Bioactive peptides of plant origin: distribution, functionality, and evidence of benefits in food and health.

The multiple functions of peptides released from proteins have immense potential in food and health. In the past few decades, research interest in bioactive peptides of plant origin has surged tremendously, and new plant-derived peptides are continually discovered with advances in extraction, purification, and characterization technology. Plant-derived peptides are mainly extracted from dicot plants possessing bioactive functions, including antioxidant, cholesterol-lowering, and antihypertensive activities. Although the distinct functions are said to depend on the composition and structure of amino acids, the practical or industrial application of plant-derived peptides with bioactive features is still a long way off. In summary, the present review mainly focuses on the state-of-the-art extraction, separation, and analytical techniques, functional properties, mechanism of action, and clinical study of plant-derived peptides. Special emphasis has been placed on the necessity of more pre-clinical and clinical trials to authenticate the health claims of plant-derived peptides.

Variations of Flavone Glycosides Profile Underscore the Necessity of Quality Control of Prepared Microctis Folium Slices.

Microctis Folium (MF), the dried leaves of Microcos paniculata, is widely used as a medical and food dual-purpose herb in South-east Asia and China. However, the quality control of MF is not well studied. A simple and reliable quality control method was urgently needed for its growing usage. Herein, at first, its main active components were identified by UPLC-ESI-qTOF-MS, and a representative MF flavone glycosides profile consisting of ten compounds was illustrated, which is the most detailed one up to now. Successively, using vitexin as the reference substance, a novel QAMS method with HPLC for quantification of the ten identified flavone glycosides was developed and methodologically validated. Furthermore, making use of the abovementioned QAMS method, quantitative profiling of 21 batches of prepared MF slices collected from different hospital pharmacies were performed. As a result, the total contents of ten flavone glucosides and the content of specific compound showed obvious variations. Using the ten compounds' contents dataset, the 21 batches of samples were divided into two distinct clusters by HCA. In sum, our results indicated that it was of great importance to take quality control of prepared MF slices and we presented a robust and simple method for their quantitative determination, which should be beneficial for the quality control of MF and its derived products.

[Oral absorption of asiatic acid nanoparticles modified with PEG].

A solvent diffusion method was used to prepare pegylated asiatic acid (AA) loaded nanostructured lipid carriers (p-AA-NLC), and the ligated intestinal circulation model was established to observe the absorption and distribution in small intestine. The concentration of AA in bile after oral administration of p-AA-NLC was detected by HPLC in healthy SD rats to indirectly evaluate the oral absorption promoting effect of PEG-modified namoparticles. The results showed that the penetration of p-AA-NLC was enhanced significantly and the transport capacity was increased greatly in small intestinal after PEG modification. As compared with the normal nanoparticles (AA-NLC), the Cmax of the drug excretion was increased by 76%, the time to reach the peak (tmax ) was decreased and the elimination half-life t1/2 was doubled in the rats after oral administration of p-AA-NLC, and the AUC0→t was 1.5 times of the AA-NLC group, indicating that the oral bioavailability of AA-NLC was significantly improved by hydrophilic modification of PEG.

[Response surface method for optimization of asiatic acid nanoparticles modified with PEG and its enhancing effects on intestinal absorption].

A solvent diffusion method was used to prepare pegylated asiatic acid (AA) loaded nanostructured lipid carriers (p-AA-NLC). Then central composite design-response surface method was used to obtain optimum condition for preparation technology of p-AA-NLC, where PEG/lipid ratio was 8.0% and AA/lipid ratio was 22.0%. Under the optimum condition, the system had particle size of (111.2±2.9) nm, Zeta potential of (-37.1±0.9) mV, drug loading of (15.4±0.2)% and entrapment efficiency greater than 90%. The deviations between observed values and predicated values were all below 5%, indicating that the established model had a good predictability. Meanwhile, a low-speed single pass perfusion model of rat in situ was set up to estimate the absorption kinetics of p-AA-NLC in small intestine, where the effective permeability (Peff), absorption rate constant (Ka) and other parameters were used to evaluate the drug absorption. It turned out that Peff and Ka in p-AA-NLC group were significantly higher than those in unmodified group (P<0.05), indicating that asiatic acid loaded nanostructured lipid carriers (AA-NLC) could enhance the effects on intestinal absorption after being modified with hydrophilic PEG.

[Effects of Forsythia suspensa Volatile Oil Loaded Nanomicellar on Transdermal and Transmucosal Drug Delivery of Phillyrin in Vitro].

Objective: To prepare all components loaded liquid preparation of Forsythia suspensa( ACLL) by the technology of nanomicellar solubilization,and to investigate the effects of Forsythia suspensa volatile oil loaded nanomicellar on the transdermal and transmucosal drug delivery of phillyrin. Methods: The volatile oil and hydrosoluble components of Forsythia suspensa were obtained by double extraction synchronously,and the major components of volatile oil were determined by GC-MS. Then the ACLL prepared by the volatile oil was added to the aqueous solution in the form of nanomicellar. The characteristics of ACLL were evaluated by the TEM,PCS and CLSM. The amount of phillyrin( PN) was determined by HPLC system. The side-by-side diffusion cell was used to investigate the effects of Forsythia suspense volatile oil loaded nanomicellar on the PN transdermal and transmucosal drug delivery, with the hydrosoluble components loaded liquid( HCLL) used as control group. Results: The Forsythia suspense volatile oil was slight yellowish and transparent liquid with a fragrant odor,the major components as follows ß-pinene( 49. 01%),α-pinene( 15. 78%), ß-ocimene( 13. 79%),linalool( 5. 91%), α-thujene( 2. 07%), ß-geranene( 1. 91%),terpinolene( 1. 84%),etc. The Forsythia suspense volatile oil loaded nanomicellar had a closed spherical shape as the TEM and CLSM images appeared. The calculated mean size was 193. 3 nm,the Zeta potential values of- 83. 8 m V. During the whole experiment, the ACLL resulted in a remarkable enhancement of PN transdermal and transmucosal absorption compared with HCLL. At 7. 0 h, the accumulated permeation amount of PN from the ACLL was 2. 04 and 1. 16 folds than that of HCLL for transdermal and transmucosal absorption,respectively. Conclusion: The permeability of PN is obviously enhanced by Forsythia suspense volatile oil loaded nanomicellar for transdermal and transmucosal absorption, these results elucidate the advantages and the mechanism of pharmacological action of all components of traditional Chinese medicine.

Preparation of morusin from Ramulus mori and its effects on mice with transplanted H22 hepatocarcinoma.

In this study, we used branches Ramulus mori from cultivated mulberry Husang-32 (Morus multicaulis Perry) as the experimental material and anhydrous ethanol as the extraction solution to obtain the crude extract from the branch bark. The ethanolic extract was successively purified through a macroporous resin, Sephadex LH-20, and semipreparative reversed-phase high-performance liquid chromatography (RP-HPLC). The high-purity monomer was identified as morusin by HPLC with diode array detection (HPLC-DAD) and its UV spectrum. The contents of morusin exhibited almost no difference between the root and branch bark in Husang-32, and morusin was not detected in the leaves. Morusin is able to inhibit the tumor growth of transplanted H22 hepatocarcinoma in mice and has no side effects. The fluorescence quantitative real-time PCR (qRT-PCR) results indicate that morusin has a marked inhibitory effect on liver cancer cells through a mechanism that may be related increases in the expression of p53, Survivin, CyclinB1, and Caspase-3 and a decrease in NF-κ B gene expression. The influence of this compound is more apparent in the Caspase-3 and the NF-κ B genes.

[Effect of suyu capsule on behavior and injury of hippocampal neurons in depression model mice].

OBJECTIVE: To observe the effect of Suyu capsule on behavior, injury of hippocampal neurons and Ca2+ ion in hippocampal synaptic in the depression model mice. METHOD: Sixty male Kunming mice were randomly divided into 5 groups, the control group, the model group and three Suyu capsule groups (the doses were 22.8, 11.4, 5.7 g x kg(-1) respectively). The model was established by separation and chronic unpredictable mild stimulation. The increased weight and crossing score, rearing score were measured by open-field and sweet water consumption of mice. Cone cell and configuration of neuron in CA1, CA3 region of hippocampus were observed by Nissl. The concentration of hippocampal synaptic Ca2+ ion was detected by fluorimetry. RESULT: Comparing with the mice of control, the increased weight was slowered ( P < 0.01), the scores of rearing and crossing were decreased (P < 0.01), sweet water consumption were decreased too (P < 0.01), numbers of cone cell in CA3 region of hippocampus were decreased obviously (P < 0.01), and Ca2+ ion in hippocampal synaptic was increased obviously. Comparing with the mice of model, Suyu capsule (22.8 g kg(-1)) could increase the increased weight on the 14th and 21 st day obviously (P < 0.05); Suyu capsule (22.8 g x kg(-1)) could increase the scores of crossing obviously (P < 0.05), Suyu capsule (22.8, 11.4 g x kg(-1)) could increase the scores of rearing obviously (P < 0.01, P < 0.05); Suyu capsule (22.8, 11.4, 5.8 g x kg(-1)) could increase sweet water consumption obviously (P < 0.01, P < 0.05, P < 0.05; Suyu capsule (22.8, 11.4, 5.8 g x kg(-1)) could increase numbers of cone cell in CA3 region of hippocampus obviously (P < 0.01, P < 0.05, P < 0.05); Suyu capsule (22.8, 11.4, 5.8 g x kg(-1)) decreased Ca2+ ion in hippocampal synaptic with dose-effect relationship (P < 0.01, P < 0.01, P < 0.05). CONCLUSION: Suyu capsule can improve all the symptoms of the depression model mice and protect injury of hippocampal neurons in the depression model mice. The possible mechanism of action is to restrict Ca2+ ion overfreight.