Prevention

Lahans, Tai

doi:10.1016/b978-044310063-5.50018-x

Cited by 2 publications

(2 citation statements)

References 16 publications

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“…The history of Ge-132 is now well-known (see e.g., [ 6 , 7 , 24 , 70 , 71 ]). It was Ge-132 that led to the active study of biological activity of germanium compounds and their application in medical practice, especially in complex cancer therapy [ 7 , 19 , 31 , 36 , 72 ]. There are clinically proven cases of the successful use of these compounds in cancer treatment; for example, the complete remission of lung cancer was achieved when taking Ge-132 [ 73 ].…”

Section: Historical Digression and Toxicity Of Germanium Compoundsmentioning

confidence: 99%

Physiological Activity of Trace Element Germanium Including Anticancer Properties

Менчиков

Popov

2023

Biomedicines

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Germanium is an essential microelement, and its deficiency can result in numerous diseases, particularly oncogenic conditions. Consequently, water-soluble germanium compounds, including inorganic and coordination compounds, have attracted significant attention due to their biological activity. The review analyzes the primary research from the last decade related to the anticancer activity of germanium compounds. Furthermore, the review clarifies their actual toxicity, identifies errors and misconceptions that have contributed to the discrediting of their biological activity, and briefly suggests a putative mechanism of germanium-mediated protection from oxidative stress. Finally, the review provides clarifications on the discovery history of water-soluble organic germanium compounds, which was distorted and suppressed for a long time.

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Section: Historical Digression and Toxicity Of Germanium Compoundsmentioning

confidence: 99%

Physiological Activity of Trace Element Germanium Including Anticancer Properties

Менчиков

Popov

2023

Biomedicines

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“…Dioscoreae rhizoma (chinese yam, shānyào, lit. “mountain medicine”) is described in traditional Chinese medicine to tonify the Qi of lung, spleen and kidney and to nourish the kidney’s essence [ 19 ]. Diosgenin was first discovered in 1937 by Tsukamoto and colleagues in Dioscorea tokoro (Dioscoreaceae) and can be found, along with its corresponding saponins dioscin and protodioscin, in many different Dioscorea species [ 20 , 21 ].…”

Section: Introductionmentioning

confidence: 99%

Identification of the Natural Steroid Sapogenin Diosgenin as a Direct Dual-Specific RORα/γ Inverse Agonist

Schwarz¹,

Perhal²,

Schöberl³

et al. 2022

Biomedicines

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The steroid sapogenin diosgenin is a well-known natural product with a plethora of described pharmacological activities including the amelioration of T helper 17 (Th17)-driven pathologies. However, the exact underlying mode of action of diosgenin leading to a dampened Th17 response is still largely unknown and specific molecular targets have yet to be identified. Here, we show that diosgenin acts as a direct ligand and inverse agonist of the nuclear receptor retinoic acid receptor (RAR)-related orphan receptor (ROR)α and RORγ, which are key transcription factors involved in Th17 cell differentiation and metabolism. IC50 values determined by luciferase reporter gene assays, employing constructs for either RORγ-Gal4 fusion proteins or full length receptors, were in the low micromolar range at around 2 µM. To highlight the functional consequences of this RORα/γ inverse agonism, we determined gene expression levels of important ROR target genes, i.e., IL-17A and glucose-6-phosphatase, in relevant cellular in vitro models of Jurkat T and HepG2 cells, respectively, by RT-qPCR (reverse transcription quantitative PCR). Thereby, it was shown that diosgenin leads to a dose-dependent decrease in target gene expressions consistent with its potent cellular ROR inverse agonistic activity. Additionally, in silico dockings of diosgenin to the ROR ligand-binding domain were performed to determine the underlying binding mode. Taken together, our results establish diosgenin as a novel, direct and dual-selective RORα/γ inverse agonist. This finding establishes a direct molecular target for diosgenin for the first time, which can further explain reported amendments in Th17-driven diseases by this compound.

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Prevention

Cited by 2 publications

References 16 publications

Physiological Activity of Trace Element Germanium Including Anticancer Properties

Physiological Activity of Trace Element Germanium Including Anticancer Properties

Identification of the Natural Steroid Sapogenin Diosgenin as a Direct Dual-Specific RORα/γ Inverse Agonist

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