Two New Indole Alkaloids from Toad Venom of Bufo bufo gargarizans

Chen, Yulin; Dai, Yinghui; Wang, Andong; Zhou, Zi-Ying; Miao, Lei; Liu, Jiao; Lin, Bin; Xia, Mingyu; Wang, Dong

doi:10.3390/molecules25194511

Cited by 10 publications

(7 citation statements)

References 10 publications

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“…While bufalin effectively induces cell cycle arrest, it shows different patterns in different cell types. Bufalin could induce cell cycle arrest at the S phase in pancreatic cancer BxPC3-luc2 cells ( Liu et al, 2016 ), lung cancer A549 cells ( Zhang and Fu, 2017 ) at G2/M phase in GBM U251 and U87MG cells ( Zhang et al, 2017 ), TNBC MDA-MB-231 and HCC-1937 cells ( Chen et al, 2020b ), pancreatic cancer PANC-1, and CFPAC-1 cells ( Li et al, 2014 ), cervical cancer Siha cells ( Liu et al, 2016 ). These results suggested that bufalin may interfere with cancer cell division, which can be further utilized with certain anticancer therapies.…”

Section: Discussionmentioning

confidence: 99%

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An overview of the past decade of bufalin in the treatment of refractory and drug-resistant cancers: current status, challenges, and future perspectives

Ye,

Zhou,

Ren

et al. 2023

Front. Pharmacol.

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Profound progress has been made in cancer treatment in the past three decades. However, drug resistance remains prevalent and a critical challenge. Drug resistance can be attributed to oncogenes mutations, activated defensive mechanisms, ATP-bind cassette transporters overexpression, cancer stem cells, etc. Chinese traditional medicine toad venom has been used for centuries for different diseases, including resistant cancers. Bufalin is one of the bufadienolides in toad venom that has been extensively studied for its potential in refractory and drug-resistant cancer treatments in vitro and in vivo. In this work, we would like to critically review the progress made in the past decade (2013–2022) of bufalin in overcoming drug resistance in cancers. Generally, bufalin shows high potential in killing certain refractory and resistant cancer cells via multiple mechanisms. More importantly, bufalin can work as a chemo-sensitizer that enhances the sensitivity of certain conventional and targeted therapies at low concentrations. In addition, the development of bufalin derivatives was also briefly summarized and discussed. We also analyzed the obstacles and challenges and provided possible solutions for future perspectives. We hope that the collective information may help evoke more effort for more in-depth studies and evaluation of bufalin in both lab and possible clinical trials.

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Section: Discussionmentioning

confidence: 99%

“… Chen et al (2020b) found that bufalin suppressed the proliferation (0.5 μM), colony formation (0.5 and 1 μM) of TNBC MDA-MB-231 and HCC-1937 cell lines, arresting cells at G2/M phase ( Chen et al, 2020b ), same as in GBM cells ( Zhang et al, 2017 ). Bufalin (0.5 µM, 48 h) caused apoptosis of both cell lines at ∼10%.…”

Section: Introductionmentioning

confidence: 99%

An overview of the past decade of bufalin in the treatment of refractory and drug-resistant cancers: current status, challenges, and future perspectives

Ye,

Zhou,

Ren

et al. 2023

Front. Pharmacol.

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“…Both alkaloids and bufadienolides are among the most prominent and most-studied compounds in toad venom. Growing studies have confirmed that both alkaloids and bufadienolides can work in treating cardiovascular diseases and cancers ( Chen et al, 2020 ). Our special and major interest in this review falls in these bufadienolides ( Figure 2 ).…”

Section: Bufadienolides In Toad Venom and Their Therapeutic Implicati...mentioning

confidence: 99%

Toad venom-derived bufadienolides and their therapeutic application in prostate cancers: Current status and future directions

Zhou

Han

et al. 2023

Front. Chem.

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Cancer is the second leading cause of death worldwide. Specially, the high incidence rate and prevalence of drug resistance have rendered prostate cancer (PCa) a great threat to men’s health. Novel modalities with different structures or mechanisms are in urgent need to overcome these two challenges. Traditional Chinese medicine toad venom-derived agents (TVAs) have shown to possess versatile bioactivities in treating certain diseases including PCa. In this work, we attempted to have an overview of bufadienolides, the major bioactive components in TVAs, in the treatment of PCa in the past decade, including their derivatives developed by medicinal chemists to antagonize certain drawbacks of bufadienolides such as innate toxic effect to normal cells. Generally, bufadienolides can effectively induce apoptosis and suppress PCa cells in-vitro and in-vivo, majorly mediated by regulating certain microRNAs/long non-coding RNAs, or by modulating key pro-survival and pro-metastasis players in PCa. Importantly, critical obstacles and challenges using TVAs will be discussed and possible solutions and future perspectives will also be presented in this review. Further in-depth studies are clearly needed to decipher the mechanisms, e.g., targets and pathways, toxic effects and fully reveal their application. The information collected in this work may help evoke more effects in developing bufadienolides as therapeutic agents in PCa.

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“…Of note, the cinobufacini injection, as a sanctioned therapy, has been used in the management of cancer, including lung and liver malignancies, in China [4,5]. Research has elucidated that the pharmacologically active components within toad venom chiefly comprise alkaloids and bufadienolides, which are distinguished for their diverse bioactive activity for different diseases [6][7][8][9]. Previous studies have shown that bufadienolides demonstrate potent cytotoxic activities against diverse cancer cell lines in vitro and in vivo, with IC 50 values in the nanomolar range [10].…”

Section: Introductionmentioning

confidence: 99%

Isolation, Identification and Chemical Modification of Bufadienolides from Bufo melanostictus Schneider and Their Cytotoxic Activities against Prostate Cancer Cells

Ye,

Lin,

Chen

et al. 2024

Molecules

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The traditional Chinese medicine toad venom (Venenum bufonis) has been extensively used to treat various diseases, including cancers, in China and other Southeast Asian countries. The major constituents of toad venom, e.g., bufadienolides and alkaloids, exhibit broad-spectrum pharmacological effects in cancers. Herein, two new bufadienolides (1 and 2), along with eleven known compounds (3–13) were successfully isolated from Bufo melanostictus Schneider. Their structures were elucidated by extensive spectroscopic data and X-ray diffraction analysis. Furthermore, four lactam derivatives were synthesized through the transformation of bufadienolides lactones. The inhibitory effects of these compounds against human prostate cancer cell lines PC-3 and DU145 were evaluated. The outcomes indicated a notable trend, with a substantial subset displaying nanomolar range IC50 values against PC-3 and DU145 cells, underscoring their pronounced cytotoxicity. Moreover, a noteworthy distinction surfaces, wherein lactones consistently outperformed their lactam counterparts, further validating their heightened potency for the treatment of prostate cancer. This study contributes significant preclinical evidence substantiating the therapeutic viability of bufadienolides and toad venom as intervention strategies for prostate cancer.

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Two New Indole Alkaloids from Toad Venom of Bufo bufo gargarizans

Cited by 10 publications

References 10 publications

An overview of the past decade of bufalin in the treatment of refractory and drug-resistant cancers: current status, challenges, and future perspectives

An overview of the past decade of bufalin in the treatment of refractory and drug-resistant cancers: current status, challenges, and future perspectives

Toad venom-derived bufadienolides and their therapeutic application in prostate cancers: Current status and future directions

Isolation, Identification and Chemical Modification of Bufadienolides from Bufo melanostictus Schneider and Their Cytotoxic Activities against Prostate Cancer Cells

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