Modulations in the biotransformation of tobacco extract and N′-nitrosonornicotine under differential dietary protein status

The modulation of the phase I and phase II biotransformation enzymes upon treatment with tobacco extract (TE) and N'-nitrosonornicotine (NNN) was investigated using male Sprague-Dawley rats fed differential protein diets. It was observed that the animals fed a low protein diet showed an overall decrease in the basal levels of hepatic and pulmonary phase I and II enzymes. TE and NNN significantly decreased the detoxifying system in the low-proteinfed animals. Animals fed 20% protein, however, showed significant increases in glutathione and glutathione S-transferase upon treatment. Furthermore, TE and NNN treatment brought about a significant depletion in the hepatic pool of vitamin A with a concomitant increase in the vitamin C levels.     

黄连提取物对动脉硬化小鼠斑块胶原类型及MMP-9/TIMP-1 比值 的影响*

目的:探讨黄连提取物对高脂喂养ApoE-/-小鼠主动脉AS斑块内胶原类型及基质金属蛋白酶-9( MMP-9)与基质金属蛋白酶组织抑制剂( TIMP-1)比值的影响,探讨黄连提取物稳定斑块的可能作用机制.方法:33只6-8周龄的ApoE基因敲除小鼠予高脂喂养13周后,待其形成成熟的AS斑块后,随机分为3组:模型组、黄连提取物组、辛伐他汀组(阳性对照组),每组11只.继续高脂喂养,并按体重比折算给予小鼠临床推荐剂量的相应药物治疗13周,处死动物,每只小鼠取主动脉根部的4个切面,行天狼猩红染色,检测各组小鼠主动脉斑块内Ⅰ、Ⅲ型胶原含量,以及斑块内MMP-9和TIMP-1的表达,计算MMP-9/TIMP-1比值.结果:给药13周后,图像分析结果显示,黄连提取物组小鼠主动脉斑块内Ⅰ型胶原含量与模型组比较有所增加,但无显著差异(P＞0.05);辛伐他汀组和黄连提取物组小鼠主动脉斑块内Ⅲ型胶原含量与模型组比较显著降低(P＜0.01).Ⅲ型/Ⅰ型胶原比值,两给药组与模型组比较均显著降低(P＜0.01).与模型组比较,黄连提取物和辛伐他汀组小鼠主动脉斑块内MMP-9的阳性表达均明显减少(P＜0.01),黄连提取物组主动脉斑块内TIMP-1的阳性表达与模型组相比明显增加(P＜0.01),辛伐他汀组TIMP-1表达有所增加,但无统计学差异(P＞0.05),两给药组之间比较无显著差异(P＞0.05).各给药组中MMP-9/TIMP-1比值均有所降低,与模型组比较具有显著差异(P＜0.05,P＜0.01).结论:在临床推荐剂量下,黄连提取物可明显改善ApoE-/-小鼠主动脉AS斑块内胶原类型,调整斑块内MMP-9/TIMP-1比值,从而促进斑块稳定.     

牡蒿提取物抗氧化作用和遗传毒性研究

本文旨在研究牡蒿提取物(Artemisia japonica Extract,AJE)对小鼠抗氧化作用和遗传毒性效果。在建立卡介苗(BCG)+脂多糖(LPS)诱导免疫性肝损伤小鼠模型的基础上,采用给小鼠灌胃不同浓度的AJE后,分别测定小鼠肝组织中丙二醛(MDA)、谷胱甘肽氧化酶(GSH-Px)和超氧化歧化酶(SOD)的活性。检查小鼠骨髓嗜多染红细胞微核率和小鼠精子畸形率。结果表明,在一定剂量范围内,牡蒿提取物有降低小鼠肝组织中MDA含量、升高GSH-Px和SOD活性的作用,微核试验和精子畸形试验结果均为阴性。说明AJE具有较强的抗氧化作用,无遗传毒性。     

灰树花子实体多糖D-组分的提取、硫酸化及免疫测定

从灰树花(Maitake)子实体中提取分离得到子实体多糖D组分,并分别考察了提取中的几个关键因素对D组分得率的影响,包括加水倍数、浸提时间、醇沉浓度、浓缩倍数。然后,对D组分进行了硫酸化修饰,得到了两种不同取代度的硫酸化多糖。最后,研究了灰树花多糖D组分及硫酸化灰树花多糖D组分对小鼠的免疫器官重量、腹腔巨噬细胞吞噬功能、血清溶血素形成及淋巴细胞转化率的影响。结果表明,在10mgkg剂量下,灰树花多糖D组分及硫酸化灰树花多糖D组分具有免疫增强作用,并且在合适的取代度下硫酸化灰树花多糖D组分比灰树花多糖D组分表现了更强的免疫调节作用。     

Physiological and Biochemical Analysis to Reveal the Molecular Basis for Black Widow Spiderling Toxicity

The early research found that the spiderlings of black widow spider (Latrodectus tredecimguttatus) exhibited obvious toxicity to animals. The present work performed a systematical analysis of the aqueous extract of newborn black widow spiderlings. The extract was shown to contain 69.42% of proteins varying in molecular weights and isoelectric points. Abdominal injection of the extract into mice and cockroaches caused obvious poisoning symptoms as well as death, with LD₅₀ being 5.30 mg/kg in mice and 16.74 µg/g in Periplaneta americana. Electrophysiological experiments indicated that the extract at a concentration of 10 µg/mL could completely block the neuromuscular transmission in isolated mouse nerve‐hemidiaphragm preparations within 21 ± 1.5 min, and 100 µg/mL extract could inhibit a certain percentage of voltage‐activated Na⁺, K⁺, and Ca²⁺ channel currents in rat dorsal root ganglion neurons. These results demonstrate that the spiderlings are rich in neurotoxic components, which play important roles in the spiderling toxicity.     

Recombinant PNPLA3 protein shows triglyceride hydrolase activity and its I148M mutation results in loss of function

The patatin-like phospholipase domain containing 3 (PNPLA3, also called adiponutrin, ADPN) is a membrane-bound protein highly expressed in the liver. The genetic variant I148M (rs738409) was found to be associated with progression of chronic liver disease. We aimed to establish a protein purification protocol in a yeast system (Pichia pastoris) and to examine the human PNPLA3 enzymatic activity, substrate specificity and the I148M mutation effect. hPNPLA3 148I wild type and 148M mutant cDNA were cloned into P. pastoris expression vectors. Yeast cells were grown in 3 L fermentors. PNPLA3 protein was purified from membrane fractions by Ni-affinity chromatography. Enzymatic activity was assessed using radiolabeled substrates. Both 148I wild type and 148M mutant proteins are localized to the membrane. The wild type protein shows a predominant lipase activity with mild lysophosphatidic acid acyl transferase activity (LPAAT) and the I148M mutation results in a loss of function of both these activities. Our data show that PNPLA3 has a predominant lipase activity and I148M mutation results in a loss of function.     

Fumigant toxicity of cassia bark and cassia and cinnamon oil compounds to <Emphasis Type="Italic">Dermatophagoides </Emphasis><Emphasis Type="Italic">farinae </Emphasis>and <Emphasis Type="Italic">Dermatophagoides pteronyssinus</Emphasis> (Acari: Pyroglyphidae)

The toxicity to adults of the American house dust mite, Dermatophagoides farinae, and the European house dust mite, Dermatophagoides pteronyssinus, of cassia bark and cassia and cinnamon oil compounds was examined using residual contact and vapour-phase toxicity bioassays. Results were compared with those of the currently used acaricides: benzyl benzoate and dibutyl phthalate. The acaricidal principles of cassia bark were identified as (E)-cinnamaldehyde and salicylaldehyde. In fabric-circle residual contact bioassays with adult D. farinae, salicylaldehyde (17.3 mg/m²) and (E)-cinnamaldehyde (25.8 mg/m²) were 2.5 and 1.7 times more toxic than benzyl benzoate (43.7 mg/m²), respectively, based on 24-h LD₅₀ values. The acaricidal activity was more pronounced in benzaldehyde, menthol, α-terpineol, and thymol (70.8–234.3 mg/m²) than in dibutyl phthalate (281.0 mg/m²). Against adult D. pteronyssinus, salicylaldehyde (17.3 mg/m²) and (E)-cinnamaldehyde (19.3 mg/m²) were 2.4- and 2.2-fold more active than benzyl benzoate (41.9 mg/m²). The toxicity of benzaldehyde, menthol, α-terpineol, and thymol (75.3–179.2 mg/m²) was higher than that of dibutyl phthalate (285.1 mg/m²). In vapour-phase toxicity tests with adult D. farinae, the test compounds described were much more effective in closed—but not in open—containers, indicating that the effect of these compounds was largely a result of action in the vapour phase.     

纳米级南瓜肌醇提取物的制备及其降血糖作用研究

本文通过制备纳米级南瓜肌醇提取物(Nanoscale pumpkin inositol extract,NPIE),观察其对链脲佐菌素诱导的糖尿病模型C57小鼠的血糖调节作用,并与普通南瓜肌醇提取物(Common pumpkin inositol extract,CPIE)的降血糖作用比较。高、低剂量CPIE组和NPIE组分别灌胃500 mg/kg、250 mg/kg的CPIE和NPIE水溶液,阳性药组灌服250 mg/kg的盐酸二甲双胍水溶液,模型对照组灌服等体积的双蒸水,实验周期均为30 d。结果显示所制备的南瓜肌醇提取物含肌醇3.12%,多糖53.21%,其中NPIE粒度平均小于500 nm;经动物实验,各给药组对正常小鼠无明显急性降糖作用,对糖尿病小鼠体重也无影响;但NPIE高剂量组对糖尿病小鼠的随机血糖和空腹血糖均具有明显降低效果,并对其糖耐量有一定改善作用,整体降糖效果较阳性药物组略弱,较CPIE强。     

Study of antimicrobial activity and root symbionts of Hemionitis arifolia

Antibacterial and antifungal activity of crude extract, alcoholic extract and extracted phenol from various parts of tropical pteridophyta, Hemionitis arifolia were tested by agar diffusion and tube dilution assay. Both the crude and alcoholic extracts of vegetative and reproductive leaves of H. arifolia showed considerable antibacterial activity against Gram negative test strain of Escherichia coli (MTCC-739). Extract from reproductive leaves also showed moderate antibacterial activity against Bacillus subtilis (MTCC-441) (Gram positive test strain) but didn’t show any antifungal activity against Candida albicans (MTCC-7353). Mycorrhizal and other symbiotic association with the root system of H. arifolia was studied and it is revealed that a number of mycorrhizal strains were present in both vegetative and reproductive form. Presence of Dark Septate Endophytic Fungi (DSF) was also detected.