Xanthohumol: An underestimated, while potent and promising chemotherapeutic agent in cancer treatment

Hamedani, Shadi Vesagh; Ebrahimzadeh, Farnoosh; Najafi, Elnaz; Shabgah, Omid Gohari; Askari, Elham; Shabgah, Arezoo Gowhari; Mohammadi, Hamed; Jadidi‐Niaragh, Farhad; Navashenaq, Jamshid Gholizadeh

doi:10.1016/j.pbiomolbio.2022.04.002

Cited by 21 publications

(14 citation statements)

References 84 publications

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“…Xanthohumol ( 1 ), a prenylated chalcone naturally occurring in hops, is known for its various biological activities, including anticancer activity [ 2 , 4 , 31 ]. Research showed that xanthohumol ( 1 ) inhibited the proliferation, migration and invasion, as well as induced apoptosis and cell cycle arrest, in many types of cancer-inhibiting carcinogenesis and metastasis [ 2 , 5 , 6 , 9 ]. Multiple crucial pathways and signaling molecules are involved in the anticancer activity of xanthohumol ( 1 ), including Akt, NF-kB, ROS and ERK1/2 [ 5 , 6 ].…”

Section: Discussionmentioning

confidence: 99%

“…Xanthohumol ( 1 ) (3′-[3″,3″-dimethylallyl]-2′,4′,4-trihydroxy-6′-methoxychalcone), the major prenylflavonoid found in the hop ( Humulus lupulus L.), is known for its various biological properties, such as anti-inflammatory, antioxidant, antibacterial, antifungal, antiplasmodial and antiviral properties [ 2 , 3 , 4 ]. One of the most important findings over the past 20 years was the discovery of its anticancer activity [ 5 , 6 , 7 , 8 , 9 ]. Xanthohumol ( 1 ) significantly suppresses the development of a wide variety of human cancer cells in vitro during the initiation, promotion and progression of carcinogenesis.…”

Section: Introductionmentioning

confidence: 99%

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Prenylated Flavonoids with Selective Toxicity against Human Cancers

Tronina

Bartmańska

Popłoński

et al. 2023

IJMS

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The antiproliferative activity of xanthohumol (1), a major prenylated chalcone naturally occurring in hops, and its aurone type derivative (Z)-6,4′-dihydroxy-4-methoxy-7-prenylaurone (2) were investigated. Both flavonoids, as well as cisplatin as a reference anticancer drug, were tested in vivo against ten human cancer cell lines (breast cancer (MCF-7, SK-BR-3, T47D), colon cancer (HT-29, LoVo, LoVo/Dx), prostate cancer (PC-3, Du145), lung cancer (A549) and leukemia (MV-4-11) and two normal cell lines (human lung microvascular endothelial (HLMEC)) and murine embryonic fibroblasts (BALB/3T3). Chalcone 1 and aurone 2 demonstrated potent to moderate anticancer activity against nine tested cancer cell lines (including drug-resistant ones). The antiproliferative activity of all the tested compounds against cancer and the normal cell lines was compared to determine their selectivity of action. Prenylated flavonoids, especially the semisynthetic derivative of xanthohumol (1), aurone 2, were found as selective antiproliferative agents in most of the used cancer cell lines, whereas the reference drug, cisplatin, acted non-selectively. Our findings suggest that the tested flavonoids can be considered strong potential candidates for further studies in the search for effective anticancer drugs.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Prenylated Flavonoids with Selective Toxicity against Human Cancers

Tronina

Bartmańska

Popłoński

et al. 2023

IJMS

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“…Xanthohumol (Xan): (1-(2,4-Dihydroxy-6-methoxy-3-(3-methylbut-2-en-1-yl)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one) ( Figure 7 ) is a prenylated chalcone flavonoid found in plants such as Humulus lupulus L. [ 183 ] with a wide spectrum of biological activities, such has anticancer [ 184 , 185 , 186 ], anti-inflammatory [ 187 ], antioxidant [ 188 ], anti-obesity [ 189 ], and antimicrobial [ 190 ] activity, as well as a protective effect on the liver [ 191 ].…”

Section: Flavonoid-loaded Polymeric Systemsmentioning

confidence: 99%

Polymeric Systems for the Controlled Release of Flavonoids

2023

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Flavonoids are natural compounds that are attracting great interest in the biomedical field thanks to the wide spectrum of their biological properties. Their employment as anticancer, anti-inflammatory, and antidiabetic drugs, as well as for many other pharmacological applications, is extensively investigated. One of the most successful ways to increase their therapeutic efficacy is to encapsulate them into a polymeric matrix in order to control their concentration in the physiological fluids for a prolonged time. The aim of this article is to provide an updated overview of scientific literature on the polymeric systems developed so far for the controlled release of flavonoids. The different classes of flavonoids are described together with the polymers most commonly employed for drug delivery applications. Representative drug delivery systems are discussed, highlighting the most common techniques for their preparation. The flavonoids investigated for polymer system encapsulation are then presented with their main source of extraction and biological properties. Relevant literature on their employment in this context is reviewed in relationship to the targeted pharmacological and biomedical applications.

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“…Xanthohumol, a flavonoid isolated from Humulus lupulus L., has anti-inflammatory, anti-tumor and anti-angiogenesis properties ( Krajka-Kuźniak et al, 2013 ; Niederau et al, 2022 ; Vesaghhamedani et al, 2022 ). It could reduce cell viability and cause G2/M arrest at the dose of 40 μM through MAPK JNK pathway for human nasopharyngeal carcinoma cells ( Hsieh et al, 2022 ).…”

Section: Natural Products Undergoing Clinical Evaluation In Pancreati...mentioning

confidence: 99%

The therapeutic potential of natural products for treating pancreatic cancer

Wang

Zhang

et al. 2022

Front. Pharmacol.

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Pancreatic cancer is one of the most malignant tumors of the digestive tract, with the poor prognosis and low 5-year survival rate less than 10%. Although surgical resection and chemotherapy as gemcitabine (first-line treatment) has been applied to the pancreatic cancer patients, the overall survival rates of pancreatic cancer are quite low due to drug resistance. Therefore, it is of urgent need to develop alternative strategies for its treatment. In this review, we summarized the major herbal drugs and metabolites, including curcumin, triptolide, Panax Notoginseng Saponins and their metabolites etc. These compounds with antioxidant, anti-angiogenic and anti-metastatic activities can inhibit the progression and metastasis of pancreatic cancer. Expecting to provide comprehensive information of potential natural products, our review provides valuable information and strategies for pancreatic cancer treatment.

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Xanthohumol: An underestimated, while potent and promising chemotherapeutic agent in cancer treatment

Cited by 21 publications

References 84 publications

Prenylated Flavonoids with Selective Toxicity against Human Cancers

Prenylated Flavonoids with Selective Toxicity against Human Cancers

Polymeric Systems for the Controlled Release of Flavonoids

The therapeutic potential of natural products for treating pancreatic cancer

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