Synthesis and antitumor activity of novel 2',3'-dideoxy-2',3'-diethanethionucleosides bearing 1,2,3-triazole residues.

A series of novel 2',3'-dideoxy-2',3'-diethanethioribonucleosides and those modified with a triazole ring were prepared in excellent yields and their antitumor activity was evaluated. Nucleosides with a triazole ring, 16a-16c, showed significantly improved activity towards a broad range of tumor cell lines.

4,5,6-Tri-O-acetyl-2,3-di-S-ethyl-2,3-dithio-d-allose diethyl dithio-acetal.

The title compound, C(20)H(36)O(6)S(4), was obtained by ethanethiol-ysis of 3,5,6-tri-O-acetyl-1,2-O-isopropyl-idene-α-d-gluco-furan--ose. One of the ethyl groups is disordered over two sites with refined occupancies of 0.869 (6) and 0.131 (6). Compared with the precursor, the absolute configuration of the stereocenters at positions C-3 and C-2 are inverted and maintained, respectively.

Synthesis and antitumor activity of novel 2',3'-diethanethio-2',3',5'-trideoxy-5'-triazolonucleoside analogues.

A series of novel 2',3'-diethanethio-2',3',5'-trideoxy-5'-triazoloribonucleosides was synthesized in excellent yields and their antitumor activity was evaluated. These nucleoside analogues with aromatic substituted triazole rings showed significantly improved activity towards a broad range of tumor cell lines and those without arene substitutes were inactive.

Clinical significance of peripheral blood neutrophil CD64 in Kawasaki disease / 中华实用儿科临床杂志

Objective To investigate the expression level of peripheral blood neutrophil CD64 in Kawasaki disease (KD),and explore its clinical significance.Methods Fifty-four patients with KD were divided into 2 groups [13 patients with coronary artery lesions(CAL) and 41 patients without CAL],and 30 age-matched patients with sepsis and 10 healthy children were studied.The levels of peripheral blood neutrophil CD64 was measured by flow cytometry.Results Before treatment,the levels of C D64 in children with KD(7.02 ± 3.21)and sepsis (11.25 ± 5.14) were significantly higher than the healthy children (2.45 ± 0.52),and the level of CD64 in the KD group was significantly lower than that in sepsis group(P ＜ 0.01).CD64 index were significantly elevated in the 2 groups of KD patients before treatment (CAL group:5.74 ± 3.09 ; without CAL:7.43-± 3.17).There was no significant difference in the CD64 level between KD patients with CAL and without CAL.CD64 index in the 2 groups of KD patients after treatment (CAL group:2.56 ± 0.73 ; without CAL:2.63-± 0.69) were significantly lower than those before treatment (all P ＜ 0.01).Conclusions The expression of peripheral blood neutrophil CD64 in KD is significantly elevated.The degree of elevation in CD64 possibly has clinical meaning in differentiating KD from sepsis,and it can be a sensitive factor of disease outcome.

Methylation and expression of RUNX3 gene promoter in papillary thyroid carcinoma / 中华耳鼻咽喉头颈外科杂志

<p><b>OBJECTIVE</b>To study the relationship between status of methylation of human runt-related transcription factor 3 (RUNX3) gene promoter in papillary thyroid carcinoma (PTC).</p><p><b>METHODS</b>Methylation-specific PCR and immunohistochemical SP technique were used to detect the methylation of RUNX3 gene promoter and expression of its protein in 56 cases of PTC and their matched adjacent non-carcinous epithelium (NCE).</p><p><b>RESULTS</b>In NCE, there was no methylation of RUNX3 gene promoter, while in PTC the methylation rate was 35.7%(20/56), which was related to the tumor TNM stage, pathological grade and lymph node metastasis (P < 0.05). The positive rates of RUNX3 protein expression in NCE and PTC were 100.0% and 60.7%, respectively, with a significant difference (χ(2) = 27.378, P < 0.05). In PTC, the positive rates of RUNX3 protein expression in gradeI and grade II were 70.0% and 37.5%, respectively (P < 0.05); the rates were 46.7% and 76.9% in lymph node metastasis group and no metastasis group, respectively (P < 0.05). Moreover, there was a distinct correlation between methylation of RUNX3 gene promoter and expression of its protein (χ(2) = 21.62, P < 0.01).</p><p><b>CONCLUSIONS</b>Methylation of promoter might be one of the important factors of inactivation of RUNX3 gene, and might play an important role in carcinogenesis and progression of PTC.</p>

Expression of Piwil2 and its relationship with tumor invasion and metastasis in papillary thyroid carcinoma / 中华耳鼻咽喉头颈外科杂志

<p><b>OBJECTIVE</b>To study the expressions of Piwil2 protein and mRNA in papillary thyroid carcinoma (PTC) and the relationship between Piwil2 and the invasion and metastasis of PTC.</p><p><b>METHODS</b>Immunohistochemistry and in situ hybridization were used to detect the expression of Piwil2 protein and mRNA in 60 cases of PTC with the matched adjacent non-cancerous epithelium (NCE).</p><p><b>RESULTS</b>The positive rates of Piwil2 protein expression in PTC and NCE were 88.3% (53/60) and 10.0% (6/60) respectively, with significant difference (χ² = 73.654, P < 0.01). The positive rates of Piwil2 mRNA expression in PTC and NCE were 85.0% (51/60) and 6.7% (4/60) respectively, also with significant difference (χ(2) = 74.148, P < 0.01). Up-regulated expressions of Piwil2 protein and mRNA were related to the invasion and metastasis of PTC (P < 0.05).</p><p><b>CONCLUSIONS</b>Piwil2 may play a role in the invasion and metastasis of PTC.</p>