Effects of a chitosan nanoparticles encapsulation on the properties of litchi polyphenols.

Litchi polyphenols have very specific biological activities. Nevertheless, the low and inconsistent oral bioavailability and instability hinder the further application of litchi polyphenols in food systems. This work prepared litchi polyphenols loaded chitosan nanoparticles (LP-CSNPs) by ionic gelation method to enhance the encapsulation on the properties of litchi polyphenols. The optimum conditions of formation via single factors and the Box-Behnken design were chitosan (CS) concentration 1.065 mg/mL, sodium tripolyphosphate (TPP) concentration 0.975 mg/mL, and the mass ratios of polyphenols and CS 1:1 with encapsulation efficiency (EE%) of 45.53%. LP-CSNPs presented the nanosized range of particle size (mean 170 nm), excellent polydispersity index (PDI) (0.156 ± 0.025), and zeta potential values (+ 35.44 ± 0.59). The in vitro release in simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8) during 100 h was 58.34% and 81.68%, respectively. LP-CSNPs could effectively improve the storage stability and had great antibacterial activity compared with unencapsulated litchi polyphenols.

Synthesis of Halopyrazole Matrine Derivatives and Their Insecticidal and Fungicidal Activities.

Matrine is a traditional botanical pesticide with a broad-spectrum biological activity that is widely applied in agriculture. Halopyrazole groups are successfully introduced to the C13 of matrine to synthesize eight new derivatives with a yield of 78-87%. The insecticidal activity results show that the introduction of halopyrazole groups can significantly improve the insecticidal activity of matrine on Plutella xylostella, Mythimna separata and Spodoptera frugiperda with a corrected mortality rate of 100%, which is 25-65% higher than matrine. The fungicidal activity results indicate that derivatives have a high inhibitory effect on Ceratobasidium cornigerum, Cibberella sanbinetti, Gibberrlla zeae and Collectot tichum gloeosporioides. Thereinto, 4-Cl-Pyr-Mat has the best result, with an inhibition rate of 23-33% higher than that of matrine. Therefore, the introduction of halogenated pyrazole groups can improve the agricultural activity of matrine.

Synthesis, characterization of two matrine derivatives and their cytotoxic effect on Sf9 cell of Spodoptera frugiperda.

The invasion of Spodoptera frugiperda has imposed a serious impact on global food security. Matrine is a botanical pesticide with a broad spectrum of insecticidal activity which was recommended for controlling Spodoptera frugiperda. In order to discover effective insecticide for Spodoptera frugiperda, two matrine derivatives modified with carbon disulfide and nitrogen-containing groups were systhesized. And their inhibition activities on Sf9 cell were evaluated. The structural configuration of compounds were characterized by IR, HPLC, MS, NMR and XRD, with yields of 52% and 65%, respectively. The IC50 of the two newly synthesized compounds on Sf9 cell reduced to 0.648 mmol/L and 1.13 mmol/L, respectively, compared with that of matrine (5.330 mmol/L). In addition, microscopic observation of Sf9 cell treated with the compounds showed that the number of adherent cells decreased, the cells shrunk, vacuolated and apoptotic bodies appeared. The two newly synthesized compounds exhibited better inhibitory effect on Sf9 cell than that of the parent matrine, suggesting that the positive effect of the introduction of 1-pyrrolidinecarbodithioate and diethylcarbamodithioate groups to matrine. The morphological observation of Sf9 cell induced by derivatives indicated that apoptosis induction may be a mechanism that inhibits insect cell proliferation and exerts insecticidal effect.

Synthesis, characterization and in vitro biological evaluation of two matrine derivatives.

Matrine is a traditional Chinese medicine and botanical pesticide with broad biological activities, including pharmacological and agricultural activities. In present work, two matrine derivatives have been successfully synthesized via introducing indole and cyclohexylamino to 13 position of matrine, respectively, with sophocarpine as starting material, and structurally characterized via infrared spectroscopy(IR), MS, 1 H NMR, 13 C NMR and X-ray crystal diffraction. The results of the in vitro biological activity tests showed that these two matrine derivatives exhibited even better activities against human cancer cells Hela229 and insect cell line Sf9 from Spodoptera frugiperda (J. E. Smith) than that of parent matrine, suggesting that the heterocyclic or cyclic group can dramatically increase the biological activity of matrine. It is worth to mention that 13-indole-matrine could possibly inhibit the growth of insect cells or human cancer cells by inducing cell apoptosis. The results of the present study provide useful information for further structural modifications of these compounds and for exploring new, potent anti-cancer agents and environment friendly pesticides.

[Hhigh-frequency ultrasound research on the normal adult sciatic nerve].

OBJECTIVE: To explore the application value of the high-frequency ultrasound examination of the normal adult sciatic nerve. METHODS: The high frequency ultrasound was used to examine 60 cases ,a total of 120 normal adult sciatic nerve (28 males and 32 females ranging in age from 19 to 38 years old, averaged 23.8 years old). The age between men and women, height and weight showed no significant difference. The cross-sectional scanning and longitudinal scanning, if necessary, Panoramic Imaging were conducted. The cross section area of sciatic nerve was measured at the hip line, the middle of the thigh, the edge of the popliteal fossa, and the relationship betwen the sciatic nerve and surrounding muscle group was observed in each cross-section. Probe was rotated 90 degree to display the long axis of sciatic nerve, to get the longitudinal section along the long axis from top to bottom. So the sciatic nerve in the vertical axis and the surrouunding muscles was displayed by above method combined with panoramic imaging. The data of coss-sectional area of sciatic nerve were obtained at the central of hip line, the middle of the thigh, the edge of the popliteal fossa, and then were divided into different groups by gender and sides to do statistical analysis. RESULTS: The applicatic nerve in thigh can be clearly displayed by high-frequency ultrasound in this group of 60 people with 120 nerves, but low display rate of sciatic nerve in hip, approximatley 31.4% (21/66). The longitudinal section of the sciatic nerve displayed as the banded isoechoic or slightly hyperechoic, parallel partial hyperechoic line could be seen in it; in the cross-section, it showed a clear edge of the sieve-like isoechoic or slightly hyperechnie, which could be oval ,trapezoidal, triangular and irregular in shape; the sciatic nerve bad visible passive movement and shape change when muscle contracted. There were statistically significant differences of cross-sectional area of sciatic nerves at the hip line ,the middle of thigh and edge of the popliteal fossa between 56 sciatic nerves in 28 males and 64 sciatic nerves in 32 females (P< 0.05); but there were no significant differences between left and right sides (P>0.05). CONCLUSION: High frequency ultrasound can be used as the first choice of the sciatic nerve when an imaging method preferred.