Therapeutic Effect of Arctiin and Arctigenin in Immunocompetent and Immunocompromised Mice Infected with Influenza A Virus

Hayashi, Kyoko; Narutaki, Kazuto; Nagaoka, Yasuo; Hayashi, Toshimitsu; Uesato, Shinichi

doi:10.1248/bpb.33.1199

Cited by 142 publications

(81 citation statements)

References 22 publications

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“…It has been reported to have multiple biological activities, such as anti-tumor, [1][2][3][4][5][6][7] anti-inflammatory, [8][9][10] and anti-viral [11][12][13][14][15] activities. Although ARG exhibits many pharmacological activities in vitro, ARG is too insoluble to be absorbed by the body, which limits its clinical applications.…”

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confidence: 99%

The Synthesis and Evaluation of Arctigenin Amino Acid Ester Derivatives

Cai

Yang

Jia

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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The use of arctigenin (ARG), a traditional medicine with many pharmacological activities, has been restricted due to its poor solubility in water. Five amino acid derivatives of ARG have been synthesized using glycine, o-alanine, valine, leucine, and isoleucine, which have t-butyloxy carbonyl (BOC) as a protective group. In this study, we examined the effects of removing these protective groups. The results showed that the amino acid derivatives have better solubility and nitrite-clearing ability than ARG. Among the compounds tested, the amino acid derivatives without protective group were the best. Based on these results, ARG and its two amino acid derivatives without protective group (ARG8, ARG10) were selected to evaluate their anti-tumor activity in vivo at a dosage of 40 mg/kg. The results indicated that ARG8 and ARG10 both exhibit more anti-tumor activity than ARG in H 22 tumor-bearing mice. The tumor inhibition rates of ARG8 and ARG10 were 69.27 and 43.58%, which was much higher than ARG. Furthermore, the mice treated with these compounds exhibited less damage to the liver, kidney and immune organs compared with the positive group. Furthermore, ARG8 and ARG10 improved the serum cytokine levels significantly compared to ARG. In brief, this study provides a method to improve the water solubility of drugs, and we also provide a reference basis for new drug development.

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confidence: 99%

The Synthesis and Evaluation of Arctigenin Amino Acid Ester Derivatives

Cai

Yang

Jia

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Arctigenin (purity >99%), isolated from dried seeds of A. lappa as previously described [17] , was provided by Dr Li-hong HU. Penicillin, streptomycin, Brefeldin A, compound C, 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR), D-glucose, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and propidium iodide (PI) were purchased from Sigma (St Louis, Mo, USA).…”

Section: Reagents and Antibodiesmentioning

confidence: 99%

Arctigenin alleviates ER stress via activating AMPK

Sun

et al. 2012

Acta Pharmacol Sin

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Aim: To investigate the protective effects of arctigenin (ATG), a phenylpropanoid dibenzylbutyrolactone lignan from Arctium lappa L (Compositae), against ER stress in vitro and the underlying mechanisms. Methods: A cell-based screening assay for ER stress regulators was established. Cell viability was measured using MTT assay. PCR and Western blotting were used to analyze gene and protein expression. Silencing of the CaMKKβ, LKB1, and AMPKα1 genes was achieved by RNA interference (RNAi). An ATP bioluminescent assay kit was employed to measure the intracellular ATP levels. Results: ATG (2.5, 5, and 10 µmol/L) inhibited cell death and unfolded protein response (UPR) in a concentration-dependent manner in cells treated with the ER stress inducer brefeldin A (100 nmol/L). ATG (1, 5, and 10 µmol/L) significantly attenuated protein synthesis in cells through inhibiting mTOR-p70S6K signaling and eEF2 activity, which were partially reversed by silencing AMPKα1 with RNAi. ATG (1-50 µmol/L) reduced intracellular ATP level and activated AMPK through inhibiting complex I-mediated respiration. Pretreatment of cells with the AMPK inhibitor compound C (25 µmol/L) rescued the inhibitory effects of ATG on ER stress. Furthermore, ATG (2.5 and 5 µmol/L) efficiently activated AMPK and reduced the ER stress and cell death induced by palmitate (2 mmol/L) in INS-1 β cells. Conclusion: ATG is an effective ER stress alleviator, which protects cells against ER stress through activating AMPK, thus attenuating protein translation and reducing ER load.

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“…Roots of A. lappa have numerous therapeutic effects, and have been used in traditional medicine for treatment of arthritis, myelination, eczema, acne, and dysphasia (7). Pharmacological studies and clinical trials also indicated that burdock roots have antiinflammatory, free radical scavenging, antioxidant, anti-tumor, anti-viral, anti-bacterial, anti-fungal, cytotoxic and genotoxic activities (8)(9)(10)(11)(12)(13)(14)(15)(16). Due to the fewer side effects associated with herbal compounds compared to chemical agents, the effect of methanolic extract of A. lappa root was evaluated in this study.…”

Section: Introductionmentioning

confidence: 99%

Effects of Methanolic Extract of Arctium lappa Root on Promastigotes and Amastigotes of Leishmania major (in vitro)

Yamchi

Dabirzadeh²,

Miri³

2016

mljgoums

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Background and Objective: Leishmania major is a flagellate protozoan parasite causing cutaneous leishmaniasis. Although pentavalent antimony compounds are the firstline drugs for leishmaniasis, their application is often accompanied by numerous limitations and side effects. Therefore, it is necessary to seek drugs of herbal origin that have fast-acting benefits and few side effects without resistance. This study aimed to evaluate the in vitro effects of methanolic extract of Arctiul lappa root on promastigotes and amastigotes of L. major.Methods: This experimental study evaluated the effects of 10, 100, 500, and 1000 µg/ml of A. lappa root methanol extract on L. major promastigotes using direct cell counting and MTT assay. The mean number of amastigotes in infected macrophages was calculated after 24 and 48 hours.Results: The half maximal inhibitory concentration (IC50) of A. lappa root methanolic extract was 131.25 µg/ml after 24 hours. The mean number of amastigotes in macrophages after 24 hours in the control group and in the A. lappa group with concentrations of 500 and 1000 µg/ml were 3.52, 2.02, and 1.27, respectively. Conclusion:The results show that the methanolic extract of A. lappa root has antileishmanial effects on the promastigotes and amastigotes of L. major in vitro.

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Therapeutic Effect of Arctiin and Arctigenin in Immunocompetent and Immunocompromised Mice Infected with Influenza A Virus

Cited by 142 publications

References 22 publications

The Synthesis and Evaluation of Arctigenin Amino Acid Ester Derivatives

The Synthesis and Evaluation of Arctigenin Amino Acid Ester Derivatives

Arctigenin alleviates ER stress via activating AMPK

Effects of Methanolic Extract of Arctium lappa Root on Promastigotes and Amastigotes of Leishmania major (in vitro)

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