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Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1α Inhibition.

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To cope with hypoxia, tumor cells have developed a number of adaptive mechanisms mediated by hypoxia-inducible factor 1 (HIF-1) to promote angiogenesis and cell survival. Due to significant roles of HIF-1 in the initiation, progression, metastasis, and resistance to treatment of most solid tumors, a

LXY6090 - a novel manassantin A derivative - limits breast cancer growth through hypoxia-inducible factor-1 inhibition.

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Hypoxia-inducible factor-1 (HIF-1) represents a novel antitumor target owing to its involvement in vital processes considered hallmarks of cancer phenotypes. Manassantin A (MA) derived from Saururus cernuus has been reported as a selective HIF-1 inhibitor. Herein, the structure of MA was optimized

Sauchinone inhibits hypoxia-induced epithelial-mesenchymal transition in pancreatic ductal adenocarcinoma cells through the Wnt/β-catenin pathway

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The hypoxic microenvironment is commonly found in various solid tumors including pancreatic ductal adenocarcinoma (PDAC). Saururus chinensis is a medicinal Chinese herb widely used because of documented anti-inflammatory and anti-angiogenic properties. Sauchinone is special active lignin extracted

Molecular-targeted antitumor agents: the Saururus cernuus dineolignans manassantin B and 4-O-demethylmanassantin B are potent inhibitors of hypoxia-activated HIF-1.

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The transcription factor hypoxia-inducible factor-1 (HIF-1) is a key regulator of tumor cell adaptation and survival under hypoxic conditions. Selective HIF-1 inhibitors represent an important new class of potential molecular-targeted antitumor therapeutic agents. Extracts of plants and marine

Saururus cernuus lignans--potent small molecule inhibitors of hypoxia-inducible factor-1.

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Hypoxia-inducible factor-1 (HIF-1) represents an important tumor-selective therapeutic target for solid tumors. In search of novel small molecule HIF-1 inhibitors, 5400 natural product-rich extracts from plants, marine organisms, and microbes were examined for HIF-1 inhibitory activities using a

Comparative study of chromatographic medium-associated mass and potential antitumor activity loss with bioactive extracts.

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Natural product drug discovery programs often rely on the use of silica (Si) gel, reversed-phase media, or size-exclusion resins (e.g., RP-C18, Sephadex LH-20) for compound purification. The synthetic polymer-based sorbent Diaion HP20SS (cross-linked polystyrene matrix) is used as an alternative to

Sauchinone exerts anticancer effects by targeting AMPK signaling in hepatocellular carcinoma cells.

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Sauchinone is a pharmacologically active compound isolated from Saururus chinensis, which has been used as a traditional Oriental medicine to treat fever, jaundice, and various inflammatory diseases. In this study, we investigated the effect of sauchinone against hepatocellular carcinoma (HCC) and

The lignan manassantin is a potent and specific inhibitor of mitochondrial complex I and bioenergetic activity in mammals.

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Dineolignans manassantin A and B from the plant Saururus cernuus are used in traditional medicine to manage a wide range of ailments such as edema, jaundice, and gonorrhea. Cell-based studies have identified several molecular target candidates of manassantin including NF-κB, MAPK, STAT3, and

Sauchinone reduces oxygen-glucose deprivation-evoked neuronal cell death via suppression of intracellular radical production.

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Sauchinone, a biologically active lignan isolated from Saururus chinensis, has been reported to show cytoprotective, anti-inflammatory and anti-apoptotic effects. However, little study has been done of the anti-ischemic/hypoxic effect of sauchinone. The present study investigates the

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