Herbal Textual Research on Farfarae Flos in Famous Classical Formulas / 中国实验方剂学杂志

By consulting ancient and modern literature， the herbal textual research of Farfarae Flos has been conducted to verify the name， origin， producing area， quality evaluation， harvesting and processing methods， so as to provide reference for the development and utilization of the famous classical formulas containing Farfarae Flos. According to the research， the results showed that Farfarae Flos was first described as a medicinal material by the name of Kuandonghua in Shennong Bencaojing（《神农本草经》）， and the name was used and justified by later generations. The main origin was the folwer buds of Tussilago farfara， in addition， the flower buds of Petasites japonicus were used as medicine in ancient times. The ancient harvesting time of Farfarae Flos was mostly in the twelfth month of the lunar calendar， and the modern harvesting time is in December or before the ground freeze when the flower buds have not been excavated. Hebei， Gansu， Shaanxi are the authentic producing areas with the good quality products. Since modern times， its quality is summarized as big， fat， purple-red color， no pedicel is better. Processing method from soaking with licorice water in the Northern and Southern dynasties to stir-frying with honey water followed by micro-fire in the Ming dynasty， and gradually evolved to the modern mainstream processing method of honey processing. Based on the research results， it is suggested that the dried flower buds of T. farfara， a Compositae plant， should be selected for the development of famous classical formulas containing Farfarae Flos， and the corresponding processed products should be selected according to the specific processing requirements of the formulas， and raw products are recommended for medicinal use without indicating processing requirements.

Herbal Textual Research on Anemarrhenae Rhizoma in Famous Classical Formulas / 中国实验方剂学杂志

Through reviewing ancient and modern literature， the textual research of Anemarrhenae Rhizoma（AR） has been conducted to verify the name， origin， changes in production areas， quality evaluation， harvesting and processing methods， so as to provide reference for the development and utilization of the famous classical formulas containing AR. Through the herbal textual research， AR was first published in Shennong Bencaojing， and has been used as the proper name for this herb for generations， and the mainstream source of AR used for generations is the rhizome of Anemarrhena asphodeloides. The high-quality production areas that have been revered throughout the ages are Hebei， Shanxi， Shaanxi， Inner Mongolia and Fangshan district of Beijing， etc. In recent times， AR produced in Yixian county of Hebei province（Xiling Zhimu）， is better known and is regarded as a very good source. At present， cultivated AR is mainly produced in Yixian county and Anguo of Hebei province， Bozhou of Anhui province and other places. The medicinal parts of AR in ancient and modern times are all rhizomes， and the quality is better if it has thick flesh， hard wood， yellow outer color and white section color. The harvesting time recorded in ancient medical books is usually in lunar February and August， with exposure to dryness， while modern harvesting is spring and autumn. The processing methods of the past dynasties were mainly to remove the hair when using， avoid iron when cutting， process with wine or salt water， while the two main specifications in modern times are raw and salted products. Based on the systematic research， it is recommended that the dried rhizome of A. asphodeloides in the famous classical formulas be used for AR. If the original formula specifies processing requirements， it should be operated according to the requirements， if the processing requirements are not indicated， the raw products can be used as medicine.

Light from heat lamps affects sow behaviour and piglet salivary melatonin levels.

The light environment regulates animal physiology and behaviour. As widely used supplementary heat sources in creep areas, the effect of visible light radiated by infrared heat lamps on pigs is worth investigating. To investigate the effects of light from heat lamps on the behaviour of sows and piglets and possible endocrine mechanisms, 24 primiparous sows were randomly assigned to three supplementary heat source treatments: (1) 250 W non-luminous ceramic heat lamps (CE, n = 8), (2) 175 W red heat lamps (RL, n = 8), and (3) 175 W transparent heat lamps (TL, n = 8). All heat lamps were turned off on Day 15 postpartum. Piglets were weighed on days 3 and 21 postpartum. The number and duration of suckling within 24 h were analysed via video recordings on days 4, 8, and 16 postpartum. Sow posture changes during the day and night were detected using the YOLOv4 target detection network model. One marked piglet from six litters randomly selected from each treatment was used for saliva collection. Saliva samples were collected at 0800, 1400, 2000, and 0200 (+1 d) on days 10 and 20 postpartum. The results showed that the mean postural change frequency of TL sows was higher than that of CE sows (P < 0.05), while that of RL sows was not different from that of CE and TL sows. However, the duration of the sows being in each posture was not affected by the treatment. The total suckling duration of TL piglets was significantly longer than that of CE piglets, but there was no significant difference in the performance of the piglets. The melatonin concentrations in the saliva of piglets at 10 and 20 days of age in the three treatments showed different diurnal rhythms, but there was no significant difference in the levels of melatonin in TL piglets between night and day. Differences in salivary cortisol levels only appeared between the CE and RL groups at 20 days of age. Based on the present results, the illuminance and spectrum of the transparent heat lamps were sufficient to stimulate sow activity and inhibit melatonin levels in piglets. However, the stimulating effect on suckling was not sufficient to significantly improve the performance of piglets. Exposure to red heat lamps, rather than ceramic lamps, resulted in the strongest circadian rhythm of salivary melatonin in piglets.

Herbal Textual Research on Schizonepetae Herba in Famous Classical Formulas / 中国实验方剂学杂志

In this paper， the name， classification， origin and other aspects of Schizonepetae Herba in the famous classical formulas were researched by referring to the related herbal literature， medical books and prescription books in the past dynasties. The results showed that Schizonepetae Herba first appeared in Shennong Bencaojing （《神农本草经》） as Jiasu， while Jingjie first appeared in Wupu Bencao （《吴普本草》）， and the name of Jingjie was mainly used as the rectification of name in later generations. The name of Jiasu is mostly derived from its smell， and the name of Jingjie is mostly derived from its pronunciation. Schizonepeta tenuifolia has been highly praised in the past as a original material， and its genuine producing area is Jiangsu， Hebei and other places， medicinal part is whole herb with spike. In modern times， the quality of Schizonepetae Herba is best described as having thin stems， green spike， and aroma. In clinical application， the raw products of Schizonepetae Herba is mainly used， and the carbonisata is mainly used for hemostasis. Famous classical formulas of Huaihuasan and Danggui Yinzi are all made of Schizonepetae Spica， so it is recommended to use the dried panicle of S. tenuifolia. In Liangxue Dihuangtang， Schizonepetae Herba Carbonisata is used， therefore， it is suggested to adopt the processing method of Schizonepetae Herba Carbonisata in the 2020 edition of Chinese Pharmacopoeia.

Herbal Textual Research on Ephedrae Herba in Famous Classical Formulas / 中国实验方剂学杂志

Ephedrae Herba is a commonly used medicine for dispersing wind and cold， which has a long medicinal history. By referring to the herbal literature， medical books and prescription books， this paper intends to carry out herbal textual research on the name， origin， medicinal part， producing area， harvesting and processing methods of Ephedrae Herba in famous classical formulas， in order to provide the basis for the development of relevant famous classical formulas. According to textual research， the main base of ancient Ephedrae Herba was Ephedra sinica. The medicinal part is the herbaceous stems of Ephedrae Herba. Before the Northern and Southern dynasties， the origin of the records was Jindi and Hedong， which is now Shanxi province. In the Northern and Southern dynasties and later generations， the producing area expanded， and now it is mainly distributed in Hebei， Shanxi， Shaanxi， Inner Mongolia， Gansu， Liaoning and other places， among which Inner Mongolia is the main producing area. The harvesting and processing methods in the past dynasties are to harvest the stems in autumn， dry them in the shade or air to 70%-80% dry， and then dry them in the sun. The processing methods in the past dynasties mainly include removing the knots， wine-fried， honey-fried， processing with vinegar and so on， at present， only honey-fried is still in use. Based on the research results， it is suggested that Ephedrae Herba in famous classical formulas should be selected the dry herbaceous stems of E. sinica. If the processing requirements are not indicated， it is suggested to use raw products of Ephedrae Herba.

Quality evaluation of Saposhnikoviae Radix based on QAMS combined with information entropy-response surface method / 中国中药杂志

This research was used with high performance liquid chromatography(HPLC), combined with information entropy-response surface method(RSM) to investigate the ethanol concentration, extraction time, liquid-to-material ratio. Taking the content of four chromogens as evaluation indexes, the weight coefficients of each index were given, and the comprehensive score was calculated to optimize the extraction process. Then, prim-O-glucosylcimifugin was used as the reference, the relative calibration factors(RCFs) of cimifugin, 4'-O-β-D-glucosyl-5-O-methylvisamminol and sec-O-glucosylhamaudo to prim-O-glucosylcimifugin were calculated respectively. The contents of four components in Saposhnikoviae Radix were determined by both external standard method(ESM)and quantitative analysis of multi-components by single marker(QAMS) method, and the results were compared. At last, combined with principal component analysis(PCA) and orthogonal partial least squares discriminant analysis(OPLS-DA) to evaluate the quality of the Saposhnikoviae Radix in different production areas. The optimal extraction process parameter of the Saposhnikoviae Radix was as follows: liquid-to-material ratio is 60∶1(mL·g~(-1)), extraction time is 35 min, and ethanol concentration is 70%. The repeatability of the RCFs was perfect, and the results calculated by the QAMS were consistent with the results from the ESM. The stoichiometric results indicate that there are obvious differences in the distribution of Saposhnikoviae Radix in different production areas, and cimifugin and prim-O-glucosylcimifugin are the characteristic compounds that cause this difference. In this study, the optimal extraction process is stable and feasible, and the method of QAMS is accurate and reliable. From the perspective of four chromogens, there are differences in the quality of the Saposhnikoviae Radix in different production areas. Therefore, the established extraction process combined with the method of QAMS can be used to evaluate the quality of Saposhnikoviae Radix and provide a scientific basis for the quality control of Saposhnikoviae Radix.

Protective effect of Qilin Pills on the reproductive function of oligoasthenospermia rats / 中华男科学杂志

Objective@#To study the protective effect of Qilin Pills (QLP) on the reproductive function of rats with oligoasthenospermia (OAS) induced by tripterygium glycosides.@*METHODS@#Twenty-eight male SD rats were randomly divided into a normal control, an OAS model control, a low-dose QLP, and a high-dose QLP group of equal number. OAS models were made in the latter three groups by intragastrical administration of tripterygium glycosides at 40 mg per kg of the body weight per day, and meanwhile the animals in the low- and high-dose QLP groups were treated with QLP at 1.62 and 3.24 g per kg of the body weight per day, respectively, while those in the OAS model group with normal saline, all for 30 consecutive days. Then all the rats were executed for obtaining the testis weight, testis viscera index, epididymal sperm concentration and motility, reproductive hormone levels, and antioxidation indexes and observation of the histomorphological changes of the testis tissue by HE staining.@*RESULTS@#After 30 days of intervention, the low- and high-dose QLP groups, as compared with the OAS model controls, showed significantly improved epididymal sperm concentration (［14.57 ± 3.95］ and ［39.71 ± 11.31］ vs ［4.71 ± 1.25］ ×10⁶/ml, P <0.05) and motility (［3.71 ± 1.11］ and ［4.29 ± 1.80］ vs ［0.57 ± 0.53］%, P <0.05), increased levels of sex hormone binding globulin (SHBG) (［94.83 ± 11.17］ and ［88.05 ± 9.21］ vs ［56.74 ± 8.29］ nmol/L, P <0.05) and free testosterone (FT) (［27.27 ± 3.63］ and ［32.80 ± 2.51］ vs ［22.81 ± 2.75］ nmol/L, P <0.05), decreased level of follicle-stimulating hormone (FSH) (［1.49 ± 0.62］ and ［1.12 ± 0.83］ vs ［1.71 ± 0.52］ mIU/ml, P <0.05), but no significant change in the total testosterone (TT) level. Meanwhile, the level of superoxide dismutase (SOD) was markedly elevated in the low- and high-dose QLP groups in comparison with the OAS model control group (［277.14 ± 15.84］ and ［299.60 ± 20.83］ vs ［250.04 ± 31.06］ U/ml, P <0.05) while that of reactive oxygen species (ROS) remarkably reduced (［397.61 ± 62.71］ and ［376.84 ± 67.14］ vs ［552.20 ± 58.07］ IU/ml, P <0.05). HE staining showed that QLP intervention significantly increased the layers and quantity of spermatogenic cells in the testicular seminiferous tubules of the OAS rats.@*CONCLUSIONS@#QLP can effectively protect the reproductive system of oligoasthenospermia rats by raising sperm quality, elevating reproductive hormone levels, reducing oxidative stress injury, and improving histomorphology of the testis.

Acousto-optic tunable filter near-infrared spectroscopy for in-line monitoring liquid-liquid extraction of Gardenia jasminoides Ellis based on statistical analysis.

This study aimed to monitor liquid-liquid extraction of Gardenia jasminoides Ellis (Zhizi in Chinese) using in-line near-infrared spectroscopy. Shanzhiside (SZS), deacetyl asperulosidic acid methyl ester (DAAME), genipin-1-ß-D-gentiobioside (GG), geniposide (GS), total acids (TA) and soluble solid content (SSC) were selected as quality control indicators, and measured by reference methods. Both partial least-squares regression (PLSR) and back propagation artificial neural networks (BP-ANN) were applied to create models to predict the content of above indicators. Paired-samples t-test and nonparametric test were used to compare differences in predictive values between two models of each indicator. Relative standard error of prediction (RSEP) and mean absolute percentage error (MAPE) were used to evaluate the predictive accuracy of the established models. The results showed that there was no significant difference in predicting DAAME, GS and TA between two models. However, PLSR model gave better accuracy in predicting GG and SZS than BP-ANN model. The BP-ANN model of SSC was better than PLSR model. This study shows that NIR spectroscopy can be used for rapid and accurate analysis of quality control indicators in the liquid-liquid extraction of Zhizi. Simultaneously, this study can serve as technical support for the application of NIR spectroscopy in the industrial production process.

The anti-infective activity of punicalagin against Salmonella enterica subsp. enterica serovar typhimurium in mice.

Punicalagin, a major bioactive component of pomegranate peel, has been proven to have antioxidant, antiviral, anti-apoptosis, and hepatoprotective properties. The aim of this study was to investigate the anti-infective activity of punicalagin in a mouse model. C57BL/6 mice were initially challenged with Salmonella enterica subsp. enterica serovar typhimurium (S. typhimurium) and then treated with punicalagin. Food and water consumption and body weight were recorded daily. On day 8 post infection, the mice were sacrificed to examine pathogen counts in tissues, hematological parameters, cytokine levels, and histological changes. Compared to mice only infected with S. typhimurium, punicalagin-treated mice had more food consumption and less weight loss. A higher survival rate and lower counts of viable S. typhimurium in feces, liver, spleen, and kidney were found in the punicalagin-treated mice. The enzyme linked immunosorbent assay showed that the levels of IL-6, IL-10, and IFN-γ in serum and the spleen and TNF-α in serum, the spleen and the liver were reduced by punicalagin. Moreover, more neutrophils and higher neutrophil-to-mononuclear cell ratios in the punicalagin-treated mice were observed. Histological examination showed that punicalagin protected cells in the liver and spleen from hemorrhagic necrosis. It is concluded that punicalagin has a beneficial effect against S. typhimurium infection in mice. The anti-infective properties, together with other nutritionally beneficial effects, make punicalagin a promising supplement in human food or animal feeds to prevent disease associated with S. typhimurium.

[Quality control in liquid-liquid extraction of Reduning injection using near-infrared spectroscopy technology].

Quantitative models were established to analyze the content of chlorogenic acid and soluble solid content in the liquid-liquid extraction of Reduning injection by near-infrared (NIR) spectroscopy. Seven batches of extraction solution from the liquid-liquid extraction of Lonicerae Japonicae Flos and Artemisiae Annuae Herba were collected and NIR off-line spectra were acquired. The content of chlorogenic acid and soluble solid content were determined by the reference methods. The partial least square (PLS) and artificial neural networks (ANN) were used to build models to predict the content of chlorogenic acid and soluble solid content in the unknown samples. For PLS models, the R2 of calibration set were 0.9872, 0.9812, RMSEC were 0.1533, 0.7943, the R2 of prediction set were 0.9837, 0.9733, RMSEP were 0.2464, 1.2594, RSEP were 3.25%, 3.31%, for chlorogenic acid and soluble solid content, respectively. For ANN models, the R2 of calibration set were 0.9903, 0.9882, RMSEC were 0.0974, 0.4543, the R2 of prediction set were 0.9868, 0.9699, RMSEP were 0.1920, 0.9427, RSEP were 2.61%, 2.75%, for chlorogenic acid and soluble solid content, respectively. Both the RSEP values of chlorogenic acid and soluble solid content were lower than 6%, which can satisfy the quality control standard in the traditional Chinese medicine production process. The RSEP values of ANN models were lower than PLS models, which indicated the ANN models had better predictive performance for chlorogenic acid and soluble solid content. The established method can rapidly measure the content of chlorogenic acid and soluble solid content. The method is simple, accurate anc reliable, thus can be used for quality control of the liquid-liquid extraction of Reduning injection.

Quality control in liquid-liquid extraction of Reduning injection using near-infrared spectroscopy technology / 中国中药杂志

Quantitative models were established to analyze the content of chlorogenic acid and soluble solid content in the liquid-liquid extraction of Reduning injection by near-infrared (NIR) spectroscopy. Seven batches of extraction solution from the liquid-liquid extraction of Lonicerae Japonicae Flos and Artemisiae Annuae Herba were collected and NIR off-line spectra were acquired. The content of chlorogenic acid and soluble solid content were determined by the reference methods. The partial least square (PLS) and artificial neural networks (ANN) were used to build models to predict the content of chlorogenic acid and soluble solid content in the unknown samples. For PLS models, the R2 of calibration set were 0.9872, 0.9812, RMSEC were 0.1533, 0.7943, the R2 of prediction set were 0.9837, 0.9733, RMSEP were 0.2464, 1.2594, RSEP were 3.25%, 3.31%, for chlorogenic acid and soluble solid content, respectively. For ANN models, the R2 of calibration set were 0.9903, 0.9882, RMSEC were 0.0974, 0.4543, the R2 of prediction set were 0.9868, 0.9699, RMSEP were 0.1920, 0.9427, RSEP were 2.61%, 2.75%, for chlorogenic acid and soluble solid content, respectively. Both the RSEP values of chlorogenic acid and soluble solid content were lower than 6%, which can satisfy the quality control standard in the traditional Chinese medicine production process. The RSEP values of ANN models were lower than PLS models, which indicated the ANN models had better predictive performance for chlorogenic acid and soluble solid content. The established method can rapidly measure the content of chlorogenic acid and soluble solid content. The method is simple, accurate anc reliable, thus can be used for quality control of the liquid-liquid extraction of Reduning injection.

[Determination of eleven major components and fingerprint chromatography for Reduning injection by UPLC].

A reliable method for simultaneous determinition of eleven representative components (neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C, shanzhiside, geniposidic acid, genipin-1-ß-D-gentiobioside, geniposide and secoxyloganin) in combination of chromatographic fingerpint analysis for Reduning injection was developed by ultra high-performance liquid chromatography (UPLC). The method was performed on an Agilent ZORBAX SB-C18 anlytical column (3. 0 mm x 100 mm, 1. 8 µm) with a guard column of Agilent UPLC Guard ZORBAX SB-C18 (3.0 mm x 5 mm) at the column temperature of 30 °C. The gradient mobile phase consisted of acetonitrile (A)-0. 1% phosphoric acid (B) with a flow rate of 0. 4 mL . min-1. The injection volumn was 2 µL. The detection wavelengths were set at 324 nm and 238 nm for quantit tive analysis and 225 nm for fingerpint chromatography. Neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C, shanzhiside, geniposidic acid, genipin-1-ß-D-gentiobioside, geniposide and secoxyloganin were baseline seperated with good linearity relationships (r >0. 999) between concentration and peak areas over the linear ranges. The average recoverys of the investigated compounds were 103.5%, 100. 2%, 103. 3%, 102. 8%, 101. 3%, 102. 8%, 97. 36%, 99. 62%, 98. 16%, 102. 8%, 99. 27%, respectively. Reduning injection of forty-five batches was analyzed by UPLC finge print chromatography. Thirty batches were selected to generate the reference fringerprint chromatography with fourteen common peaks. The similarity values between the reference fringerprint chromatography and the remaining fifteen batches were higher than 0. 99. The developed method was fast, accurate and sensitive. It could be used as a reference for the quality control of multiple components determination and fingerprint chromatography for Reduning injection in future.

Determination of eleven major components and fingerprint chromatography for Reduning injection by UPLC / 中国中药杂志

A reliable method for simultaneous determinition of eleven representative components (neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C, shanzhiside, geniposidic acid, genipin-1-β-D-gentiobioside, geniposide and secoxyloganin) in combination of chromatographic fingerpint analysis for Reduning injection was developed by ultra high-performance liquid chromatography (UPLC). The method was performed on an Agilent ZORBAX SB-C18 anlytical column (3. 0 mm x 100 mm, 1. 8 µm) with a guard column of Agilent UPLC Guard ZORBAX SB-C18 (3.0 mm x 5 mm) at the column temperature of 30 °C. The gradient mobile phase consisted of acetonitrile (A)-0. 1% phosphoric acid (B) with a flow rate of 0. 4 mL . min-1. The injection volumn was 2 µL. The detection wavelengths were set at 324 nm and 238 nm for quantit tive analysis and 225 nm for fingerpint chromatography. Neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C, shanzhiside, geniposidic acid, genipin-1-β-D-gentiobioside, geniposide and secoxyloganin were baseline seperated with good linearity relationships (r >0. 999) between concentration and peak areas over the linear ranges. The average recoverys of the investigated compounds were 103.5%, 100. 2%, 103. 3%, 102. 8%, 101. 3%, 102. 8%, 97. 36%, 99. 62%, 98. 16%, 102. 8%, 99. 27%, respectively. Reduning injection of forty-five batches was analyzed by UPLC finge print chromatography. Thirty batches were selected to generate the reference fringerprint chromatography with fourteen common peaks. The similarity values between the reference fringerprint chromatography and the remaining fifteen batches were higher than 0. 99. The developed method was fast, accurate and sensitive. It could be used as a reference for the quality control of multiple components determination and fingerprint chromatography for Reduning injection in future.

Oxygen-coupled redox regulation of the skeletal muscle ryanodine receptor/Ca2+ release channel (RyR1): sites and nature of oxidative modification.

In mammalian skeletal muscle, Ca(2+) release from the sarcoplasmic reticulum (SR) through the ryanodine receptor/Ca(2+)-release channel RyR1 can be enhanced by S-oxidation or S-nitrosylation of separate Cys residues, which are allosterically linked. S-Oxidation of RyR1 is coupled to muscle oxygen tension (pO2) through O2-dependent production of hydrogen peroxide by SR-resident NADPH oxidase 4. In isolated SR (SR vesicles), an average of six to eight Cys thiols/RyR1 monomer are reversibly oxidized at high (21% O2) versus low pO2 (1% O2), but their identity among the 100 Cys residues/RyR1 monomer is unknown. Here we use isotope-coded affinity tag labeling and mass spectrometry (yielding 93% coverage of RyR1 Cys residues) to identify 13 Cys residues subject to pO2-coupled S-oxidation in SR vesicles. Eight additional Cys residues are oxidized at high versus low pO2 only when NADPH levels are supplemented to enhance NADPH oxidase 4 activity. pO2-sensitive Cys residues were largely non-overlapping with those identified previously as hyperreactive by administration of exogenous reagents (three of 21) or as S-nitrosylated. Cys residues subject to pO2-coupled oxidation are distributed widely within the cytoplasmic domain of RyR1 in multiple functional domains implicated in RyR1 activity-regulating interactions with the L-type Ca(2+) channel (dihydropyridine receptor) and FK506-binding protein 12 as well as in "hot spot" regions containing sites of mutation implicated in malignant hyperthermia and central core disease. pO2-coupled disulfide formation was identified, whereas neither S-glutathionylated nor sulfenamide-modified Cys residues were observed. Thus, physiological redox regulation of RyR1 by endogenously generated hydrogen peroxide is exerted through dynamic disulfide formation involving multiple Cys residues.

Antifeedant activity of spin-labeled derivatives of deoxypodophyllotoxin against Brontispa longissima larvae.

To continue our search for natural product-based compounds for the control of Brontispa longissima larvae, eight spin-labeled podophyllotoxin derivatives (4a-h) and the intermediates 2 and 3 were tested for their insect antifeedant activity against third-instar larvae of B. longissima. Among all the tested compounds, 4a, 4c, 2 and 3 showed pronounced antifeedant activities with AFC50 values of 0.16, 0.31, 0.15 and 0.28 mg/mL, respectively. The different antifeedant activity ranges of these compounds indicated that variation of the structures of L-amino acids in these compounds markedly affected the activity profiles of this compound class, and some important SAR information has been revealed from it.

Clinical outcome of the combined nutritional support for colorectal cancer patients at nutritional risk: a retrospective study of 60 cases / 中华临床营养杂志

ObjectiveTo explore the clinical outcome of the combined nutrition support for colorectal cancer patients.MethodsTwo research arms were obtained using a cohort sampling method.Ann A ( the study group): from 2009 to 2010,30 colorectal cancer patients were enrolled.They received nutritional risk screening (NRS) 2002 after admission.Nutritional risk was defined as NRS 2002 score ≥3 three days before operation.Patients with nutritional risk received enteral nutrition (EN) for bowel preparation without laxative drug and enema.After operation,they received EN combined with parenteral nutrition (PN) supports provided.Arm B (control group): 30 cases with historically confirmed colorectal cancer were enrolled from 2007 to 2008.They received routine bowel preparation (diet control,laxative drug,and enema) and PN supports after operation.Nutritional parameters,the rate of infectious complications,the rate of systemic inflammatory response syndrome,and the duration of hospital stay were analyzed.ResultsThere were no significant difference in body weight and plasma albumin between these two arms ( P ＞ 0.05 ). The incidence of systemic inflammatory response syndrome (13.3 ％ ),infectious complications (10.0％ ),and the duration of hospital stay [ (12.3 ± 6.5 ) d ] in arm A were significantly lowerthan those in arm B [33％,30％,and (15.0 ±7.2) d,respectively] (P =0.038,P =0.042,P =0.045).Conclusion For the colorectal cancer patients,nutritional risk screening on admission,bowel preparation with eneral nutrition before operation,and combined nutritional support after operation can improve the clinical outcome.

[Antitumor effect of calcium phosphate cement incorporating doxorubicin microspheres].

OBJECTIVE: To investigate the antitumor effect of calcium phosphate cement incorporated with doxorubicin microspheres. METHODS: The absorbance at 490 nm of SaoS-2 cells cultured for 5 days in the media containing the extract of the cement incorporating doxorubicin microspheres was measured using Cell Counting Kit-8. SaoS-2 cells were adjusted to the density of 2x10(7) ml(-1) and injected into the left buttock of nude mouse in the volume of 0.2 ml. The cell suspension (0.1 ml) mixed with an equal volume of the cement extract were injected into the right buttock and on the back of the bilateral ears of nude mice. At 12 days after the cell injection, the tumor tissues were obtained and weighed to calculate the tumor inhibition rate, and the pathological samples were observed with HE staining. RESULTS: The extract of the bone cement containing doxorubicin microspheres showed inhibitory effects on the tumor growth in a dose-dependent manner. The tumor inhibition rate reached 61.0% in high-dose group. Tumor necrosis was found in high dose group, but virtually absent in low-dose group. CONCLUSIONS: CPC containing doxorubicin PLGA microspheres can inhibit tumor cell growth both in vitro and in vivo.

Synergistic myoprotection of L-arginine and adenosine in a canine model of global myocardial ischaemic reperfusion injury / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Endogenous nitric oxide and adenosine increase simultaneously to keep the balance of energy demand and supply when the oxygen supply is insufficient, which suggests that nitric oxide and adenosine might exert a synergistic myoprotection during tissue hypoxia. In this study, we tested this hypothesis utilizing a canine model of prolonged global myocardial ischaemic reperfusion injury.</p><p><b>METHODS</b>In this double blind, controlled study, the hearts of 24 anaesthetized mongrel dogs were arrested for 2 hours with aortic cross clamping and blood cardioplegia. The treatment groups were those supplemented with 2 mmol/L L-arginine (ARG), supplemented with 1 mmol/L adenosine (ADO), ARG + ADO supplemented with both, and no supplementation (control) (n = 6 in each group). Haemodynamics, biochemical indices, adenosine triphosphate (ATP) content and myeloperoxidase activities of myocardium were determined to evaluate myocardial injury. Statistical comparison was performed by two way ANOVA.</p><p><b>RESULTS</b>Although the requirements for inotropic supports were higher, the cardiac outputs were lower in control group than in ARG, ADO and the combination groups. Plasma cardiac troponin I levels were higher and the areas of hydropic changes were larger in control group than in ARG and ADO groups. Combination of arginine and adenosine provided further myoprotection with respect to better cardiac performance, lower release of cardiac troponin I, and smaller areas of hydropic changes compared with ARG and ADO groups. ATP content was higher, but myeloperoxidase activities of myocardium were significantly lower in the combination group than in control, ARG and ADO groups (P < 0.05).</p><p><b>CONCLUSIONS</b>Combination of L-arginine and adenosine provides synergistic myoprotection in a canine model of global myocardial ischaemia. Thus, the combination is recommended when the heart is exposed to a prolonged ischaemia during cardiac surgery.</p>

Reaction mechanism and regulation of mammalian thioredoxin/glutathione reductase.

Thioredoxin/glutathione reductase (TGR) is a recently discovered member of the selenoprotein thioredoxin reductase family in mammals. In contrast to two other mammalian thioredoxin reductases, it contains an N-terminal glutaredoxin domain and exhibits a wide spectrum of enzyme activities. To elucidate the reaction mechanism and regulation of TGR, we prepared a recombinant mouse TGR in the selenoprotein form as well as various mutants and individual domains of this enzyme. Using these proteins, we showed that the glutaredoxin and thioredoxin reductase domains of TGR could independently catalyze reactions normally associated with each domain. The glutaredoxin domain is a monothiol glutaredoxin containing a CxxS motif at the active site, which could receive electrons from either the thioredoxin reductase domain of TGR or thioredoxin reductase 1. We also found that the C-terminal penultimate selenocysteine was required for transfer of reducing equivalents from the thiol/disulfide active site of TGR to the glutaredoxin domain. Thus, the physiologically relevant NADPH-dependent activities of TGR were dependent on this residue. In addition, we examined the effects of selenium levels in the diet and perturbations in selenocysteine tRNA function on TGR biosynthesis and found that expression of this protein was regulated by both selenium and tRNA status in liver, but was more resistant to this regulation in testes.