4.7 Review

Bufalin for an innovative therapeutic approach against cancer

Related references

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Article Pharmacology & Pharmacy

Folic Acid-Functionalized Metal-Organic Framework Nanoparticles as Drug Carriers Improved Bufalin Antitumor Activity Against Breast Cancer

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Summary: In this study, pH-sensitive and redox-responsive folic acid-modified metal-organic frameworks (FA-MOF/But) were designed and constructed as drug carriers for Bufalin. It was found that these nanoparticles showed improved water solubility, stability, intracellular uptake, and cytotoxicity compared to the free Bufalin. In addition, the FA-MOF/But nanoparticles also demonstrated enhanced anticancer activity, reduced side effects, and improved accumulation at the tumor site in vivo.

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Research Progress in Pharmacological Activities and Applications of Cardiotonic Steroids

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Bufalin stimulates antitumor immune response by driving tumor-infiltrating macrophage toward M1 phenotype in hepatocellular carcinoma

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Summary: This study found that bufalin can promote the polarization of tumor-infiltrating macrophages (TIMs) towards the tumor-inhibitory M1 phenotype to improve the efficacy of immunotherapy for hepatocellular carcinoma (HCC). Bufalin inhibits the overexpression of p50 nuclear factor kappa B (NF-kappa B) factor and activates the NF-kappa B signaling pathway, resulting in the production of immunostimulatory cytokines and the activation of antitumor T cell immune response. Bufalin also enhances the antitumor activity of anti-PD-1 antibody in HCC.

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Novel Strategies for Solubility and Bioavailability Enhancement of Bufadienolides

Huili Shao et al.

Summary: Toad venom contains bufadienolides, which have various pharmacological activities including antitumor, cardiovascular, anti-inflammatory, analgesic, and immunomodulatory effects. However, the clinical application of bufadienolides is limited due to their poor solubility and bioavailability. Strategies such as structural modification and drug delivery systems have been explored to overcome these limitations.

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Bufalin inhibits ovarian carcinoma via targeting mTOR/HIF-α pathway

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Summary: Bufalin, extracted from natural product Chansu, has been tested as an antitumour agent in ovarian cancer. It inhibits cell growth and migration by suppressing mTOR activation and HIF-1 alpha induction, potentially enhancing the efficacy of cisplatin in patients.

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Design of dual targeting immunomicelles loaded with bufalin and study of their anti-tumor effect on liver cancer

Hao Gou et al.

Summary: In this study, a dual targeting immunomicelles (DTIs) loaded with bufalin were designed and synthesized, which have features of temperature sensitivity, high stability, and slow drug release. Compared with free bufalin, the cellular uptake and cytotoxicity of DTIs-BF against liver cancer cells were significantly enhanced, showing better therapeutic effects.

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Bufalin enhances the killing efficacy of NK cells against hepatocellular carcinoma by inhibiting MICA shedding

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Co-delivery of bufalin and nintedanib via albumin sub-microspheres for synergistic cancer therapy

Ying Xu et al.

Summary: Albumin sub-microspheres developed using coaxial-electrospray technology for co-delivery of bufalin and nintedanib show superior tumor targeting efficiency and synergistic therapeutic effect. This provides a novel method for fabricating an albumin-based drug delivery system and a potential efficient combination therapeutic strategy for tumor treatment.

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Bufalin inhibits the malignant development of non-small cell lung cancer by mediating the circ_0046264/miR-522-3p axis

Jing Jin et al.

Summary: Bufalin exerts anti-tumor effects in NSCLC by modulating the circ_0046264/miR-522-3p pathway, which could be a potential functional mechanism of bufalin in NSCLC.

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Tumor-Targeted Delivery of Bufalin-Loaded Modified Albumin-Polymer Hybrid for Enhanced Antitumor Therapy and Attenuated Hemolysis Toxicity and Cardiotoxicity

Ying Xu et al.

Summary: A novel albumin polymer hybrid was designed for targeted delivery of the anticancer drug bufalin, demonstrating improved antitumor effects and reduced side effects.

AAPS PHARMSCITECH (2021)

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Fang-Jie Li et al.

Summary: Toad venom, a traditional natural medicine in China, has shown potential in cancer treatment with its wide range of anticancer activities, likely through mechanisms such as apoptosis induction, cell cycle arrest, metastasis suppression, reversal of drug resistance, or growth inhibition of cancer cells. Research on the chemical constituents and anticancer mechanisms of toad venom is important for further studies and development of cancer treatments.

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Bufalin targets the SRC-3/MIF pathway in chemoresistant cells to regulate M2 macrophage polarization in colorectal cancer

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Summary: Bufalin can reduce the polarization of M2 macrophages induced by chemoresistant cells, but has no direct effect on M2 macrophage polarization itself. Bufalin targets the SRC-3 protein to reduce MIF release and regulate the polarization of M2 macrophages. Additionally, Cinobufacini, which contains Bufalin as its main active monomer, can enhance the anti-tumour effect of oxaliplatin by regulating M2 macrophage polarization in vivo and in the clinic.

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Therapeutic potential of targeting membrane-spanning proteoglycan SDC4 in hepatocellular carcinoma

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Bufalin induces mitochondrial dysfunction and promotes apoptosis of glioma cells by regulating Annexin A2 and DRP1 protein expression

Yao Li et al.

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Bufalin suppresses tumour microenvironment-mediated angiogenesis by inhibiting the STAT3 signalling pathway

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