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白皮杉醇
FOOD RESEARCH INTERNATIONAL · 2022 · IF 7.425

The bioactivity of prenylated stilbenoids and their structure-activity relationship

Shengtao Bo,Sui Kiat Chang,Youxia Shan,Yipeng Chen,Hui Liu,Bailin Li,Yueming Jiang,Hong Zhu,Bao Yang

Dietary prenylated stilbenoids present in many food resources, and have good bioactivities. However, their structure–activity relationships are rarely reported. In this work, eighteen C- and O-prenylated stilbenoids were chemically semisynthesized using one-step approach. They all could inhibit sugar digestive enzymes, including α-glucosidase and α-amylase. 4-Geranyl piceatannol from jackfruit showed the strongest activity by suppressing dipeptidyl peptidase-IV (DPP-IV) activity. The enzyme inhibition kinetics were measured and the inhibition mechanism was revealed. Evaluation of antioxidant activity highlighted that the introduction of prenyl with increasing prenyl chain length can significantly increase the antioxidant activity of stilbenoids. Our results suggested that prenylated stilbenoids could be used as functional food additives to decrease postprandial blood sugar levels by inhibiting sugar digestive enzymes and DPP-IV. Prenylated stilbenoids present remarkable DPP-IV inhibitory activity, providing more useful information for the prevention of type 2 diabetes.

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Frontiers in Veterinary Science · 2022 · IF 3.471

The anti-Toxoplasma activity of the plant natural phenolic compound piceatannol

Jiang Yucong,Shi Yuehong,Hu Dandan,Song Xingju

Toxoplasma gondii is an obligate intracellular protozoan that infects the nucleated cells of warm-blooded animals and causes life-threatening disease in immunocompromised patients. Due to the limited effectiveness and prominent side effects of existing drugs, there is an urgent need to develop new therapeutic options against T. gondii. Piceatannol is a natural plant compound with multiple functions such as antibacterial, antileukemic and antiparasitic activities. In the present study, the anti-T. gondii activity of piceatannol was evaluated. Piceatannol potently inhibited Toxoplasma with a half-maximal effective concentration (EC50) of 28.10 μM. Piceatannol showed a significant inhibitory effect on intracellular proliferation, inhibiting intracellular parasites at a rate of 98.9% when treatment with 100 μM piceatannol. However, the invasion ability of tachyzoites was not affected by piceatannol. By immunofluorescence assay, we noted that the parasite showed abnormalities in cell division after exposure to piceatannol. To determine the in vivo effect of piceatannol on acute infection, a model was established by infecting BALB/c mice with the virulent RH strain of T. gondii. Mice infected with 500 tachyzoites showed a significant therapeutic effect when treated with 15 mg/kg of piceatannol. These results suggest that piceatannol is a promising drug for the treatment of T. gondii.

CAS / MDL: 10083-24-6
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FASEB JOURNAL · 2018 ·Vol. 32 ·期 6 ·3398-3410 · IF 5.595

Tetrandrine attenuates the bone erosion in collagen-induced arthritis rats by inhibiting osteoclastogenesis via spleen tyrosine kinase

Yugai Jia,Yumeng Miao,Mengfan Yue,Mei Shu,Zhifeng Wei,Yue Dai

Tetrandrine, a bisbenzylisoquinoline alkaloid, was previously demonstrated to attenuate inflammation and cartilage destruction in the ankles of mice with collagen-induced arthritis (CIA). Here, we explored the underlying mechanism by which tetrandrine prevented arthritis-induced bone erosion by focusing on the differentiation and function of osteoclasts. We found that daily administration of tetrandrine (30 mg/kg) markedly reduced the bone damage and decreased the number of osteoclasts in CIA rats. In vitro , tetrandrine inhibited receptor activator of NF-κB ligand (RANKL)-induced osteoclastogenesis at the early stage and reduced the expressions of osteoclast-related marker genes. In bone marrow-derived macrophages and RAW264.7 cells, tetrandrine inhibited RANKL-induced translocation of NF-κB-p65 and nuclear factor of activated T cell 1 (NFATc1) through suppressing spleen tyrosine kinase (Syk)-Bruton's tyrosine kinase-PLCγ2-Ca 2+ signaling. Of interest, tetrandrine did not affect the phosphorylation of immunoreceptor tyrosine-based activation motifs, the conventional upstream of Syk, but it inhibited the activity of Syk by enhancing its ubiquitination and degradation. The anti–osteoclastogenesis effect of tetrandrine nearly disappeared when it was used in combination with the Syk inhibitor piceatannol or in constitutively activated Syk-overexpressing cells. Taken together, tetrandrine attenuated CIA-induced bone destruction by inhibiting osteoclastogenesis through hindering the translocation of NF-κB-p65 and NFATc1 via reducing the activation of Syk.—Jia Y., Miao, Y., Yue, M., Shu, M., Wei, Z., Dai Y. Tetrandrine attenuates the bone erosion in collagen-induced arthritis rats by inhibiting osteoclastogenesis via spleen tyrosine kinase. FASEB J. 32, 3398–3410 (2018). www.fasebj.org

CAS / MDL: 104987-11-3 10083-24-6
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Scientific Reports · 2017 · IF 4.259

Possible Involvement of F1F0-ATP synthase and Intracellular ATP in Keratinocyte Differentiation in normal skin and skin lesions

Xie Xiaoyun,Han Chaofei,Zeng Weiqi,Chen Chen,Lu Lixia,Liu Queping,Peng Cong,Zhao Shuang,Su Juan,Chen Xiang

The F1F0-ATP synthase, an enzyme complex, is mainly located on the mitochondrial inner membrane or sometimes cytomembrane to generate or hydrolyze ATP, play a role in cell proliferation. This study focused on the role of F1F0-ATP synthase in keratinocyte differentiation, and its relationship with intracellular and extracellular ATP (InATP and ExATP). The F1F0-ATP synthase β subunit (ATP5B) expression in various skin tissues and confluence-dependent HaCaT differentiation models was detected. ATP5B expression increased with keratinocyte and HaCaT cell differentiation in normal skin, some epidermis hyper-proliferative diseases, squamous cell carcinoma, and the HaCaT cell differentiation model. The impact of InATP and ExATP content on HaCaT differentiation was reflected by the expression of the differentiation marker involucrin. Inhibition of F1F0-ATP synthase blocked HaCaT cell differentiation, which was associated with a decrease of InATP content, but not with changes of ExATP. Our results revealed that F1F0-ATP synthase expression is associated with the process of keratinocyte differentiation which may possibly be related to InATP synthesis.

CAS / MDL: 1404-19-9 10083-24-6
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2017 · IF 2.329

Different thermal drying methods affect the phenolic profiles, their bioaccessibility and antioxidant activity in Rhodomyrtus tomentosa (Ait.) Hassk berries

Guanghe Zhao,Ruifen Zhang,Lei Liu,Yuanyuan Deng,Zhencheng Wei,Yan Zhang,Yongxuan Ma,Mingwei Zhang

Extended shelf life and convenient industrial application have led to increasingly wide use of drying technology in fruits and vegetables processing. However, drying process usually has a negative effect on the active ingredients in fruits and vegetables. In this study, the effects of three thermal drying methods (hot air drying (HD), microwave drying (MD) and combined microwave-hot-air-drying (CD)) on phenolic profiles, their bioaccessibility and antioxidant activity in Rhodomyrtus tomentosa berries were estimated. The total phenolics, flavonoids and anthocyanins contents of CD-berries were significantly higher than those of HD- and MD-ones. CD-berries had higher contents of individual phenolics and showed stronger antioxidant activity than HD- and MD-ones. Conversely, the bioaccessibility of phenolics in HD-berries was remarkably higher than that of MD- and CD-ones, although the latter 2 provided more bioaccessible phenolics than the former after in vitro gastrointestinal digestion. Thus, combined microwave-hot-air-drying (CD) is a more suitable drying technique for Rhodomyrtus tomentosa berries to maintain their phenolics and antioxidant activity.

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