in BF211-treated A549 cells, and the putative target proteins of BF211 were associated with various cellular functions, including transcription, translation, mRNA splicing, ribosomal protein synthesis and proteasome function. In A549 cells, BF211 (5, 10, and 20 nmol/L) dose-dependently inhibited the enzymatic activities of proteasome. But BF211 displayed a moderate affinity in binding to proteasome β1 subunit and no binding affinity to the β2 and β5 subunits. Moreover, BF211 (0.1, 1, and 10 nmol/L) did not inhibit the proteasome activities in the cell lysates. BF211 (5, 10, and 20 nmol/L) significantly decreased the expression level of proteasome β1 subunit and the levels of integral 26S proteasome in A549 cells. Similarly, knockdown of the β1 subunit with siRNA in A549 cells significantly decreased integral 26S proteasome and proteasome activity. Conclusion: BF211 inhibits proteasome activity in A549 cells by decreasing β1 subunit expression and disrupting proteasome assembly.Keywords: bufalin; ChanSu; cardiac steroids; proteasome β1 subunit; proteasome assembly; A549 human lung cancer cells; In the present study, to identify the possible signaling network activated by BF211 in cancer cells, we conducted a SILAC-based proteomic analysis and compared the protein expression profiles of A549 human lung cancer cells treated with either BF211 or a solvent control. Our findings suggested that BF211 influences proteasome function, and we further evaluated the effects and potential mechanisms mediating this phenomenon.

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Antitumor activity of extracts and compounds from the skin of the toad Bufo bufo gargarizans Cantor

Cited by 219 publications

References 48 publications

The advantages of using traditional Chinese medicine as an adjunctive therapy in the whole course of cancer treatment instead of only terminal stage of cancer

The advantages of using traditional Chinese medicine as an adjunctive therapy in the whole course of cancer treatment instead of only terminal stage of cancer

BMI-1 is important in bufalin-induced apoptosis of K562 cells

Bufalin derivative BF211 inhibits proteasome activity in human lung cancer cells in vitro by inhibiting β1 subunit expression and disrupting proteasome assembly

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