奥沙利铂周围神经毒性模型大鼠行为学检测方法的比较

目的进行两种大鼠机械性痛觉敏感性测量方法、两种冷刺激缩足反应测量方法的比较研究。方法雌性Wistar大鼠,腹腔注射奥沙利铂4 mg/kg,建立标准奥沙利铂周围神经毒性大鼠模型。检测机械和冷热温度刺激下大鼠行为学变化,并对不同行为学检测方法的特点进行比较分析。结果模型组大鼠较正常组相比50%缩足阈明显降低(P0.05)、出现痛觉过敏及痛觉超敏(P0.05)、冷刺激诱发的缩足次数增多(P0.05),两组大鼠对热痛刺激反应均无明显差异,与临床患者症状表现基本一致。结论 Von Frey纤维丝刺激检测中4 g和15 g方法可更好的模拟临床患者的痛觉过敏、超敏反应;up-down法客观量化的反应出大鼠缩足阈值下降的程度。冷温度刺激中,丙酮喷洒法可较直观的观察大鼠受到冷刺激后的反应。     

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071

Herein we report the discovery and SAR of a novel series of M(1) agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M(1) agonist with high selectivity, clean ancillary pharmacology and enantiospecific activity.     

Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.     

江西吉安乌鸫的繁殖生态研究

2009～2010年对江西省吉安地区乌鸫Turdus merula的繁殖进行了调查研究,结果表明:当地乌鸫的营巢时间在3月9日至16日,产卵时间是3月18日至26日,平均窝卵数5.14(4～6)枚(n=14),平均卵大小29.71 mm×21.16 mm,平均卵重6.63 g(n=71).孵卵和暖巢主要由雌鸟承担,但雄鸟也有暖巢行为,孵化率为65.83%,育雏期13～15 d,离巢率高达100%.与高海拔的乌鸫相比,当地乌鸫产大窝小卵,这一特征保证了大窝雏数和高离巢率,繁殖对策属于r-选择.     

黑曲霉原生质体诱变选育果胶酶高产菌株

通过UV和NTG诱变筛选获得了2株高产果胶酶突变株。以果胶酶产生菌黑曲霉EIM6为诱变材料,采用1．5％的溶壁酶和1．5％的纤维素酶处理其对教生长期菌丝体2h获得高质量的原生质体。采用UV25S或50μg／mL NTG诱变30min,构建原生质体突变库,经刚果红果胶平板筛选获得果胶酶突变株,通过液体深层培养复筛获得高产突变株EIM6-U11、EIM6-N5,酶活力分别从46598．08、46598．08U／mL提高至68596．57、68879．56U／mL,分别提高了47．21％、47．82％。连续8次传代经发酵测酶活力表明高产突变株EIM6-U11、EIM6-N5具有较高的遗传稳定性。     

汉防己甲素联合顺铂对乳腺癌细胞的作用

目的:汉防己甲素和顺铂联合作用乳腺癌细胞,来提高癌细胞对顺铂的敏感性.方法:运用原子力显微镜对乳腺癌细胞表面的超微结构进行表征;MTr法和流式细胞术检测细胞的生长抑制率和细胞周期变化.结果:顺铂和汉防己甲素分别作用乳腺癌细胞48h IC50值为26.33μmoL/l和5.6μmok/l;联合用药组的IC50值为汉防己甲素2.5μmol/L和顺铂13.32μmol/l,在低浓度的联合用药作用乳腺癌细胞24h细胞膜表面结构被破坏,产生孔洞,作用48h被严重破坏使细胞周期在S比例增加为51.7%±0.30%.结论:提高了癌细胞对抗癌药物的敏感性,联合用药通过改变了细胞膜的结构对癌细胞进行有效杀伤,抑制肿瘤细胞生长.     

以肠道外症状为首发表现的结肠癌47例临床分析

目的:分析以肠道外症状为首发表现的结肠癌临床特征,旨在提高结肠癌诊治水平。方法:收集我院1994年1月至2008年1月间以肠道外症状为首发表现的结肠癌47例,对其临床特点进行回顾性分析。结果:47例以肠道外症状为首发表现的结肠癌中位发病年龄为65岁;贫血症状多见,占78.7%(37/47),长期低热3例,肝转移瘤4例,肺转移瘤2例,皮肌炎1例;肿瘤多发生于右半结肠,占74.5%(35/47);病理类型:乳头状腺癌为主,占61.7%(29/47);Dukes分期:B期占44.7%(21/47),C期占42.6%(20/47);结肠镜是重要诊断方法,结肠镜与钡灌肠有互补优势;手术是主要治疗手段,综合治疗可延长患者生存期。结论:以肠道外症状为首发表现的结肠癌以贫血多见,病变多位于右半结肠,结肠镜是主要确诊方法,以手术为主的综合治疗可改善患者预后。     

以肠道外症状为首发表现的结肠癌47例临床分析

目的:分析以肠道外症状为首发表现的结肠癌临床特征,旨在提高结肠癌诊治水平.方法:收集我院1994年1月至2008年1月间以肠道外症状为首发表现的结肠癌47例,对其临床特点进行回顾性分析.结果:47例以肠道外症状为首发表现的结肠癌中位发病年龄为65岁;贫血症状多见,占78.7％(37/47),长期低热3例,肝转移瘤4例,肺转移瘤2例,皮肌炎1例;肿瘤多发生于右半结肠,占74.5％(35/47);病理类型:乳头状腺癌为主,占61.7％(29/47);Dukes分期:B期占44.7％(21/47),C期占42.6％(20/47);结肠镜是重要诊断方法,结肠镜与钡灌肠有互补优势;手术是主要治疗手段,综合治疗可延长患者生存期.结论:以肠道外症状为首发表现的结肠癌以贫血多见,病变多位于右半结肠,结肠镜是主要确诊方法,以手术为主的综合治疗可改善患者预后.     

The composition and timing of flower odour emission by wild <Emphasis Type="Italic">Petunia axillaris</Emphasis> coincide with the antennal perception and nocturnal activity of the pollinator <Emphasis Type="Italic">Manduca sexta</Emphasis>

In the genus Petunia, distinct pollination syndromes may have evolved in association with bee-visitation (P. integrifolia spp.) or hawk moth-visitation (P. axillaris spp). We investigated the extent of congruence between floral fragrance and olfactory perception of the hawk moth Manduca sexta. Hawk moth pollinated P. axillaris releases high levels of several compounds compared to the bee-pollinated P. integrifolia that releases benzaldehyde almost exclusively. The three dominating compounds in P. axillaris were benzaldehyde, benzyl alcohol and methyl benzoate. In P. axillaris, benzenoids showed a circadian rhythm with an emission peak at night, which was absent from P. integrifolia. These characters were highly conserved among different P. axillaris subspecies and P. axillaris accessions, with some differences in fragrance composition. Electroantennogram (EAG) recordings using flower-blends of different wild Petunia species on female M. sexta antennae showed that P. axillaris odours elicited stronger responses than P. integrifolia odours. EAG responses were highest to the three dominating compounds in the P. axillaris flower odours. Further, EAG responses to odour-samples collected from P. axillaris flowers confirmed that odours collected at night evoked stronger responses from M. sexta than odours collected during the day. These results show that timing of odour emissions by P. axillaris is in tune with nocturnal hawk moth activity and that flower-volatile composition is adapted to the antennal perception of these pollinators.