MOLECULES
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2024
·Vol. 29
·期 1
·278
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IF 4.2
Shunfang Liu,Yaozhen He,Minding Feng,Yongtong Huang,Wenhao Wu,Jiu Wang
Arctigenin (ATG) is a broad-spectrum antitumor drug with an excellent inhibitory effect on malignant tumors such as breast cancer, glioblastoma, liver cancer, and colon cancer. However, the clinical application of ATG is limited by its poor water solubility and quick hydrolysis in the liver, intestine, and plasma, which might hinder its application. Sialic acid (SA) recognizes selectin receptors overexpressed on the surface of tumor-associated macrophages. In this study, SA was conjugated with octadecylamine (ODA) to prepare SA-ODA, which was employed to prepare SA functionalized nanoliposomes (SA-Lip) to achieve breast cancer targeting. The formulations were finely optimized using the Box–Behnken design to achieve higher ATG loading. The size, ζ potential, entrapment efficiency, drug loading, and release behavior of ATG@SA-Lip were fully investigated in comparison with conventional ATG@Lip. The ATG@SA-Lip displayed more potent cytotoxicity and higher cellular internalization compared to ATG@Sol and ATG@Lip in both MCF7 and 4T1 cells. Notably, ATG@SA-Lip showed the lowest impact on the immune system. Our study demonstrates that SA-Lip has strong potential as a delivery system for the targeted delivery of ATG.Keywords:sialic acid receptor;nanoliposomes;targeted delivery;arctigenin;antitumor in vivo
研究领域:
药学
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肿瘤学
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纳米技术
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CARBOHYDRATE CHEMISTRY
·
2019
·
IF 0.828
Yemin Xue,Zonghui Zhang,Jingjing Hou,Zhigang Cao,Lingxian Zhang,Fen Lou,Puxu Xu
For preparation of resveratrol and arctigenin from peanut hulls and arctium lappa fruits, respectively, a recombinant β-glucosidase (TmBglA) from hyperthermophile Thermotoga maritima was purified and characterized. The hydrolytic activity was the highest at 90 °C and pH 6.2 for arctiin with Km of 1.61 mM and kcat of 197.4 s−1, and 90 °C and 5.8 for polydatin with Km of 0.38 mM and kcat of 47.6 s−1. The enzyme produced 215.4 mg L−1 resveratrol and 355.7 mg L−1 arctigenin from 400 mg L−1 polydatin and 540 mg L−1 arctiin after 60 min of incubation at 80 °C, with capable of hydrolyzing up to 92.1 and 94.9% of polydatin and arctiin, respectively. The enzymatic hydrolysis of peanut hulls and fructus arctii displayed a conversion yield of 3.8 and 0.33 mg resveratrol and arctigenin per gram of substrate material flour, respectively. Of the reported β-glucosidase, TmBglA exhibited the highest thermostability, kcat, kcat/Km, and conversion productivity for hydrolyzing polydatin and arctiin, and has great potential applications in functional food and medicine production.
研究领域:
生物化学
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酶工程
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功能性食品
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医药学
✓ 已验证
DOI
高影响因子
Antioxidants
·
2024
·Vol. 13
·期 6
·684
·
IF 6
Siqi Chen,Yajing Li,Enchan Wu,Qing Li,Lan Xiang,Jianhua Qi
Aging is often accompanied by irreversible decline in body function, which causes a large number of age-related diseases and brings a huge economic burden to society and families. Many traditional Chinese medicines have been known to extend lifespan, but it has still been a challenge to isolate a single active molecule from them and verify the mechanism of anti-aging action. Drugs that inhibit senescence-associated secretory phenotypes (SASPs) are called “senomorphics”. In this study, arctigenin (ATG), a senomorphic, was screened from the Chinese medicineFructus arctiiusing K6001 yeast replicative lifespan. Autophagy, oxidative stress, and telomerase activity are key mechanisms related to aging. We found that ATG may act through multiple mechanisms to become an effective anti-aging molecule. In exploring the effect of ATG on autophagy, it was clearly observed that ATG significantly enhanced autophagy in yeast. We further verified that ATG can enhance autophagy by targeting protein phosphatase 2A (PP2A), leading to an increased lifespan. Meanwhile, we evaluated the antioxidant capacity of ATG and found that ATG increased the activities of the antioxidant enzymes, thereby reducing reactive oxygen species (ROS) and malondialdehyde (MDA) levels to improve the survival of yeast under oxidative stress. In addition, ATG was able to increase telomerase activity by enhancing the expression ofEST1,EST2, andEST3genes in yeast. In conclusion, ATG exerts anti-aging effects through induction of autophagy, antioxidative stress, and enhancement of telomerase activity in yeast, which is recognized as a potential molecule with promising anti-aging effects, deserving in-depth research in the future.
研究领域:
药理学
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衰老研究
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分子生物学
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中药学
✓ 已验证
DOI
PubMed
高影响因子
AQUACULTURE
·
2022
·
IF 5.135
Yang Hu,Huan Wang,Lei Liu,Jia-yun Yao,Jiong Chen
Micropterus salmoides rhabdovirus (MSRV) is a fish viral pathogen that causes severe disease and huge economic losses in the largemouth bass (M. salmoides ) farming industry in aquaculture. Currently, there is no treatment strategy for MSRV. Thus, anti-MSRV drugs are urgently needed. In this study, it was found that the ethanol extract of Arctium lappa L. had good anti-MSRV activity, and the inhibition rate of G and N protein expression of MSRV was >95%. Further studies showed that arctigenin, a natural component of A. lappa L., could inhibit MSRV infection in a dose-dependent mode on grass carp ovary (GCO) cells. In addition, arctigenin could effectively inhibit the cytopathic changes caused by virus and significantly reduce the titer of virus. The pretreatment and post-treatment experiments showed that arctigenin had preventive and therapeutic effects on MSRV infection. TOA and TOR studies indicated that arctigenin may play an antiviral role in the early stage of virus replication. Interestingly, we found that arctigenin treatment significantly inhibited mitochondrial damage in GCO cells by preserving mitochondrial function and maintaining mitochondrial membrane potential levels (ΔΨm). More importantly, arctigenin was also effective against MSRV infection in largemouth bass. The survival rate of infected fish was increased by 16% and 20% respectively by adding 0.5% and 1% arctigenin in the diet. Additionally, the virus titer of the largemouth bass in the arctigenin treatment group was significantly decreased. In summary, arctigenin is confirmed to be a natural product with the excellent anti-MSRV activity, and its application in the treatment of MSRV is promising in aquaculture.
研究领域:
水产养殖
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病毒学
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药理学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2020
·
IF 3.943
Jia-Hui Cheng,Xiang Xu,Ying-Biao Li,Xu-Dong Zhao,Fumie Aosai,Su-Yun Shi,Cheng-Hua Jin,Jing-Shu Piao,Juan Ma,Hu-Nan Piao,Xue-Jun Jin,Lian-Xun Piao
Toxoplasma gondii ( T. gondii ) is a known neurotropic protozoan that remains in the central nervous system and induces neuropsychiatric diseases in intermediate hosts. Arctigenin (AG) is one of the major bioactive lignans of the fruit Arctium lappa L. and has a broad spectrum of pharmacological activities such as neuroprotective, anti-inflammatory and anti- T. gondii effects. However, the effect of AG against depressive behaviors observed in T. gondii -infected hosts has not yet been clarified. In the present study, we analyzed the effects of AG against T. gondii -induced depressive behaviors in intermediate hosts using a microglia cell line (BV2 cells) and brain tissues of BALB/c mice during the acute phase of infection with the RH strain of T. gondii . AG attenuated microglial activation and neuroinflammation via the Toll-like receptor/nuclear factor-kappa B (NF-κB) and tumor necrosis factor receptor 1/NF-κB signaling pathways, followed by up-regulating the dopamine and 5-hydroxytryptamine levels and inhibiting the depression-like behaviors of hosts. AG also significantly decreased the T. gondii burden in mouse brain tissues. In conclusion, we elucidated the effects and underlying molecular mechanisms of AG against depressive behaviors induced by T. gondii infection.
研究领域:
神经科学
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药理学
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传染病学
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免疫学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）