helichrysetin and xanthohumol

helichrysetin has been researched along with xanthohumol* in 2 studies

Other Studies

2 other study(ies) available for helichrysetin and xanthohumol

Article	Year
The role of chalcones: helichrysetin, xanthohumol, and flavokawin-C in promoting neurite outgrowth in PC12 Adh cells. Natural product research, 2018, Volume: 32, Issue:10 Chalcones are a group of compounds widely distributed in plant kingdom. The aim of this study was to assess the neurite outgrowth stimulatory activity of selected chalcones, namely helichrysetin, xanthohumol and flavokawin-C. Using adherent rat pheochromocytoma (PC12 Adh) cells, the chalcones were subjected to neurite outgrowth assay and the extracellular nerve growth factor (NGF) levels were determined. Xanthohumol (10 μg/mL) displayed the highest (p < 0.05) percentage of neurite-bearing PC12 Adh cells and the highest (p < 0.05) NGF level in the culture medium of xanthohumol-treated cells. While, helichrysetin induced a moderately high numbers of neurite-bearing cells, flavokawin-C did not stimulate neurite outgrowth. This work supports the potential use of xanthohumol as a potential neuroactive compound to stimulate neurite outgrowth. Topics: Animals; Chalcone; Chalcones; Drug Evaluation, Preclinical; Flavonoids; Nerve Growth Factors; Neurites; Neuronal Outgrowth; PC12 Cells; Propiophenones; Rats	2018
Synthesis of xanthohumol analogues and discovery of potent thioredoxin reductase inhibitor as potential anticancer agent. Journal of medicinal chemistry, 2015, Feb-26, Volume: 58, Issue:4 The selenoprotein thioredoxin reductases (TrxRs) are attractive targets for anticancer drugs development. Xanthohumol (Xn), a naturally occurring polyphenol chalcone from hops, has received increasing attention because of its multiple pharmacological activities. We synthesized Xn and its 43 analogues and discovered that compound 13n displayed the highest cytotoxicity toward HeLa cells (IC50 = 1.4 μM). Structure-activity relationship study indicates that the prenyl group is not necessary for cytotoxicity, and introducing electron-withdrawing group, especially on the meta-position, is favored. In addition, methylation of the phenoxyl groups generally improves the potency. Mechanistic study revealed that 13n selectively inhibits TrxR and induces reactive oxygen species and apoptosis in HeLa cells. Cells overexpressing TrxR are resistant to 13n insult, while knockdown of TrxR sensitizes cells to 13n treatment, highlighting the physiological significance of targeting TrxR by 13n. The clarification of the structural determinants for the potency would guide the design of novel potent molecules for future development. Topics: Antineoplastic Agents, Phytogenic; Apoptosis; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; Flavonoids; HeLa Cells; Hep G2 Cells; HL-60 Cells; Humans; Molecular Structure; Propiophenones; Structure-Activity Relationship; Thioredoxin-Disulfide Reductase; Tumor Cells, Cultured	2015

Article

Year

The role of chalcones: helichrysetin, xanthohumol, and flavokawin-C in promoting neurite outgrowth in PC12 Adh cells.

Natural product research, 2018, Volume: 32, Issue:10

Chalcones are a group of compounds widely distributed in plant kingdom. The aim of this study was to assess the neurite outgrowth stimulatory activity of selected chalcones, namely helichrysetin, xanthohumol and flavokawin-C. Using adherent rat pheochromocytoma (PC12 Adh) cells, the chalcones were subjected to neurite outgrowth assay and the extracellular nerve growth factor (NGF) levels were determined. Xanthohumol (10 μg/mL) displayed the highest (p < 0.05) percentage of neurite-bearing PC12 Adh cells and the highest (p < 0.05) NGF level in the culture medium of xanthohumol-treated cells. While, helichrysetin induced a moderately high numbers of neurite-bearing cells, flavokawin-C did not stimulate neurite outgrowth. This work supports the potential use of xanthohumol as a potential neuroactive compound to stimulate neurite outgrowth.

Topics: Animals; Chalcone; Chalcones; Drug Evaluation, Preclinical; Flavonoids; Nerve Growth Factors; Neurites; Neuronal Outgrowth; PC12 Cells; Propiophenones; Rats

2018

Synthesis of xanthohumol analogues and discovery of potent thioredoxin reductase inhibitor as potential anticancer agent.

Journal of medicinal chemistry, 2015, Feb-26, Volume: 58, Issue:4

The selenoprotein thioredoxin reductases (TrxRs) are attractive targets for anticancer drugs development. Xanthohumol (Xn), a naturally occurring polyphenol chalcone from hops, has received increasing attention because of its multiple pharmacological activities. We synthesized Xn and its 43 analogues and discovered that compound 13n displayed the highest cytotoxicity toward HeLa cells (IC50 = 1.4 μM). Structure-activity relationship study indicates that the prenyl group is not necessary for cytotoxicity, and introducing electron-withdrawing group, especially on the meta-position, is favored. In addition, methylation of the phenoxyl groups generally improves the potency. Mechanistic study revealed that 13n selectively inhibits TrxR and induces reactive oxygen species and apoptosis in HeLa cells. Cells overexpressing TrxR are resistant to 13n insult, while knockdown of TrxR sensitizes cells to 13n treatment, highlighting the physiological significance of targeting TrxR by 13n. The clarification of the structural determinants for the potency would guide the design of novel potent molecules for future development.

Topics: Antineoplastic Agents, Phytogenic; Apoptosis; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; Flavonoids; HeLa Cells; Hep G2 Cells; HL-60 Cells; Humans; Molecular Structure; Propiophenones; Structure-Activity Relationship; Thioredoxin-Disulfide Reductase; Tumor Cells, Cultured

2015