Bufadienolides from amphibians: A promising source of anticancer prototypes for radical innovation, apoptosis triggering and Na+/K+-ATPase inhibition

Sousa, Lívia Queiroz de; Machado, Kátia da Conceição; Oliveira, Samara Ferreira de Carvalho; Araújo, Lidiane da Silva; Monção-Filho, Evaldo dos Santos; Melo‐Cavalcante, Ana Amélia de Carvalho; Vieira-Júnior, Gerardo M.; Ferreira, Paulo Michel Pinheiro

doi:10.1016/j.toxicon.2017.01.004

Cited by 77 publications

(56 citation statements)

References 130 publications

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“…Most amphibians produce secretions that are released onto their skin when myocytes surrounding the granular glands contract in response to stimuli promoted by the sympathetic nervous system [1]. Amphibian secretions have been used for centuries as ethno-pharmaceutical drugs in Asia and in the Americas for the treatment of several diseases, such as hemorrhages, allergies, inflammations and infections, and more recently have been considered as a prolific source of potential drug leads [2,3]. Among the molecules constituting amphibian skin secretions, a myriad of peptides have gained attention due to their wide range of biological activities.…”

Section: Introductionmentioning

confidence: 99%

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

et al. 2020

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Amphibian skin is a multifunctional organ that plays key roles in defense, breathing, and water balance. In this study, skin secretion samples of the fire salamander (Salamandra salamandra) were separated using RP-HPLC and de novo sequenced using MALDI-TOF MS/MS. Next, we used an in silico platform to screen antioxidant molecules in the framework of density functional theory. One of the identified peptides, salamandrin-I, [M + H]+ = 1406.6 Da, was selected for solid-phase synthesis; it showed free radical scavenging activity against DPPH and ABTS radicals. Salamandrin-I did not show antimicrobial activity against Gram-positive and -negative bacteria. In vitro assays using human microglia and red blood cells showed that salamandrin-I has no cytotoxicity up to the concentration of 100 µM. In addition, in vivo toxicity tests on Galleria mellonella larvae resulted in no mortality at 20 and 40 mg/kg. Antioxidant peptides derived from natural sources are increasingly attracting interest. Among several applications, these peptides, such as salamandrin-I, can be used as templates in the design of novel antioxidant molecules that may contribute to devising strategies for more effective control of neurological disease.

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Section: Introductionmentioning

confidence: 99%

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

et al. 2020

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“…Traditional Chinese medicines (TCM), including plants, animal parts, and minerals, have drawn a great deal of attention in recent years for their potential in the treatment of HCC and can prevent recurrence after resection of small HCC (5)(6)(7). In TCM practice, Chansu (venom of toad skin) and Chanpi (the skin of toad) have been used in the treatment of tumors, including HCC (8)(9)(10). Bufalin has been recognized as a prominent digoxinlike component and a potential Na + -K + -ATPase inhibitor from Chansu and Chanpi (11,12).…”

Section: Introductionmentioning

confidence: 99%

Determination of Endogenous Bufalin in Serum of Patients With Hepatocellular Carcinoma Based on HPLC-MS/MS

Han

Yang²,

et al. 2020

Front. Oncol.

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Bufalin is a cardiotonic steroid and a key active ingredient of the Chinese medicine ChanSu. It has significant anti-tumor activity against many malignancies, including hepatocellular carcinoma (HCC). Previous studies have shown that human bodies contain an endogenous bufalin-like substance. This study aimed to confirm whether the endogenous bufalin-like substances is bufalin and further detect the differences between HCC and control groups of endogenous bufalin concentration by the high-performance liquid chromatography coupled tandem mass spectrometry (HPLC-MS/MS). The results confirmed the endogenous bufalin-like substance is bufalin. Totally, 227 serum samples were collected: 54 from HCC patients and 173 from healthy volunteers constituting a control group. Both the test group and the control group contained bufalin in serum, revealing that bufalin is indeed an endogenous substance. The bufalin concentration was 1.3 nM in HCC patients and 5.7 nM in normal people (P < 0.0001). These results indicate that human bodies contain endogenous bufalin, and it may be negatively correlated with the incidence of HCC.

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“…Both bufalin and cinobufagin have the potential antitumor activity, and research from different groups has focused on it. [5][6][7]. Chan Su is described as 'dried toad venom' in English, 'toad cake' in China, 'Senso' in Japan, and 'Somsa' in Korea [1,8].…”

Section: Introductionmentioning

confidence: 99%

Bufalin, a bufanolide steroid from the parotoid glands of the Chinese toad, suppresses hERG K⁺ currents expressed in HEK293 cells

Song

Zhang

Song

et al. 2017

Fundamemntal Clinical Pharma

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In this study, we investigated the effect of bufalin on the human ether-à-go-go-related gene (hERG) K channels using the perforated patch recording technique. We measured a half-maximal inhibitory concentration (IC ) of 24.83 μM and maximal inhibitory effect of 39.45 ± 1.14% with bufalin. These findings suggest that bufalin is a potent hERG K channel blocker and may provide a new way for understanding Chan Su-induced arrhythmia.

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Bufadienolides from amphibians: A promising source of anticancer prototypes for radical innovation, apoptosis triggering and Na+/K+-ATPase inhibition

Cited by 77 publications

References 130 publications

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

Determination of Endogenous Bufalin in Serum of Patients With Hepatocellular Carcinoma Based on HPLC-MS/MS

Bufalin, a bufanolide steroid from the parotoid glands of the Chinese toad, suppresses hERG K⁺ currents expressed in HEK293 cells

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Bufadienolides from amphibians: A promising source of anticancer prototypes for radical innovation, apoptosis triggering and Na+/K+-ATPase inhibition

Cited by 77 publications

References 130 publications

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

The Antioxidant Peptide Salamandrin-I: First Bioactive Peptide Identified from Skin Secretion of Salamandra Genus (Salamandra salamandra)

Determination of Endogenous Bufalin in Serum of Patients With Hepatocellular Carcinoma Based on HPLC-MS/MS

Bufalin, a bufanolide steroid from the parotoid glands of the Chinese toad, suppresses hERG K+ currents expressed in HEK293 cells

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Bufalin, a bufanolide steroid from the parotoid glands of the Chinese toad, suppresses hERG K⁺ currents expressed in HEK293 cells