Syntheses, Characterization, Crystal Structures and Xanthine Oxidase Inhibitory Activity of Hydrazones.

Four new fluoro-containing hydrazones were synthesized from 4-fluorobenzaldehyde with chloro- and nitro-substituted benzohydrazides. They are 3-chloro-N'-(4-fluorobenzylidene)benzohydrazide (1), 2-chloro-N'-(4-fluorobenzylidene)benzohydrazide (2), N'-(4-fluorobenzylidene)-4-nitrobenzohydrazide (3), and N'-(4-fluorobenzylidene)-3-nitrobenzohydrazide (4). The compounds have been characterized by IR and 1H NMR spectra, as well as X-ray single crystal determination. Xanthine oxidase (XO) inhibitory activity indicated that the nitro substituted compounds 3 and 4 have effective activity. Docking simulation was performed to insert the compounds into the crystal structure of xanthine oxidase at the active site to investigate the probable binding modes.

[Properties of new exotic traditional Chinese medicinal Vernonia amygdalina leaves:a literature research].

The leaves of Vernonia amygdalina Delile of the family Asteraceae(also known as "bitter leaf"), rich in biological activities, are used as both medicine and food for a long time in West tropical Africa. They have been introduced into Southeast Asia and Fujian and Guangdong provinces of China in recent years. However, little is known about the properties of the plant in traditional Chinese medicine(TCM), which limits its combination with other Chinese medicinal herbs. In this study, 473 articles on V. amygdalina leaves were selected from PubMed, Web of Science, CNKI, Wanfang Data and VIP to summarize their components, pharmacological effects and clinical research. V. amygdalina leaves presented anti-microbial, hypoglycemic, anti-hypertensive, lipid-lowering, anti-tumor, anti-inflammatory, antioxidant, and other pharmacological effects. On the basis of the theory of TCM properties, the leaves were inferred to be cold in property and bitter and sweet in flavor, acting on spleen, liver, stomach and large intestine and with the functions of clearing heat, drying dampness, purging fire, removing toxin, killing insects and preventing attack of malaria. They can be used to treat dampness-heat diarrhea, interior heat and diabetes, malaria, insect accumulation and eczema(5-10 g dry leaves by decoction per day and an appropriate amount of crushed fresh leaves applying to the affected area for external use). Due to the lack of TCM properties, V. amygdalina leaves are rarely used medicinally in China. The determination of medicinal properties of the leaves is conducive to the introduction of new exotic medicinal herbs and the development of new TCM resources, which facilitated further clinical application and research and development of Chinese medicinal herbs.

[Moxibustion at Baihui combined with acupuncture for cervical vertigo: a Meta-analysis and trial sequential analysis].

OBJECTIVE: To evaluate the efficacy and safety of moxibustion at Baihui (CV20) combined with acupuncture in treatment of cervical vertigo. METHODS: From the databases, such as CNKI, VIP, WanFang, CBM, PubMed, Cochrane Library and Embase, the studies of randomized controlled trials (RCTs) on moxibustion at CV20 combined with acupuncture for cervical vertigo were searched from inception to September 15th, 2021. The Cochrane risk of bias assessment tool was utilized to evaluate the quality of the included literature. Using RevMan5.3, Stata12.0 and TSA0.9.5.0 10 Beta software, the Meta-analysis and trial sequential analysis (TSA) were performed. RESULTS: Seventeen RCTs with 1 232 patients were included. Meta-analysis showed that in the trial group (moxibustion at CV20 combined with acupuncture), the total effective rate (RR=1.17, 95%CI［1.12, 1.22］, P<0.000 1), the curative and remarkably-effective rate (RR＝1.28，95%CI［1.20，1.36］，P<0.000 1) and the score of cervical vertigo (WMD=2.88, 95%CI［1.87, 3.89］, P<0.000 1) were all better when compared with the control group (simple acupuncture or electroacupuncture group). The results of trial sequential analysis indicated that for the cumulative Z-score of each RCT, the Z-curve crossed the conventional test boundary and TSA boundary, which further confirmed the clinical efficacy of moxibustion at CV20 combined with acupuncture on cervical vertigo. CONCLUSION: The clinical efficacy of moxibustion at CV20 combined with acupuncture is determined in treatment of cervical vertigo.

New model of PIRADS and adjusted prostatespecific antigen density of peripheral zone improves the detection rate of initial prostate biopsy: a diagnostic study.

This study explored a new model of Prostate Imaging Reporting and Data System (PIRADS) and adjusted prostate-specific antigen density of peripheral zone (aPSADPZ) for predicting the occurrence of prostate cancer (PCa) and clinically significant prostate cancer (csPCa). The demographic and clinical characteristics of 853 patients were recorded. Prostate-specific antigen (PSA), PSA density (PSAD), PSAD of peripheral zone (PSADPZ), aPSADPZ, and peripheral zone volume ratio (PZ-ratio) were calculated and subjected to receiver operating characteristic (ROC) curve analysis. The calibration and discrimination abilities of new nomograms were verified with the calibration curve and area under the ROC curve (AUC). The clinical benefits of these models were evaluated by decision curve analysis and clinical impact curves. The AUCs of PSA, PSAD, PSADPZ, aPSADPZ, and PZ-ratio were 0.669, 0.762, 0.659, 0.812, and 0.748 for PCa diagnosis, while 0.713, 0.788, 0.694, 0.828, and 0.735 for csPCa diagnosis, respectively. All nomograms displayed higher net benefit and better overall calibration than the scenarios for predicting the occurrence of PCa or csPCa. The new model significantly improved the diagnostic accuracy of PCa (0.945 vs 0.830, P < 0.01) and csPCa (0.937 vs 0.845, P < 0.01) compared with the base model. In addition, the number of patients with PCa and csPCa predicted by the new model was in good agreement with the actual number of patients with PCa and csPCa in high-risk threshold. This study demonstrates that aPSADPZ has a higher predictive accuracy for PCa diagnosis than the conventional indicators. Combining aPSADPZ with PIRADS can improve PCa diagnosis and avoid unnecessary biopsies.

Tetranuclear Copper(II) Complexes Derived from 5-Bromo-2-((2-(2-hydroxyethylamino)ethylimino)methyl)phenol: Synthesis, Characterization, Crystal Structures and Catalytic Oxidation of Olefins.

An acetate bridged tetranuclear copper(II) complex, [Cu4L2(µ2-η1:η1-CH3COO)6(CH3OH)2] (1), and a chloride, phenolate and azide co-bridged tetranuclear copper(II) complex, [Cu4L2Cl2(µ-Cl)2(µ1,1-N3)2]2CH3OH (2), where L is the deprotonated form of the Schiff base 5-bromo-2-((2-(2-hydroxyethylamino)ethylimino)methyl)phenol (HL), have been synthesized and characterized by elemental analysis, IR and UV spectra, and single crystal X-ray diffraction. Single crystal X-ray analysis revealed that the Cu atoms in both complexes are in square pyramidal geometry. In complex 1, two [CuL] units and [Cu2(µ2-η1:η1-CH3COO)4] core are linked through two acetate ligands. In complex 2, [Cu2LCl(µ-Cl)] units are linked together by two end-on azido ligands. The Schiff base ligand coordinates to the Cu atoms through four N and O donor atoms. The molecules of both complexes are linked through hydrogen bonds to generate three dimensional networks. The catalytic property of the complexes for epoxidation reactions of some alkenes was studied using tert-butylhydroperoxide as the terminal oxidant under mild conditions in acetonitrile.

Side-Group Effect on the Slow Relaxations of {Dy2} Single-Molecule Magnets with Confined N2O6 Donors.

Deep insights into and substantial enhancement of the effective anisotropy energy barrier for magnetization reversal (Ueff) are vitally important for the technological applications of dysprosium(III)-based single-molecule magnets (Dy-SMMs). To fully refine the ligand-field effect on spin relaxation, four centrosymmetric {Dy2} entities with formula [Dy2(CH3OH)2L2(RCOO)2] (H2L = 2-hydroxy-N'-((pyridin-2-yl)methylene)benzohydrazide) have been solvothermally prepared by varying the side groups of carboxylate coligands (RCOO-, R = CF3 for 1, H for 2, CH3 for 3, and Cp2Fe for 4). Structural analyses reveal that all of the DyIII carriers in 1-4 have the same N2O6 donor environments, and the non-coordinative R groups attached to the equatorial carboxylate bridges have not substantially changed the binding ability of the shortest Dy-Ophenolate bonds located at the axial position of the ligand field. Interestingly, the side groups have monotonically decreased the zero-field Ueff barriers of these weak antiferromagnetically coupled {Dy2} analogues from 721 K down to 379 K. Further electronic structure calculations demonstrate that the main magnetic axes of 1-4 are highly dominated by these comparable Dy-Ophenolate short bonds, and the g tensors have produced gradually increased transverse components responsible significantly for the decreased Ueff barriers. Additionally, thermally assisted relaxations occur preferably through the second (for 1) and the first (for 2-4) Kramer doublets. These interesting findings afford a new side-group effect to comprehensively understand the magnetostructural relationships and advance the rational design of high-performance Dy-SMMs.

[Effect of ZhuLian's type â ¡ inhibition needling technique on endocrine metabolism in rats with polycystic ovary syndrome and insulin resistance].

OBJECTIVE: To observe the effect of ZhuLian's type Ⅱ inhibition needling technique on sex hormones, insulin resistance and ovarian morphology in rats with polycystic ovary syndrome (PCOS), so as to explore its mechanism on regulating endocrine and metabolic dysfunction of PCOS. METHODS: Twenty-four female SD rats were randomly divided into control, model and ZhuLian acupuncture groups (n=8 in each group). The PCOS model was established by continuous gavage of letrozole combined with high-fat diet. Rats of the ZhuLian acupuncture group were stimulated at "Guanyuan"(CV4) and bilateral "Guilai"(ST29), "Zusanli"(ST36), "Sanyinjiao"(SP6), and "Fenglong"(ST40) by ZhuLian's type Ⅱ inhibition needling technique for 30 min, continuously intervented for 28 days. The body weight was measured before and after modeling and after intervention. The ovarian volume was calculated. HE staining was used to observe the changes of ovarian histology. Plasma levels of luteinizing hormone (LH), follicle stimulating hormone (FSH) and fasting insulin (FINS) were measured by ELISA. LH/FSH ratio and insulin resistance index (HOMA-IR) were calculated. RESULTS: After modeling, the rats' body weight and the ovarian volume were increased (P<0.05), and the ovaries showed polycystic changes in the model group compared with the control group. And the FINS level, HOMA-IR, LH content and LH/FSH ratio were significantly increased (P<0.05), while the FSH level was decreased (P<0.05). After the intervention, the rats' body weight and ovarian volume were decreased (P<0.05), and a small number of preantral follicles and more antral follicles were observed under microscope, and the levels of LH, LH/FSH, FINS and HOMA-IR were significantly decreased (P<0.05), while FSH content was increased (P<0.05) in the ZhuLian acupuncture group than in the model group. CONCLUSION: ZhuLian's type Ⅱ inhibition needling technique can improve the endocrine and metabolic disorders in PCOS rats, which may be related to the regulation of endocrine system.

The complete mitochondrial genome of Lixus subtilis Boheman, 1835 (Coleoptera, Curculionidae) and its phylogenetic implications.

The first complete mitochondrial genome of Lixus subtilis Boheman is reported in this study. The circular genome is 15,223 bp long, including a standard set of 21 transfer RNAs (tRNAs), 2 ribosomal RNAs (rRNAs), 13 protein-coding genes, and a non-coding control region. The trnI gene was not found in the L. subtilis mitogenome. All tRNAs had the typical cloverleaf structure, except for trnS1, which lacked the dihydrouridine arm. The phylogenetic tree of 13 Curculionidae species based on the concatenated nucleotide sequences of complete mitochondrial genomes strongly supported that L. subtilis is closely related to Curculioninae and Molytinae.

Slow relaxation of Dy(III) single-ion magnets dominated by the simultaneous binding of chelating ligands in low-symmetry ligand-fields.

Electronic effect and geometry distortion of low-symmetry ligand-field on the anisotropy barrier (Ueff) of spin reversal have been compared in three Dy(III) single-ion magnets through the simultaneous binding of chelating ligands. The substitution of N,O-salicylaldoxime by N,N'-1,10-phenanthroline in the distorted triangular-dodecahedronal field sharply decreases the Ueff by 286 K due to an increase in non-preferred transverse anisotropy, while the geometry distortion with CShM = 1.569 went down to 1.376 only lowering the Ueff by 12 K. The co-coordination strategy of heterodonor ligands highlights the importance of ligand-surroundings on the relaxation dynamics.

[Efficacy and action mechanism of ZHU Lian inhibition type â acupuncture for acne with spleen-stomach dampness-heat].

OBJECTIVE: To observe the efficacy of ZHU Lian inhibition type Ⅰ acupuncture for acne with spleen-stomach dampness-heat, and to explore its possible action mechanism. METHODS: A total of 82 patients of acne with spleen-stomach dampness-heat were randomly divided into an observation group and a control group, 41 cases in each group. The patients in the control group were treated with danshentong capsules (1 g, 3 times per day) and 0.1% adapalene gel smear (once every night) for 4 weeks. The patients in the observation group were treated with ZHU Lian inhibition type Ⅰ acupuncture at Hegu (LI 4), Neiting (ST 44), Quchi (LI 11), Yangbai (GB 14), Sibai (ST 2), Qihai (CV 6), Xuehai (SP 10), Yinlingquan (SP 9) and skin lesions, once every other day, 7 times as a course of treatment, totaling for 2 courses of treatment. The skin lesion score of the global acne grading system (GAGS) and quality of life-acne (Qol-Acne) score as well as the serum levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) were compared between the two groups before and after treatment; the clinical efficacy were compared between the two groups, and the recurrence rate was evaluated 4 weeks after treatment. RESULTS: After treatment, the skin lesion scores of GAGS in the two groups were reduced (P<0.05), and the score in the observation group was lower than that in the control group (P<0.05). After treatment, the Qol-Acne scores were increased in the two groups (P<0.05), and the score in the observation group was higher than that in the control group (P<0.05). The serum levels of TNF-αand IL-6 in the two groups were reduced after treatment (P<0.05), and those in the observation group were lower than the control group (P<0.05). The total effective rate was 95.1% (39/41) in the observation group, which was higher than 82.9% (34/41) in the control group (P<0.05). Four weeks after treatment, the recurrence rate of acne lesions was 10.3% (4/39) in the observation group, which was lower than 32.4% (11/34) in the control group (P<0.05). CONCLUSION: ZHU Lian inhibition type Ⅰ acupuncture is effective for acne with spleen-stomach dampness-heat, and the recurrence rate is low. Its mechanism may be related to the reduction of serum inflammatory factor TNF-α and IL-6.

[Effect of electroacupuncture combined with Zhuang-medicine-thread moxibustion on silent information regulator-1/nuclear factor κB signaling pathway in gastric antrum of diabetic gastroparesis rats].

OBJECTIVE: To observe the effect of electroacupuncture (EA) combined with Zhuang-medicine-thread moxibustion on silent information regulator-1 (SIRT1)/nuclear factor kappa B (NF-κB) signal pathway and inflammatory factor expression in gastric antrum tissue of diabetic gastroparesis (DGP) rats, so as to explore its mechanism underlying improvement of DGP. METHODS: Male SD rats were randomly divided into normal, model, medication, EA, Zhuang-medicine-thread moxibustion (moxibustion) and EA+moxibustion groups (n=12 per group). The DGP model was established by intraperitoneal injection of streptozotocin (STZ). Rats of the medication group were treated by gavage of 0.15 mg/mL mosapride citrate suspension. EA (10 Hz /50 Hz, 2 mA) or moxibustion (3 cones) or EA+moxibustion was applied to "Zhongwan"(CV12), bilateral "Neiguan"(PC6) and bilateral "Sanyinjiao"(SP6) of the related group for 20 min, once a day for 3 weeks. Blood glucose, gastric emptying rate and intestinal propulsion rate were measured. The levels of serum interleukin (IL)-6, IL-8, IL-10 and tumor necrosis factor-α(TNF-α) were detected by ELISA; the phosphorylation level of the phosphorylated inhibitor of nuclear factor κBα inhibitor (pIκ-Bα), the protein and mRNA expression of NF-κB p65 and SIRT1 in the gastric antrum tissue were detected by Western blot and real-time quantifitative PCR, respectively. RESULTS: (1) Compared with the normal group, the levels of blood glucose, serum IL-6, IL-8, TNF-α, and gastric pIκ-Bα and NF-κB p65 protein and mRNA expressions were significantly increased (P<0.01), and the gastric emptying rate, intestinal propulsion rate, serum IL-10 level, and SIRT1 protein and mRNA expressions were considerably decreased in the model group (P<0.01). (2) In contrast to the model group, the blood glucose in the EA, moxibustion and EA+moxibustion groups, serum IL-6, IL-8 and TNF-α levels in the 4 treatment groups, as well as NF-κB p65 protein expression in the medication and EA+moxibustion groups, and NF-κB p65 mRNA expression and pIκ-Bα protein and mRNA expression in the 4 treatment groups were significantly decreased (P<0.01, P<0.05); while the gastric emptying rate and intestinal propulsive rate and IL-10 content in the 4 treatment groups, and SIRT1 protein and mRNA expression in the medication and EA+moxibustion groups were obviously increased (P<0.05, P<0.01). (3) The effects of EA+moxibustion were significantly superior to those of simple EA and moxibustion in increasing gastric emptying rate, IL-10, SIRT1 protein expression (P<0.05, P<0.01), and in lowering IL-8 and TNF-α contents, pIκ-Bα protein and mRNA expression and NF-κB p65 mRNA expression (P<0.05, P<0.01). No significant differences were found among the 4 intervention groups in promoting the intestinal propulsive rate and among the EA, moxibustion and EA+moxibustion groups in lowering blood glucose (P>0.05). CONCLUSION: EA combined with Zhuang-medicine-thread moxibustion can effectively reduce the level of serum inflammatory factors and regulate SIRT1/NF-κB signal pathway in DGP rats, which may contribute to its function in improving gastrointestinal movement.

Enhancing the Magnetic Anisotropy in Low-Symmetry Dy-Based Complexes by Tuning the Bond Length.

One mononuclear complex [Dy(Htpy)(NO3)2(acac)] (1) and a tpy--extended 1D chain {[Dy(CH3OH)(NO3)2(tpy)]·CH3OH}n (2) (Htpy = 4'-(4-hydroxyphenyl)-2,2':6',2''-terpyridine, Hacac = acetylacetone) were successfully designed to investigate the effect of bond length tuning around the DyIII cation on the magnetic dynamics of single-molecule magnets (SMMs). Interestingly, two magnetic entities possess the same local coordination sphere (N3O6-donor) as well as the configuration (Muffin, Cs) of dysprosium centers. Only a slight difference in structure results from purposefully substituting the acetylacetone ligand in 1 with hydroxyl oxygen from tpy- linkage and one methanol molecule in 2. However, the remarkable differences in dynamics behavior were clearly found between them. Compound 1 possesses a thermal-activated effective energy barrier (Ueff/kB) of 22.7 K under a 0 kOe direct current (dc) field and negligible hysteresis loop at 2.0 K, while complex 2 shows high-performance SMM behavior with the largest energy barrier of 354.36 K among the reported nine-coordinated DyIII-based systems and the magnetic hysteresis up to 4.0 K at a sweep rate of 200 Oe s-1. These experimental results combined with the previous reported data reveal that the shortest bond and the bond length difference around the DyIII center synergistically determine the dynamics of SMMs. The uniaxial anisotropy increases with the decrease of the shortest bond and the increase of the bond length difference, which is confirmed by the theoretical calculations.

Photo-oligomerization by shifting the coordination site in a luminescent coordination polymer.

A layered coordination polymer (CP) with the fine-tuned alignment of four diolefinic ligands has been designed by shifting the coordination site of the ligand. The trimeric and tetrameric cyclobutane derivatives were reversely achieved by the photoinitiated [2+2] cycloaddition of the CP due to the favorable Schmidt's distance. More interestingly, a dynamic fluorescence shift was observed during the photo-oligomerization and heat-cycloreversion of the CP system.

Photocatalytic hydrogen evolution activity over Pt-assisted metal-organic frameworks dominated by transition metal ions and local coordination environments.

Three isostructural pillared-layer frameworks with M-BDC-X layers supported by ditopic HL connectors, [M(HL)(BDC)0.5X] n (HL = 4'-(4-hydroxyphenyl)-4,2':6',4″-terpyridine, BDC = terephthalate, M = Cd, X = Cl for (1), M = Cd, X = formate for (2), and M = Co, X = formate for (3)), were solvothermally synthesized, and used as photocatalysts for Pt-assisted visible-light-initiated hydrogen evolution from water splitting. These water-durable frameworks exhibit varied hydrogen production rates of 361.2, 271.3, and 327.5 µmol · g-1 · h-1 in 12 h due to their slightly different donor environments of the octahedral CdII and CoII ions. Further experimental and theoretical investigations reveal that the metal ions and the local coordination surroundings have essentially dominated the conduction band minimum and electric resistance of the charge transport, which play highly important roles for the improved catalytic hydrogen evolution ability. These findings demonstrate the electronic effect of the slightly ligand field modifications on the boosting hydrogen generation activity in the noble metal-assisted MOF photocatalytic systems.

Encapsulated anion-dominated photocatalytic and adsorption performances for organic dye degradation and oxoanion pollutant capture over cationic Cu(i)-organic framework semiconductors.

Decontamination of industrial wastewater containing toxic organic dye molecules and oxoanions is urgently desirable for environmental sustainability and human health. Water-stable porous metal-organic frameworks (MOFs) have emerged as highly efficient photocatalysts and/or adsorbents for water purification through controllable integration of the constitutive requirements. To reveal the inclusion anion effect of microporous MOFs on wastewater treatment, two isostructural MOFs incorporating positive charge and semiconductive characteristics, {[Cu(tpt)]·3H2O·0.5SO4}n (1) and {[Cu(tpt)]·2H2O·ClO4}n (2, tpt = 2,4,6-tris(4-pyridyl)-1,3,5-triazine), have been synthesized and employed as dual-functional materials for both dye photodegradation and oxoanion removal. The two MOFs possess the same 3-fold interpenetrating cationic backbones but are encapsulated by highly disordered sulfate or perchlorate in the open channels. These included anions have significantly tuned the hydrophilicity of the channels, extended the visible-light absorption, optimized the bandgap and decreased the conduction band potential. Under the low-energy irradiation of a 30 W LED lamp, MOF 1 has selectively and efficiently degraded rhodamine B compared to 2 with accelerated kinetics, resulting from the stronger reduction ability and less migration resistance of the photogenerated electrons. Instead, MOF 2 can quickly capture harmful MnO4- and Cr2O72- by exchanging with the entrapped ClO4-, with maximum adsorption amounts of 557 and 168 mg g-1, respectively, under ambient conditions. The improved decolorization of the aqueous solution over 2 benefits essentially from the shape and charge memory effect and the smaller hydration energy of ClO4- than SO42-. These interesting observations highlight the importance of the included anions inside the porous MOF semiconductors on wastewater treatment.

Substituent group-tunable hydrogen evolution activity observed in isostructural Cu(ii)-based coordination polymer photocatalysts.

Elucidations on the structure-activity correlations of non-Pt coordination polymer (CP)-based photocatalysts are highly significant for both the enhancement in catalytic activity and large-scale industrial applications of sustainable hydrogen from water splitting. Herein, three isostructural [Cu(HL)2(R-BDC)]n (denoted as Cu-CP-R, HL = 4'-(4-hydroxyphenyl)-4,2':6',4''-terpyridine, R-BDC = 2-R-1,4-benzenedicarboxylate, R = NO2, OH and Br) CPs were solvothermally synthesized by varying the substituents attached to benzenedicarboxylate, which together with two previously reported analogues (R = NH2 and H) were used as photocatalysts to systematically explore the substitution effect on the hydrogen evolution activity. These five CPs feature isomorphic layered motifs with axially elongated CuII octahedra extended alternately by ditopic HL and R-BDC2- connectors, in which R behaves structurally as a non-coordinate group. The hydrogen production rate over the Cu-CP-R photocatalysts increased from 0.21 to 2.34 mmol g-1 h-1, which followed the order of -NH2 > -NO2 > -H > -OH > -Br. Furthermore, the combined experimental and theoretical investigations reveal that the free R moiety significantly dominates the photocatalytic activity by shifting the d states of the CuII ion towards the Fermi level, controlling the potential of the conduction band and quickening the charge transfer ability. These important findings can provide informative hints for the design of high-performance, earth-abundant non-noble metal CP-based semi-conductive photocatalysts.

Anti-Osteoporotic Activity of an Edible Traditional Chinese Medicine Cistanche deserticola on Bone Metabolism of Ovariectomized Rats Through RANKL/RANK/TRAF6-Mediated Signaling Pathways.

Given the limitations of existing therapeutic agents for treatment of postmenopausal osteoporosis, there still remains a need for more options with both efficacy and less adverse effects. Cistanche deserticola Y. C. Ma is known as a popular tonic herb traditionally used to treatment deficiency of kidney energy including muscle weakness in minority area of Asian counties. Based on the theory of "kidney dominate bone," an ovariectomized (OVX) rat model of postmenopausal osteoporosis was used to evaluate the therapeutic effect of C. deserticola extract (CDE) on bone loss. Forty eight female Sprague-Dawley rats, aged about 12 weeks, were randomly assigned into six groups including sham group orally administrated with 0.5% carboxymethyl cellulose sodium (CMC-Na) (sham), positive group treated with 1 mg/kg of estradiol valerate (EV), low, moderate, and high dosage groups orally administrated with 200, 400, and 800 mg/kg/day of CDE, respectively. After 3 months of continuous intervention, CDE exhibited significant anti-osteoporotic activity evidenced by the enhanced total bone mineral density, ameliorated bone microarchitecture; increased alkaline phosphatase activity; decreased deoxypyridinoline, cathepsin K, tartrate-resistant acid phosphatase, and malondialdehyde levels; whereas the body, uterus, and vagina weights in OVX rats were not influenced by CDE intervention. In addition, a seemed contradictory phenomenon on levels of calcium and phosphorus between OVX and sham rats were observed and elucidated. Mechanistically, CDE significantly down-regulated the levels of TRAF6, RANKL, RANK, NF-κB, IKKß, NFAT2, and up-regulated the phosphatidylinositol 3-kinase (PI3K), AKT, osteoprotegerin, and c-Fos expressions, which implied CDE could suppress RANKL/RANK-induced activation of downstream NF-κB and PI3K/AKT pathways, and ultimately, preventing activity of the key osteoclastogenic proteins NFAT2 and c-Fos. All of the data suggested CDE possessed potential anti-osteoporotic activity and this effect was, at least in part, involved in modulation of RANKL/RANK/TRAF6-mediated NF-κB and PI3K/AKT signaling as well as c-Fos and NFAT2 levels. Therefore, CDE may represent a useful promising remedy candidate for treatment of postmenopausal osteoporosis.

Hollow Zn-Co Based Zeolitic Imidazole Framework as a Robust Heterogeneous Catalyst for Enhanced CO2 Chemical Fixation.

The efficient chemical conversion of carbon dioxide (CO2 ) into value-added fine chemicals is an intriguing but challenging route in sustainable chemistry. Herein, a hollow-structured bimetallic zeolitic imidazole framework composed of Zn and Co as metal centers (H-ZnCo-ZIF) has been successfully prepared via a post-synthetic strategy based on controllable chemical-etching of the preformed solid ZnCo-ZIF in tannic acid. The creation of hollow cavities inside each monocrystalline ZIFs could be achieved without destroying the intrinsic frameworks, as characterized by field-emission scanning electron microscopy, transmission electron microscopy, and X-ray diffraction technologies. The as-synthesized H-ZnCo-ZIF exhibited remarkable catalytic activity in the cycloaddition of CO2 with epoxides to the corresponding cyclic carbonates, outperforming the solid ZnCo-ZIF analogue due to the improved mass transfer originating from the hollow structure. More importantly, due to stabilization of metal centers in the ZIF framework by the tannic acid shell, H-ZnCo-ZIF exhibited good recyclability, and no activity loss could be observed in six runs. The present study provides a simple and effective strategy to enhance the catalytic performance of ZIFs by creating a hollow structure via chemical etching.

Clinical characterization and mutation spectrum in patients with familial adenomatous polyposis in China.

BACKGROUND AND AIM: Familial adenomatous polyposis (FAP) is the most common adenomatous polyposis syndrome. Patients with FAP are screened for germline mutations of two genes, APC and MUTYH. However, limited data exist on the clinical characterization and genotypic spectrum of FAP in China. This study was aimed to determine APC and MUTYH mutational status in a small cohort of FAP probands in China and to characterize the genotype-phenotype correlation in mutated patients. METHODS: Mutation screening of 46 unrelated probands was performed using multigene panels by next-generation sequencing. Clinical data of the index were used to assess genotype-phenotype correlations. RESULTS: Overall, 42 out of 46 (91.30%) unrelated probands found mutations, including 35 (76.09%) with APC mutations, 3 (6.52%) with MUTYH mutations, and 4 (8.70%) with both APC and MUTYH mutations. Ten APC genetic alterations variants were novel. The hereditary pattern of the family with both APC and MUTYH mutations was autosomal dominant inheritance. Upper gastrointestinal polyp was the most common extracolonic manifestations. The onset time for patients with both APC and MUTYH mutations was earlier than MUTYH mutation carriers and similar to APC mutation carriers. But the age of carcinogenesis for patients with both APC and MUTYH mutations was later than APC mutation carriers and similar to MUTYH mutation carriers. CONCLUSION: In this study, we show the importance of using multigene panels that allow for a parallel comprehensive screening. We suggest that genetic testing of patients with suspected adenomatous polyposis syndromes should include APC and MUTYH gene mutation analyses simultaneously.

Self-supported Co-doped FeNi carbonate hydroxide nanosheet array as a highly efficient electrocatalyst towards the oxygen evolution reaction in an alkaline solution.

The evolution of molecular hydrogen from electrochemical water splitting has currently emerged as one of the promising strategies to address the ever-increasing energy crisis and environmental pollution. The development of low-cost, highly efficient and long-term durable electrocatalysts is still challenging for practical large-scale water splitting applications. Herein, a highly crystallized Co-doped FeNi carbonate hydroxide nanosheet array was strongly grown on a conductive nickel foam (Co-FeNi CH/NF) and was used as an oxygen evolution reaction (OER) electrocatalyst. The ternary Co-FeNi CH/NF electrode exhibited an improved OER activity and good durability for at least 20 hours. The electrode delivered current densities of 10 and 500 mA cm-2 at extremely low overpotentials of 202 and 254 mV along with a small Tafel slope of 37.5 mV dec-1 in a 1.0 M KOH electrolyte solution. The incorporation of an equivalent amount of cobalt into the trigonal FeNi CH crystal lattice significantly increased the electrochemical active surface area and reduced the electron transport resistance by effectively regulating the electronic structure of the resultant electrocatalyst. These interesting observations highlight the importance of the subtle combinations of the active earth-abundant metals with electronic structure modulations.