Emodin succinyl ester inhibits malignant proliferation and migration of hepatocellular carcinoma by suppressing the interaction of AR and EZH2

Khan, Hanif; Jia, Wei; Yu, Zhuo; Zaib, Tahir; Feng, Jun; Jiang, Yanan; Song, Haibin; Bai, Yunlong; Yang, Baofeng; Feng, Hai

doi:10.1016/j.biopha.2020.110244

Cited by 20 publications

(10 citation statements)

References 23 publications

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“…Indeed, there are now several reports of the development of novel emodin-containing drugs to improve its anti-cancer efficacy. 34,42,57,58 This section will address the anti-cancer properties of emodin derivatives and/or formulations as they relate to colon, liver, pancreatic cancer.…”

Section: Anti-cancer Properties Of Emodin Derivatives and Formulationsmentioning

confidence: 99%

“…Several studies have documented improved efficacy of emodin derivatives in liver cancer. 34,42,57,58 In one study, a novel series of emodin derivatives were designed and synthesized via the introduction of an amino acid using linkers of varying lengths and composition. 34 In vitro anti-proliferation tests revealed that these derivatives exhibited moderate to potent anti-proliferative activity against HepG2 cells.…”

Section: Anti-cancer Properties Of Emodin Derivatives and Formulationsmentioning

confidence: 99%

“…57 Similarly, emodin succinyl ester (50-200 mg/kg) dose-dependently suppressed tumorigenicity in xenograft and diethylnitrosamine (DEN)-induced HCC mouse models. 58…”

Section: Anti-cancer Properties Of Emodin Derivatives and Formulationsmentioning

confidence: 99%

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Therapeutic Potential of Emodin for Gastrointestinal Cancers

et al. 2022

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Gastrointestinal (GI) cancers cause one-third of all cancer-related deaths worldwide. Natural compounds are emerging as alternative or adjuvant cancer therapies given their distinct advantage of manipulating multiple pathways to both suppress tumor growth and alleviate cancer comorbidities; however, concerns regarding efficacy, bioavailability, and safety are barriers to their development for clinical use. Emodin (1,3,8-trihydroxy-6-methylanthraquinone), a Chinese herb-derived anthraquinone, has been shown to exert anti-tumor effects in colon, liver, and pancreatic cancers. While the mechanisms underlying emodin’s tumoricidal effects continue to be unearthed, recent evidence highlights a role for mitochondrial mediated apoptosis, modulated stress and inflammatory signaling pathways, and blunted angiogenesis. The goals of this review are to (1) highlight emodin’s anti-cancer properties within GI cancers, (2) discuss the known anti-cancer mechanisms of action of emodin, (3) address emodin’s potential as a treatment complementary to standard chemotherapeutics, (4) assess the efficacy and bioavailability of emodin derivatives as they relate to cancer, and (5) evaluate the safety of emodin.

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Section: Anti-cancer Properties Of Emodin Derivatives and Formulationsmentioning

confidence: 99%

Section: Anti-cancer Properties Of Emodin Derivatives and Formulationsmentioning

confidence: 99%

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Therapeutic Potential of Emodin for Gastrointestinal Cancers

et al. 2022

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“…AKT1 is an important regulator of the tumorigenic processes, migration, Evidence-Based Complementary and Alternative Medicine spreading, therapeutic sensitivity, resistance, survival, and proliferation of LC cells, and is a promising theragnostic target [64][65][66][67]. AR expression and activity influence angiogenesis, stemness, invasion, angiogenesis, epithelialmesenchymal transition (EMT), migration, and oncogenesis of LC cells, and it is a prognostic determinant and responsive marker for anticancer therapies [68][69][70][71][72][73]. EGFR is responsible for the modulation of proliferation, metastasis, migration, self-renewal potential, EMT, angiogenesis, anchorage-independent growth, invasion, and drug sensitivity of LC cells and tumors, and its expression and activity are implicated in the initiation, recurrence, progression, metastasis, and aggressiveness of LC in patients [74][75][76][77][78][79][80][81][82][83].…”

Section: Discussionmentioning

confidence: 99%

Investigation of Anti-Liver Cancer Activity of the Herbal Drug FDY003 Using Network Pharmacology

Lee

Park³

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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Globally, liver cancer (LC) is the sixth-most frequently occurring and the second-most fatal malignancy, responsible for 0.83 million deaths annually. Although the application of herbal drugs in cancer therapies has increased, their anti-LC activity and relevant mechanisms have not been fully studied from a systems perspective. To address these issues, we conducted a system-perspective network pharmacological investigation into the activity and mechanisms underlying the action of the herbal drug. FDY003 reduced the viability of human LC treatment. FDY003 reduced the viability of human LC cells and elevated their chemosensitivity. There were a total of 16 potential bioactive chemical components in FDY003 and they had 91 corresponding targets responsible for the pathological processes in LC. These FDY003 targets were functionally involved in regulating the survival, proliferation, apoptosis, and cell cycle of LC cells. Additionally, we found that FDY003 may target key signaling cascades connected to diverse LC pathological mechanisms, namely, PI3K-Akt, focal adhesion, IL-17, FoxO, MAPK, and TNF pathways. Overall, this study contributed to integrative mechanistic insights into the anti-LC potential of FDY003.

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“…Recently, emodin succinyl ester was synthesized to inhibit the migration and invasion of HCC cells by restraining the interaction of androgen receptor and enhancer of zeste homolog 2. In vivo tumorigenicity tests using xenograft and diethylnitrosamine-induced HCC mouse model further validated its significant efficacy in preventing HCC aggression [ 203 ]. Viewed from the metabolic perspective, ATP citrate lyase, a key enzyme responsible for generating cytosolic acetyl-CoA, was overexpressed in cancer cells to regulate stemness and metastasis.…”

Section: Modification Of Emodin For Better Therapeutic Potentialmentioning

confidence: 99%

Advances in the study of emodin: an update on pharmacological properties and mechanistic basis

Zheng

et al. 2021

Chin Med

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Rhei Radix et Rhizoma, also known as rhubarb or Da Huang, has been widely used as a spice and as traditional herbal medicine for centuries, and is currently marketed in China as the principal herbs in various prescriptions, such as Da-Huang-Zhe-Chong pills and Da-Huang-Qing-Wei pills. Emodin, a major bioactive anthraquinone derivative extracted from rhubarb, represents multiple health benefits in the treatment of a host of diseases, such as immune-inflammatory abnormality, tumor progression, bacterial or viral infections, and metabolic syndrome. Emerging evidence has made great strides in clarifying the multi-targeting therapeutic mechanisms underlying the efficacious therapeutic potential of emodin, including anti-inflammatory, immunomodulatory, anti-fibrosis, anti-tumor, anti-viral, anti-bacterial, and anti-diabetic properties. This comprehensive review aims to provide an updated summary of recent developments on these pharmacological efficacies and molecular mechanisms of emodin, with a focus on the underlying molecular targets and signaling networks. We also reviewed recent attempts to improve the pharmacokinetic properties and biological activities of emodin by structural modification and novel material-based targeted delivery. In conclusion, emodin still has great potential to become promising therapeutic options to immune and inflammation abnormality, organ fibrosis, common malignancy, pathogenic bacteria or virus infections, and endocrine disease or disorder. Scientifically addressing concerns regarding the poor bioavailability and vague molecular targets would significantly contribute to the widespread acceptance of rhubarb not only as a dietary supplement in food flavorings and colorings but also as a health-promoting TCM in the coming years.

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Emodin succinyl ester inhibits malignant proliferation and migration of hepatocellular carcinoma by suppressing the interaction of AR and EZH2

Cited by 20 publications

References 23 publications

Therapeutic Potential of Emodin for Gastrointestinal Cancers

Therapeutic Potential of Emodin for Gastrointestinal Cancers

Investigation of Anti-Liver Cancer Activity of the Herbal Drug FDY003 Using Network Pharmacology

Advances in the study of emodin: an update on pharmacological properties and mechanistic basis

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