作者: Tomczyk, Michał ; Kapral-Piotrowska, Justyna ; Jakimiuk, Katarzyna ; Wiater, Adrian ; Pawlikowska-Pawlęga, Bożena ; Gruszecki, Wiesław I ; Strawa, Jakub W

In this report, we discuss the effects of undescribed flavone derivatives, HZ4 and SP9, newly isolated from the aerial parts of Hottonia palustris L. and Scleranthus perennis L. on membranes. Interaction of flavonoids with lipid bilayers is important for medicinal applications. The experiments were performed with FTIR and NMR techniques on liposomes prepared from DPPC (dipalmitoylphosphatidylcholine) and EYPC (egg yolk phosphatidylcholine). The data showed that the examined polyphenols incorporate into the polar head group region of DPPC phospholipids at both 25 °C and 45 °C. At the lower temperature, a slight effect in the spectral region of the ester carbonyl group is observed. In contrast, at 45 °C, both compounds bring about the changes in the spectral regions attributed to antisymmetric and symmetric stretching vibrations of CH₂ and CH₃ moieties. Similarly, as in DPPC lipids, the tested compounds interact with the fingerprint region of the polar head groups of the EYPC lipids and cause its reorganization. The outcomes obtained by NMR analyses confirmed the localization of both flavonoids in the polar heads zone. Unraveled effects of HZ4 and SP9 in respect to lipid bilayers can partly determine their biological activities and are crucial for their usability in medicine as disease-preventing phytochemicals.

2021-07-25·Zhen ci yan jiu = Acupuncture research

[Effect of electroacupuncture on 5-HT7R in gastric antrum and colon tissues of functional diarrhea rats].

Article

作者: Li, Chun-Yu ; Wang, Xiao-Yan ; Wang, Shi-Jun ; Zhang, Ya-Nan ; Gao, Shan-Shan ; Fu, Chen-Yu

目的：观察电针不同穴位对功能性腹泻(FD)模型大鼠胃窦、结肠中五羟色胺7受体(5-HT7R)表达的影响，探讨电针对FD大鼠胃肠运动的调节机制及经穴脏腑相关性。方法：将40只雄性SD大鼠随机分为正常组、模型组、足三里组、阴陵泉组、阴谷组，每组8只。连续14 d用束缚+冷刺激+饮食失节的复合病因法制备FD大鼠模型。模型复制成功后，足三里组、阴陵泉组、阴谷组大鼠给予相应穴位电针干预30 min，强度0.5 mA，1次/d，共7 d。计算各组大鼠粪便含水量并按Bristol分级进行粪便性状评分，测定胃内残留率、小肠推进率，并采用免疫组织化学法检测胃窦、结肠中5-HT7R蛋白的表达，实时荧光定量PCR法检测胃窦、结肠中5-HT7R mRNA的表达。结果：与正常组比较，模型组大鼠粪便含水量、粪便性状评分、小肠推进率均明显升高(P<0.01)，胃内残留率降低(P<0.01)，胃窦、结肠组织中5-HT7R蛋白和mRNA表达升高(P<0.05)。与模型组比较，足三里组、阴陵泉组大鼠粪便含水量、粪便性状评分、小肠推进率均明显降低(P<0.01，P<0.05)，胃内残留率明显升高(P<0.01)，胃窦与结肠中5-HT7R蛋白和mRNA表达明显降低(P<0.05)。与阴谷组比较，足三里组、阴陵泉组大鼠粪便含水量、粪便性状评分均明显降低(P<0.01，P<0.05)，胃内残留率升高(P<0.01)，胃窦中5-HT7R蛋白和mRNA、结肠中5-HT7R蛋白表达降低(P<0.05)；足三里组小肠推进率降低(P<0.05)，结肠中5-HT7R mRNA表达降低（P<0.05）。结论：电针“足三里”“阴陵泉”能改善FD模型大鼠的症状，其机制可能与降低胃窦、结肠组织的5-HT7R蛋白和mRNA的表达有关，且该作用具有一定的穴位特异性。.

2018-06-01·3 Biotech4区 · 工程技术

Heliomycin and tetracinomycin D: anthraquinone derivatives with histone deacetylase inhibitory activity from marine sponge-associated Streptomyces sp. SP9

4区 · 工程技术

Article

作者: Hebishy, Ali Mohamed Salah ; Ali, Neama Hassan ; Elmallah, Mohammed Ismail Youssef ; Faraag, Ahmed Hassan Ibrahim ; Abdelfattah, Mohamed Saleh

Several actinomycetes strains were isolated from different marine sponges collected from the Red Sea shore in Egypt. The efficiency of their crude extracts to inhibit histone deacetylase (HDAC) enzyme was investigated in the nuclear extract of Hela cell line. The crude extract corresponding to Streptomyces sp. SP9 isolated from the marine sponge Pseudoceratina arabica showed a promising HDAC inhibitory activity with 64 and 81% at 50 and 100 µg/ml, respectively. The strain was identified as Streptomyces sp. by phylogenetic analyses based on its 16S rRNA gene sequence. The major compounds of Streptomyces sp. SP9 were isolated and purified by different chromatographic methods. The chemical structure of the isolated compounds was identified on the basis of their spectroscopic data including mass, ¹H and ¹³C NMR, and by comparison with those of authenticated samples. Structures of compounds 1 and 2 were established as heliomycin and tetracenomycin D, respectively. These compounds exhibited HDAC inhibitory activities with IC₅₀ values of 29.8 ± 0.04 µg/ml for heliomycin (1) and 10.9 ± 0.02 µg/ml for tetracenomycin D (2). A computational docking study for compounds 1 and 2 against HDAC1, HDAC2, and HDAC3 was performed to formulate a hypothetical mechanism by which the tested compounds inhibit HDAC. Tetracenomycin D (2) showed a good binding interactions with HDAC2 (- 5.230 kcal/mol) and HDAC3 (- 6.361 kcal/mol).

100 项与 SP-9 相关的药物交易

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