Research of the core items of Physical Literacy Guidelines for Children and Adolescents / 中国学校卫生

Objective@#Physical literacy is the breakthrough point and fundamental goal to achieve the integration of sports and education, sports and public health and expand the function of physical education. Studying the children and adolescents physical literacy is a common responsibility for children and adolescents health, sports and health education workers. This article was based on the latest research evidence and expert opinions in China, aiming to develop the core items of physical literacy guidelines for Chinese children and adolescents.@*Methods@#This article systematically combed the dimensions and index system of children and adolescents physical literacy through systematic literature review. After five rounds of Delphi methods, the core items were extracted.@*Results@#The core items included four interrelated dimensions of body, emotion, behavior, and cognition, which were specifically composed of four components: physical ability, emotional experience, physical activity related behaviors, and knowledge understanding and application ability.@*Conclusion@#Children and adolescents are the key periods, sensitive periods, and window periods to cultivate physical literacy. The core items can provide framework recommendations for further refining guidelines. More empirical studies should be carried out in the future, in order to accumulate enough evidences and further to improve Physical Literacy guidelines, better to guide physical literacy promotion.

Relationship between daily physical activity and sleep quality among college students / 中国学校卫生

Objective@#To explore the relationship between daily physical activity and sleep quality among college students during COVID-19 epidemic, so as to provide scientific basis for improving physical health and sleep of college students.@*Methods@#A stratified random sampling method was used to select a total of 2 808 college students from two universities (one in each of sports and non sports categories) in Beijing, Tianjin, and Wuhan in March 2020. The Pittsburgh Sleep Quality Index scale and the Bouchard Physical Activity Diary were used to collect sleep status and sleep duration (SD), sedentary behavior (SED), low intensity physical activity (LPA), and moderate to vigorous physical activity (MVPA). The Mann Whitney U test or Kruskal Wallis test was used to analyze the variability of parameters among college students. Multiple Logistic regression was used to analyze the relationship between physical activity and sleep quality.@*Results@#During the epidemic, male students had higher MVPA times(0.5 h) than female students(0 h) ( Z =-4.21, P <0.01); students aged 18 and younger had higher SED times(11.1 h) than students aged 19 to 21 and older(9.3,10.3 h) ( F =7.90, P <0.05). The SED was higher for students living in urban, combined urban rural areas(10.5,9.5 h) than for their rural counterparts(9.5 h) ( F =9.56, 10.73, P <0.01). Sport majors had higher LPA and MVPA times(3.9, 1.0 h) than non sports majors(3.0,0 h) ( Z =-2.99, -4.73, P <0.01), and lower SED and sleep times(8.3,9.8 h) than non sports majors(11.1,11.1 h) ( Z =-4.73, -2.42, P <0.01). The LPA time of students with general sleep quality and sleep disorder was lower than that of students with good sleep quality ( F =7.67, P <0.05), and SED time was higher than that of students with good sleep quality ( F =8.62, P <0.05). After controlling for gender, age, place of residence, and specialty, multiple Logistic regression analysis showed that LPA time deficit was a risk factor for sleep quality ( OR =0.84, 95% CI =0.71-0.99, P <0.05).@*Conclusion@#During the COVID-19 epidemic period, college students generally suffer from excessive sedentary time and insufficient physical activity, which vary in sex, region and specialty. The overall sleep quality of students is not optimistic, and the lack of low intensity physical activity may increase the risk of sleep disorders.

miR-17-5p mitigates endometriosis by directly regulating VEGFA

Endometriosis is a common disease in women, which impairs the quality of life in patients. Recently, accumulating evidences reported that miRNAs play an essential role in diagnosis and treatment of endometriosis.However, the regulatory mechanism of miRNAs has not been fully explored. The expression of miR-17-5p andVEGFA was detected using qRT-PCR. The protein level of VEGFA was measured via Western blot. Cellproliferation was determined by CCK-8 assay. Cell migration and invasion were measured via transwell assay.The relationship of miR-17-5p and VEGFA were verified via luciferase reporter assay. Then miR-17-5p wasremarkably down-regulated in endometriosis tissues, serums and cells, and overexpression of miR-17-5pinhibited cell proliferation, migration and invasion in endometriosis. Results showed that VEGFA was significantly up-regulated in endometriosis tissues and cells and acted as a target of miR-17-5p. Moreover, miR17-5p negatively regulated VEGFA expression in endometriosis. Otherwise, up-regulation of VEGFAimproved cell proliferative, migrated and invasive ability in ECSCs with transfection of miR-17-5p mimicsgroup. Our data showed miR-17-5p inhibits cell proliferation, migration and invasion in endometriosis bydirectly repressing VEGFA expression.

Biotransformation of Natural Saponins / 中国实验方剂学杂志

Saponin is a kind of complex compounds with triterpenoid or spiral aglycones.Natural saponins are used as substrates,and many novel compounds are obtained by biotransformation technology. Especially, converted products of saponins with strong activities provide valuable lead compounds for the research and development of new drugs. Saponins can be divided into triterpenoid saponin and steroidal saponin according to the structure of the mother nucleus. There are about 89 reported saponin components,including 56 triterpenoid saponins and 33 steroidal saponins. Biological enzyme catalysis,microbial transformation and intestinal microflora transformation are the main bioconversion technologies and key development directions of saponins. The research and optimization technology of biological enzyme and microbial transformation of saponins are the effective methods to prepare active secondary saponins. The biotransformation reaction of saponins mainly includes hydrolysis,redox and rearrangement,resulting in the formation of aglycones,secondary glycosides and their derivatives. The hydrolysis of saponin sugar chains was the main biological transformation pathway, and could generate a number of secondary saponins with less glycosyl groups. The secondary saponins could be absorbed into blood and become real active ingredients in body. Preparation of rare secondary saponins,discovery of lead compounds and development of new drugs are the main directions of biotransformation of saponins. The studies on the metabolism and mechanism of natural saponins by microbial and intestinal microbial biotransformation will also become hotspots. According to relevant papers at home and abroad,the researches on transformation technique,transformation approach and transformation reaction of saponins from natural products in the past thirty years were summarized, and the prospects of research and development were also analyzed to provide scientific basis for further study and comprehensive utilization of these conversion products.

Optimal relationship between physical activity and body fat indexes during puberty / 中国学校卫生

Objective@#To explore the optimal correlation between physical activity and body fat indexes during pubertal transition,and to provide a reference for reducing obesity of adolescents and making the interventional measures.@*Methods@#A total of 366 junior high school students were recruited. ActiGraPh-GT3X accelerometer was used to collect daily physical activity data for 7 days. InBody 520 was used to assess body composition. Pearson partial correlation was used to analyze the correlation between physical activity level and body composition. Curve fitting was used to construct the optimal model of physical activity and body fat index.@*Results@#There was no gender difference in waist height ratio and fat mass between boys and girls(P>0.05), and the percentage of body fat in boys was significantly lower than that in girls(t=-4.73,P<0.01). There was no gender difference in light physical activity (LPA) time between boys and girls (P>0.05).The time of moderate physical activity (MPA), moderate-to-vigorous physical activity (MVPA) and vigorous physical activity (VPA) in boys was significantly higher than that in girls (P<0.01).The sedentary time in boys was significantly lower than that in girls (t=2.64，3.23，4.24，-2.85，P<0.01). For overweight and obese group, less time was spent in LPA, MPA, MVPA and VPA compared with normal group, while more time spent in sedentary time. Waist height ratio, fat mass and body fat percentage among male and female adolescents were positively correlated with sedentary time (F=14.63，15.54,P<0.01), while negatively correlated with LPA, MPA and MVPA time (P<0.05).@*Conclusion@#The body fat percentage was higher in boys than in girls,and the level of physical acitivity was even higher in boys than in girls.The adolescents of normal weight has got a higher level of physical activity than over weight or obese adolescents. Long-term adherence to certain physical activities and appropriate reduction of sedentary time are of vital importance for teenagers to effectively control their weight and prevent chronic diseases.

Synthesis and antitumor activity of fluoroquinolon-3-yl-s-triazole sulfide ketones and their derivatives from ciprofloxacin / 药学学报

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.

Synthesis and anti-proliferative activity of fluoroquinolone (rhodanine unsaturated ketone) amide derivatives / 药学学报

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.

Design, synthesis, antibacterial and anti-cell proliferation activities of 1,2,4triazino3,4-h 1,8naphthyridine-8-one-7-carboxylic acid derivatives / 药学学报

To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.

Synthesis and antitumor activity of fluoroquinolon-3-yl s-triazole sulfanylacetylhydrazones and s-triazole hydrazone derivatives (V) / 中国药学杂志

OBJECTIVE: To explore an efficient modification strategy for conversion of antibacterial fluoroquinolones to antitumor ones. METHODS: An azole heterocyclic ring, s-triazole, as a bioisotere of the C-3 carboxylic acid for ofloxacin(1), functional acyl-hydrazones and hydrazones, was used as the modified side-chain for the C-3 bioisotere, then the C-3 s-triazole acylhydrazones and s-triazole hydrazone derivatives were designed and their in vitro antitumor activity was evaluated by MTT assay. RESULTS: Fourteen target compounds were synthesized, and they exhibited stronger antitumor activity than the parent ofloxacin. And most importantly, hydrazone derivatives had higher activity than their corresponding acylhydrazone compounds. CONCLUSION: s-Triazole-hydrazone moiety is warranted special attention as an efficient bioisosteric replacement of the C-3 carboxylic acid for further development of antitumor fluoroquinolone lead compounds.

Synthesis, antitumor activity and SAR of C-3 oxadiazole sulfanylacetylhydrazone-substituted fluoroquinolone analogues / 药学学报

To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.

Chemical constituents from rhizomes of Cyperus rotundus / 中草药

Objective: To study the chemical components from the rhizomes of Cyperus rotundus. Methods: The compounds were isolated and purified by chromatographic techniques, and their structures were elucidated by spectral methods. Results: A new isoflavonoid, 5, 7, 4'-trihydroxy-2'-methoxy-3'-prenylisoflavone (1), along with nine phenolic compounds, 6-O-p-hydroxybenzoyl- 6-epi-aucubin (2), 6-O-p-hydroxybenzoyl-6-epi-monomelittoside (3), verproside (4), syringopicroside B (5), syringopicroside C (6), oleuropeinic acid (7), oleuroside (8), 10-hydroxyoleuropein (9), and senburiside I (10), were obtained from the rhizomes of C. rotundus. Conclusion: Compound 1 is a new isoflavone, named cyperotundone A, and compounds 2-10 are isolated from this plant for the first time.

Steroidal saponins and phenylic constituents from Lilium lancifolium and their anti-oxidant activities / 中草药

Objective: To study the steroidal saponins and phenylic constituents in the bulbs of Lilium lancifolium and their anti-oxidant activities in vitro. Methods: The constituents were isolated and purified by chromatographic technique and recrystallization, and their structures were identified by spectral methods together with physiochemical analyses. The anti-oxidant effects of these constituents on DPPH and ABTS were screened in vitro. Results: Eleven constituents were isolated including seven first-found ones (1-5, 9, and 10) and four known compounds in this plant. They were cis-1-O-p-coumaroylglycerol (1), trans-1-O-p-coumaroylglycerol (2), caffeoyl glyceride (3), 3,4- dihydroxybenzaldehyde (4), salicylic acid (5), (25R,26R)-26-methoxyspirostan-5- ene-3β-O-α-L-rhamnopyranosyl-(1→2)-[β-D-glucopyranosyl- (1→6)]-β-D-glucopyranoside (6), (25R,26R)-3β, 17α-dihydroxy-26-methoxyspirostan-5-ene-3β-0-a-Z.-rhamnopyranosyl-(l- >2)-[β-D-glucopyranosyl-(l-"6)]-β-D-glucopyranoside (7), diosgenin 3-O-{O-α-L-rhamnopyranosyl-(1→2)-O-[β-D-xylopyranosyl- (1→3)]-β-D-glucopyranoside} (8), (25R)-3β,17α-dihydroxy- 5α-spirostan-6-one-3-O-α-L-rhamnopyranosyl-(1→2) -β-D-glucopyranoside (9), (25R)-3β-hydroxy-5α-spirostan-6-one-3- O-α-L-rhamnopyranosyl-0 (1→2)-β-D-glucopyranoside (10), and (25R)-spirost-5-ene-3β-O-α-L-rhamnopyranosyl-(1→2) -[β-D-glucopyranosyl-(1→6)]-β-D-glucopyranoside (11). Compounds 1-5 showed the favorable scavenging effects on DPPH and ABTS. Conclusion: The study suggests that the phenylic constituents from the bulbs of L. lancifolium have the anti-oxidant effects.

Chemical constituents of antineoplastic actinomycete strain (N2010-37) of bottom mud in mangrove (I) / 中草药

Objective: To study the chemical constituents in the cultured filaments of an antitumor actinomycete strain (N2010-37). Methods: Compounds were isolated and purified by chromatographic techniques and recrystallization, and the structures were identified by spectral methods together with physicochemical analysis. The antitumor effects of these compounds were tested in vitro by MTT method. Results: Three compounds were identified including two anthrones and one novel macrolide. They were (3S, 4R, 7R, 8R, 9S)-3, 8-dihydroxy-4, 7,9-trimethyl-2,6-cyclononanediiolacetone (1), 2-hydroxy-1-methoxy-3- methylanthraquinone (2), and 1, 6, 8-thihydroxy-3-methylanthraquinone (3). Conclusion: Compound 1 is a new compound, and compounds 1 and 3 show the favorable cytotoxic activity against human chronic granulocytic leukemia cell line K562 strain by MTT method in vitro.