Clinical efficacy of the partial rectus muscle transportation procedure for paralytic strabismus.

AIM: To analyze the clinical efficacy of the partial rectus muscle transportation (PRT) procedure for paralytic strabismus due to single rectus muscle palsy. METHODS: In total, 28 patients (31 eyes) who underwent the PRT procedure for paralytic strabismus due to single rectus muscle palsy were retrospectively examined. The following data were collected pre- and postoperatively: angle of deviation in the primary position, presence of diplopia in the primary position, presence of compensatory head posture, and motility of the affected eye. The follow-up period was 6mo. RESULTS: Based on the preoperative and intraoperative findings, different operations were performed: 2 eyes were treated with PRT, 26 eyes were treated with PRT combined with the recession of the antagonist muscle (Am) of the paralytic rectus muscle, and 3 eyes were treated with PRT along with the recession of the Am and the yoke muscle (Ym). On the first day after the operation, 24 patients were found to be orthophoric in the primary position, without diplopia or abnormal head posture. Moreover, 2 patients with monocular lateral rectus muscle palsy had mild overcorrection to 5 prism diopters (PD) and 8 PD, respectively, whereas 2 patients with binocular lateral rectus muscle palsy had mild undercorrection to 8 PD and 10 PD, respectively. During the 6-month follow-up period, the mean deviation was rectified from 96.79±41.21 PD to 0.64±2.38 PD (t=12.48, P<0.001), whereas the deviations in the 2 patients with mild overcorrection were corrected to orthotropia. The mean preoperative limitation of motility improved from -4.55±0.51 to -2.65±0.61 (t=-15.13, P<0.001) after 6mo postoperatively. CONCLUSION: PRT is an effective treatment for complete paralytic strabismus due to single rectus muscle palsy, and can achieve stable clinical efficacy.

(R)-2-Phenyl-4,5-Dihydrothiazole-4-Carboxamide Derivatives Containing a Diacylhydrazine Group: Synthesis, Biological Evaluation, and SARs.

A series of (R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a diacylhydrazine moiety were designed and synthesized. Their structures were confirmed by melting points, 1H NMR, 13C NMR, and elemental analysis (EA). Their antifungal and insecticidal activities were evaluated. The antifungal activity result indicated that most title compounds against Cercospora arachidicola, Alternaria solani, Phytophthora capsici, and Physalospora piricola exhibited apparent antifungal activities at 50 mg/L, and better than chlorothalonil or carbendazim. The EC50 values of (R)-N'-benzoyl-2-(4-chlorophenyl)-4,5-dihydrothiazole-4-carbohydrazide (I-5) against six tested phytopathogenic fungi were comparable to those of chlorothalonil. The CoMSIA model showed that a proper hydrophilic group in the R1 position, as well as a proper hydrophilic and electron-donating group in the R2 position, could improve the antifungal activity against Physalospora piricola, which contributed to the further optimization of the structures. Meanwhile, most title compounds displayed good insecticidal activities, especially compound (R)-N'-(4-nitrobenzoyl)-2-(4-nitrophenyl)-4,5-dihydrothiazole-4-carbohydrazide (III-3). The insecticidal mechanism results indicated that compound III-3 can serve as effective insect Ca2+ level modulators by disrupting the cellular calcium homeostasis in Mythimna separata.

Synthesis, insecticidal evaluation and mode of action of novel anthranilic diamide derivatives containing sulfur moiety as potential ryanodine receptor activators.

Anthranilic diamide insecticide could control lepidopteran pests by selectively binding and activating insect ryanodine receptors (RyRs), and the unique mode of action is different from other conventional insecticides. In order to discover new anthranilic diamide insecticide as ryanodine receptors activators, a series of 11 novel anthranilic diamides derivatives (Ia-k) were synthesized and confirmed by melting point, 1H NMR, 13C NMR and elemental analyses. The preliminary bioactivity revealed that most title compounds showed moderate to remarkable activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella). Especially, compounds Ia and If, which exhibited 100% larvicidal activity against oriental armyworm at 1.0 mg L-1, and comparable to that of chlorantraniliprole (100% at 1 mg L-1). If displayed 60% insecticidal activity against diamondback moth at 0.01 mg L-1, better than chlorantraniliprole (45% at 0.01 mg L-1). The preliminary structure activity relationships were discussed. In addition, the calcium imaging experiment indicated that the insect ryanodine receptor is the potential target of If.

Synthesis, insecticidal evaluation and 3D-QSAR study of novel anthranilic diamide derivatives as potential ryanodine receptor modulators.

BACKGROUND: Anthranilic diamide insecticides control lepidopteran pests through selectively binding and activating insect ryanodine receptors. In order to search for potential insecticides targeting the ryanodine receptors, a series of anthranilic diamide analogs including trifluoromethyl, nitro, or chloro groups were designed and synthesized by the principle of bioisosterism and structural optimization. RESULTS: Insecticidal data indicated that some compounds displayed good activity against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella). In particular, the larvicidal activity of 6p against P. xylostella was 95% at 0.01 mg L-1 , equivalent to chlorantraniliprole (85%, 0.01 mg L-1 ). The comparative molecular similarity index analysis model obtained indicated that hydrogen bond acceptor and electron-withdrawing groups in the R'3 group are favourable for insecticidal activity against M. separata, which is consistent with the structure-activity relationships. Moreover, the calcium imaging experiment indicated, like chlorantraniliprole, that 6h and 6p are interacting with the ryanodine receptor. CONCLUSION: Introducing trifluoromethyl, nitro, or chloro groups to a specific position in the N-phenylpyrazole could improve or maintain the activity against M. separata and P. xylostella. 6h and 6p could be used as potential lead compounds for ryanodine receptor modulators. © 2018 Society of Chemical Industry.

Strain-Tunable Electronic Properties and Band Alignments in GaTe/C2N Heterostructure: a First-Principles Calculation.

Recently, GaTe and C2N monolayers have been successfully synthesized and show fascinating electronic and optical properties. Such hybrid of GaTe with C2N may induce new novel physical properties. In this work, we perform ab initio simulations on the structural, electronic, and optical properties of the GaTe/C2N van der Waals (vdW) heterostructure. Our calculations show that the GaTe/C2N vdW heterostructure is an indirect-gap semiconductor with type-II band alignment, facilitating an effective separation of photogenerated carriers. Intriguingly, it also presents enhanced visible-UV light absorption compared to its components and can be tailored to be a good photocatalyst for water splitting at certain pH by applying vertical strains. Further, we explore specifically the adsorption and decomposition of water molecules on the surface of C2N layer in the heterostructure and the subsequent formation of hydrogen, which reveals the mechanism of photocatalytic hydrogen production on the 2D GaTe/C2N heterostructure. Moreover, it is found that in-plane biaxial strains can induce indirect-direct-indirect, semiconductor-metal, and type II to type I or type III transitions. These interesting results make the GaTe/C2N vdW heterostructure a promising candidate for applications in next generation of multifunctional optoelectronic devices.

Anthranilic diamides derivatives as potential ryanodine receptor modulators: Synthesis, biological evaluation and structure activity relationship.

A series of novel anthranilic diamides derivatives (7a-s) containing halogen, trifluoromethyl group and cyano group were designed, synthesized, and characterized by melting point, 1H NMR, 13C NMR and elemental analyses. The bioactivity revealed that most of them showed moderate to excellent activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella). Above all, the larvicidal activity of 7o against oriental armyworm was 100% and 40% at 0.25 and 0.1 mg L-1, comparable to that of the standard chlorantraniliprole (100%, 0.25 mg L-1 and 20%, 0.1 mg L-1). What is more, 7o against diamondback moth displayed 90% insecticidal activity at 0.01 mg L-1, superior to chlorantraniliprole (45%, 0.01 mg L-1). The experiments 7o on the American cockroach (Periplaneta Americana) heart beating rates (Dorsal vessel) and contractile force were compared with chlorantraniliprole. In addition, 7o could affect the calcium homeostasis in the central neurons of the third larvae of oriental armyworm, which revealed that the ryanodine receptor is the potential target of 7o. The density functional theory (DFT) calculation results revealed the amide bridge, the benzene ring of anthraniloyl moiety and pyrazole ring might play an important role in the insecticidal activity through hydrophobic interactions and π-π conjugations.

Microbial transformation of bufotalin by Alternaria alternata AS 3.4578.

The microbial transformation of a cytotoxic bufadienolide, bufotalin (1), was carried out. Three transformed products from 1 by Alternaria alternata were isolated. Their structures were characterized as 3-keto-bufotalin (2), 12 beta-hydroxyl-bufotalin (3), and 3-keto-12 beta-hydroxyl-bufotalin (4) based on the extensive NMR studies. Among them, 3 and 4 were new compounds with strong in vitro cytotoxic activities against HeLa cells.

Structural determination of flavonoids from Sophora flavescens.

Eight flavonoids were isolated from Sophora flavescens. Among them, three prenylflavanones: (2S)-6[2(3-hydroxyisopropyl)-5-methyl-4-hexenyl]-5-methoxy-7,2', 4'-trihydroxyflavanone (1), (2S)-5, 4'-dimethoxy-8-lavandulyl-7, 2'-dihydroxy flavanone (2) and (2S)-8-(5-hydroxy-2-isopropenyl-5-methylhexyl)-7-methoxy-5,2', 4'-trihydroxyflavanone (3) are new compounds. Their chemical structures were determined by spectral methods including 2D NMR.

[Multiple factor analysis of visual function in hypermetropic children].

OBJECTIVE: To investigate the characteristics of hypermetropic children whose visual acuity (VA) is declined or accompanied by esotropia. METHODS: One hundred and ninety children were given optometry, strabismus degree and binocular vision measurement. RESULTS: Declined VA appeared in 170 children, while esotropia occurred in 173. Sixty-one got binocular single vision, 17 had fusion function, and 11 had stereoaculty. Spherical equivalent had a linear relationship with VA (P < 0.01), but not with the strabismus degree (P > 0.05). The influence factors of binocular vision were age of discovery, VA and the strabismus degree, while the stereoaculty was influenced by the strabismus degree, spherical equivalent and VA. CONCLUSION: Low VA and strabismus are the most common complaint in children. Ametropia and strabismus do great harm to juvenile binocular vision, and stereoaculty is damaged seriously. We suggest an early examination of visual function in children.