Anti-hepatitis B virus activity of wogonin in vitro and in vivo

Guo, Qinglong; Zhao, Li; Qin, You; Yang, Yong; Gu, Hong-Yan; GuoLiang, Song; Lu, Na; Xin, Jian

doi:10.1016/j.antiviral.2007.01.002

Cited by 163 publications

(100 citation statements)

References 19 publications

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“…The anti-HBV activity of wogonin was already reported in 2000, demonstrating its ability to suppress hepatitis B surface antigen (HBsAg) secretion in cell culture [30] . Recently, the suppression of both HBsAg and hepatitis B e-antigen (HBeAg) secretion was shown with an IC50 of 4 µg/mL [31] . Moreover, the HBV-DNA level was reduced in a dose-dependent manner.…”

Section: -Arylbenzofuran Derivativesmentioning

confidence: 99%

“…Furthermore, immunohistological staining of human HBV-transgenic mouse livers confirmed the potential of wogonin in HBsAg reduction. Therefore, it is currently under early development as anti-HBV drug [31] . Another flavonoid molecule, ellagic acid, isolated from Phyllanthus urinaria exhibits a rather peculiar anti-HBV function.…”

Section: -Arylbenzofuran Derivativesmentioning

confidence: 99%

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Natural products as promising drug candidates for the treatment of hepatitis B and C

Wohlfarth

Efferth

2008

Acta Pharmacol Sin

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Hepatitis B virus (HBV) or hepatitis C virus (HCV) infections are a major threat worldwide. Combination therapy of interferon-α and ribavirin is currently the treatment of choice for HCV-infected patients. However, this regimen is only effective in approximately 50% of patients and provokes severe side-effects. Numerous natural alternatives for treating HCV have been suggested. Deoxynojirimycin and its derivatives are iminosugars which exert anti-HCV activity by inhibiting α-glucosidases. A non-immunosuppressive derivate of cyclosporine A, NIM811, exerts anti-HCV activity by binding to cyclophilin. Other natural products with promising anti-HCV activity are 2-arylbenzofuran derivatives, Mellein, and pseudoguaianolides. For HBV treatment, several drugs are available, specifically targeting the virus polymerase (lamivudine, entecavir, telbivudine, and adefovir dipivoxil). The efficacy of these drugs is hampered by the development of resistance due to point mutations in the HBV polymerase. Due to drug resistance and adverse side-effects, the search for novel drugs is mandatory. Wogonin, ellagic acid, artemisinin and artesunate, chrysophanol 8-O-β-D-glucoside, saikosaponin C, and protostane triterpenes are active against HBV. Natural products need to be investigated in more detail to explore their potential as novel adjuncts to established HBV or HCV therapy.

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Section: -Arylbenzofuran Derivativesmentioning

confidence: 99%

Section: -Arylbenzofuran Derivativesmentioning

confidence: 99%

Natural products as promising drug candidates for the treatment of hepatitis B and C

Wohlfarth

Efferth

2008

Acta Pharmacol Sin

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“…Wogonin (5,7-dihydroxy-8-methoxyflavone, WG, Figure 1), a naturally occurring flavonoid isolated from the root of Scutellaria baicalensis Georgi, is a traditional Chinese herbal medicine widely used in the treatment of inflammatory conditions. WG has attracted considerable attention due to multiple pharmacological benefits (Shieh et al, 2000;Chi et al, 2001;Guo et al, 2007;Park et al, 2007;Li-Weber, 2009;Lim et al, 2010) including anti-inflammatory, anti-oxidant, anti-hepatitis B virus, anticonvulsant and neuro-protective effects, as well as anti-cancer effects. With new data constantly emerging, the promising therapeutic potential of WG as an anti-tumor agent both in vitro and in vivo has been made clear.…”

Section: Introductionmentioning

confidence: 99%

A wogonin-loaded glycyrrhetinic acid-modified liposome for hepatic targeting with anti-tumor effects

Tian¹,

Wang

Wang³

et al. 2013

Drug Delivery

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Liver cancer has become one of the most common fatal cancers worldwide, with morbidity rates increasing each year. Wogonin (WG) is an attractive candidate for the development of new anti-cancer drugs. In this study, a novel glycyrrhetinic acid (GA)-modified WG liposome was developed for use in targeted anti-cancer therapy. Three types of WG preparations were investigated: free wogonin in solution (WG), passively targeted wogonin liposomes (WG-Lip) and GA-modified wogonin liposomes (GA-WG-Lip). The entrapment efficiency, size and zeta potential were measured. Cellular uptake, cytotoxicity, in vivo bio-distribution and anti-tumor efficacy were also investigated. Addition of GA to the liposomes did not diminish the high entrapment efficiency observed in the liposomes without GA. GA-WG-Lip showed the greatest uptake and had an IC 50 value 1.46 times higher than that of WG-Lip. The GA-modified liposomes rapidly accumulated in the liver with a long retention time, and also displayed a better tumor inhibitory ratio than that of the unmodified liposomes. Overall, the data indicated that use of the GA-modified WG liposomes conferred improvements in biodistribution, accumulation at the tumor and therapeutic efficacy, perhaps due to increased receptor-mediated uptake of liposomes by liver-targeted cells. Together, these data show that GA-WG-Lip is a promising means of targeted therapy for liver cancer.

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“…Flavonoids are associated with multiple biological effects, including antitumor, anti-oxidation, anti-inflammation, antiviral and hepatoprotective activities, as well as in the prevention of cardiovascular diseases (11)(12)(13)(14)(15)(16). Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is extracted from Artemisia asiatica (A. asiatica) Nakai, and this isolated flavonoid contains pharmacologically active ingredients.…”

Section: Introductionmentioning

confidence: 99%

Application of eupatilin in the treatment of osteosarcoma

Wu²,

Dong

et al. 2015

Oncology Letters

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Abstract. 5,7-dihydroxy-3' ,4' ,6-trimethoxyflavone, commonly known as eupatilin, is a traditional Asian medicinal plant, which is mainly used for the treatment of gastritis, as well as its use as an anti-inflammatory agent. Eupatilin is a bioactive compound; however, its effects on osteosarcoma (OS) have remained to be elucidated. Therefore, the present study aimed to investigate the effects of eupatilin on this malignant bone tumor, using the U-2 OS cell line. The experimental results revealed that eupatilin inhibited U-2 OS cell growth in a concentration-dependent manner and induced G2/M phase cell cycle arrest and apoptosis. Additionally, western blot analysis indicated that eupatilin was able to trigger the mitochondrial apoptotic pathway, demonstrated by the enhanced Bax/B cell lymphoma-2 ratio, decrease in mitochondrial membrane potential, release of cytochrome c, caspase-3 and -9 activation and poly(ADP-ribose)polymerase cleavage detected in the U-2 OS cells. These results indicated that eupatilin was able to inhibit U-2 OS cancer cell proliferation by the induction of apoptosis via the mitochondrial intrinsic pathway. Eupatilin may therefore represent a novel anticancer drug for use in the treatment of osteosarcoma. IntroductionOsteosarcoma (OS) is considered to be one of the most common and aggressive primary bone tumors of the musculoskeletal system, and predominantly occurs in childhood and adolescence (1,2). There are various potential treatments for OS, including radiotherapy, surgery and chemotherapy; however, the results of these available treatments remain unsatisfactory (3). Significant nephrotoxic and cardiotoxic side-effects are induced by chemopreventative medicines, thereby limiting the efficacy of their use in the treatment of OS (4). Manipulation of apoptosis is one of the major targets in the treatment of cancer.Apoptosis describes genetically-dependent programmed cell death type I, and is characterized by cell shrinkage, signal transduction (5), nucleic condensation (6,7) and DNA and cellular protein degradation (8). Previous studies have revealed that few therapeutic treatments exist that result in an enhanced ability of human tumor cell lines to undergo apoptosis (9,10). Therefore, the development of novel agents to induce or increase the phenomenon of apoptosis present a promising approach for the development of cancer treatments. Novel inducers of apoptosis may provide alternative and efficacious therapeutic anticancer strategies.Flavonoids are associated with multiple biological effects, including antitumor, anti-oxidation, anti-inflammation, antiviral and hepatoprotective activities, as well as in the prevention of cardiovascular diseases (11-16). Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is extracted from Artemisia asiatica (A. asiatica) Nakai, and this isolated flavonoid contains pharmacologically active ingredients. Eupatilin has been demonstrated to exert anticancer, anti-oxidative and anti-inflammatory effects (17). A previous report indicated that Stillen™ (DA-9601...

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Anti-hepatitis B virus activity of wogonin in vitro and in vivo

Cited by 163 publications

References 19 publications

Natural products as promising drug candidates for the treatment of hepatitis B and C

Natural products as promising drug candidates for the treatment of hepatitis B and C

A wogonin-loaded glycyrrhetinic acid-modified liposome for hepatic targeting with anti-tumor effects

Application of eupatilin in the treatment of osteosarcoma

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