Identification and characterization of shark VNARs targeting the Helicobacter pylori adhesin HpaA.

Helicobacter pylori (H. pylori) is recognized as a pathogen associated with several gastrointestinal diseases. The current treatments exhibit numerous drawbacks, including antibiotic resistance. H. pylori can adhere to and colonize the gastric mucosa through H. pylori adhesin A (HpaA), and antibodies against HpaA may be an effective therapeutic approach. The variable domain of immunoglobulin new antigen receptor (VNAR) is a novel type of single-domain antibody with a small size, good stability, and easy manufacturability. This study isolated VNARs against HpaA from an immune shark VNAR phage display library. The VNARs can bind both recombinant and native HpaA proteins. The VNARs, 2A2 and 3D6, showed high binding affinities to HpaA with different epitopes. Furthermore, homodimeric bivalent VNARs, biNb-2A2 and biNb-3D6, were constructed to enhance the binding affinity. The biNb-2A2 and biNb-3D6 had excellent stability at gastrointestinal pH conditions. Finally, a sandwich ELISA assay was developed to quantify the HpaA protein using BiNb-2A2 as the capture antibody and BiNb-3D6 as the detection antibody. This study provides a potential foundation for novel alternative approaches to treatment or diagnostics applications of H. pylori infection.

A novel shark single-domain antibody targeting OGT as a tool for detection and intracellular localization.

Introduction: O-GlcNAcylation is a type of reversible post-translational modification on Ser/Thr residues of intracellular proteins in eukaryotic cells, which is generated by the sole O-GlcNAc transferase (OGT) and removed by O-GlcNAcase (OGA). Thousands of proteins, that are involved in various physiological and pathological processes, have been found to be O-GlcNAcylated. However, due to the lack of favorable tools, studies of the O-GlcNAcylation and OGT were impeded. Immunoglobulin new antigen receptor (IgNAR) derived from shark is attractive to research tools, diagnosis and therapeutics. The variable domain of IgNARs (VNARs) have several advantages, such as small size, good stability, low-cost manufacture, and peculiar paratope structure. Methods: We obtained shark single domain antibodies targeting OGT by shark immunization, phage display library construction and panning. ELISA and BIACORE were used to assess the affinity of the antibodies to the antigen and three shark single-domain antibodies with high affinity were successfully screened. The three antibodies were assessed for intracellular function by flow cytometry and immunofluorescence co-localization. Results: In this study, three anti-OGT VNARs (2D9, 3F7 and 4G2) were obtained by phage display panning. The affinity values were measured using surface plasmon resonance (SPR) that 2D9, 3F7 and 4G2 bound to OGT with KD values of 35.5 nM, 53.4 nM and 89.7 nM, respectively. Then, the VNARs were biotinylated and used for the detection and localization of OGT by ELISA, flow cytometry and immunofluorescence. 2D9, 3F7 and 4G2 were exhibited the EC50 values of 102.1 nM, 40.75 nM and 120.7 nM respectively. VNAR 3F7 was predicted to bind the amino acid residues of Ser375, Phe377, Cys379 and Tyr 380 on OGT. Discussion: Our results show that shark single-domain antibodies targeting OGT can be used for in vitro detection and intracellular co-localization of OGT, providing a powerful tool for the study of OGT and O-GlcNAcylation.

Notoginsenoside R1: A systematic review of its pharmacological properties.

Notoginsenoside R1 is one of major bioactive compounds extracted from Panax notoginseng (Burk.) dry roots and rhizomes of F.H. Chen, which has been increasingly used for enhancing cognition and physical health worldwide. The objective of this study was to review the pharmacological effects of notoginsenoside R1 in a systematic manner. We performed searches on databases including MEDLINE (Pubmed), Google Scholar and Web of Science, the System for Information on to select the original research publications reporting the biological and pharmacological effects of notoginsenoside R1 from in vitro and in vivo studies regardless of publication language and study design. Notoginsenoside R1 exhibited potent characteristics of neuroprotective, anti-inflammatory, anti-apoptosis and anti-ischemia-reperfusion injury properties etc. The cytotoxic effects of notoginsenoside R1 were dependent on different types of cell lines. Other pharmacological effects including accumulation of lipopolysac chaired-induced microcirculation, endothelial injury, hypoxia-reoxygenation injury effects have been mentioned, but the results were considerably diverged. A higher quality of evidence on clinical trial studies is highly recommended to confirm the efficacy of notoginsenoside R1.

Anti-exercise-fatigue and promotion of sexual interest activity of total flavonoids from wasps drone-pupae in male mice.

The aim of this research was to evaluate the anti-exercise-fatigue and promotion of sexual interest of total flavonoids from drone pupae of wasps. DPTF was prepared by ethanol extracting and its extraction conditions were optimized by response surface methodology. Then, anti-exercise-fatigue and promotion of sexual interest of DPTF were evaluated. The optimums extraction conditions by RSM were ethanol concentration 65%, extraction time 3 h and solid-to-liquid 20:1(mL/g). No mortality and general symptoms of toxicity were observed in the DPTF treated mice(1 g/kg,3 g/kg,5 g/kg body weight) the body weight and food consumption were not significantly changed compared with the normal control group. The relative weights of main organ did not markedly change. DPTF can significantly extend the duration of the swimming time to exhaustion and the times of capture the female in mice, decrease BUN, LAC and Cr levels, increase LG, GG and T activities in the DPTF treated mice. The dose of 5 g/kg body weight is the optimal dose for anti-exercise-fatigue activity and promotion of sexual interest in male mice. In conclusion, DPTF is promising traditional natural-based therapeutic remedy for relieving exercise-fatigue with high safety.

Structure Properties, Acquisition Protocols, and Biological Activities of Oleuropein Aglycone.

Oleuropein aglycone, which is the major phenolic component of extra virgin olive oil, is gaining popularity and importance in scientific and public communities. This paper summarizes the structure properties, acquisition protocols, and biological activities of oleuropein aglycone. There are three hydrolytic methods used to obtain oleuropein aglycone from oleuropein-enzymatic hydrolysis, acid hydrolysis, and acetal hydrolysis. Enzymatic hydrolysis can be achieved with exogenous enzymes and endogenous enzymes. In addition, the diverse pharmacological effects of oleuropein aglycone are summaried. These pharmacological effects include anti-Alzheimer's disease, anti-breast cancer, anti-inflammatory, anti-hyperglycemic, anti-oxidative, and lipid-lowering properties. Therefore, we can use hydrolysis and biological activities to study oleuropein aglycone in the future.

The Potential of Using Bee Pollen in Cosmetics: a Review.

During ancient times in China, bee pollen was used for skin whitening and beauty. Around 70% of substances in bee pollen are biologically active, such as proteins, carbohydrates, lipids and fatty acids, phenolic compounds, vitamins and bioelements.This review describes the cosmeceutical properties of bee pollen and the mechanism of its active components action, its beneficial influence on human skin. As a natural bee product, bee pollen may effectively enhance protective mechanisms against skin aging, skin dryness, ultraviolet B radiation, oxidative damage, inflammatory and melanogenesis, which are involved in a wide range of negative effects on human skin, thus they have attracted attention for health and cosmetic applications.

Maca Cosmetics: A Review on Constituents, Therapeutics and Advantages.

Herbal cosmetics are the focus of attention nowadays, they have various therapeutics, including, anti-oxidant, anti-radiation, anti-aging, anti-inflammatory. Maca contains polysaccharides, phenolics, alkaloids, minerals and amino acids, which is said to suitable component for cosmetics due to the single action or synergy action. The review summarized the existed and potential therapeutic effects of maca ingredients in cosmetics. And compared to the marketed cosmetics, maca cosmetics have the merits of mild, low-toxicity and the clear relationship efficacy.

Ginsenosides: A Potential Neuroprotective Agent.

Ginseng is a traditional Chinese medicine with a wide range of pharmacological activities. Ginsenosides are the major constituents of ginseng. Ginsenosides have the unique biological activity and medicinal value, such as antitumor, anti-inflammatory, antioxidation, and inhibition of cell apoptosis. With the increase of stress in life, the incidence of nervous system diseases is also increasing. Neurological diseases pose a huge burden on people's life and health. In recent years, some studies have shown that ginsenosides have a certain role in the prevention and treatment of neurological diseases. However, the research is still in its infancy, and the relevant mechanisms are complex. In the paper, we review the effects and mechanisms of ginsenosides on epilepsy, depression, cerebral ischemia reperfusion injury, Alzheimer's disease, and Parkinson's disease. We hope to provide a theoretical basis for the treatment of nervous system diseases by ginsenosides.

A Review: The Bioactivities and Pharmacological Applications of Polygonatum sibiricum polysaccharides.

Traditional Chinese Medicine (TCM) has been widely used in China and is regarded as the most important therapeutic. Polygonatum sibiricum (PS), a natural plant used in traditional Chinese medicine, has various functions associated with a number of its components. There are many compositions in PS including polysaccharides, steroids, anthraquinone, alkaloids, cardiac glycosides, lignin, vitamins, various acids, and so on. Of these, polysaccharides play a significant role in PS-based therapeutics. This article summarizes Polygonatum sibiricum polysaccharides (PSP) have many pharmacological applications and biological activities, such as their antioxidant activity, anti-aging activity, an anti-fatigue effect, immunity enhancement effect, antibacterial effect, anti-inflammatory effect, hypolipidemic and antiatherosclerotic effects, anti-osteoporosis effect, liver protection, treatment of diabetes mellitus (DM), anti-cancer effect, and may help prevent Alzheimer's disease, and so on. This review summarized the extraction method, purification method, compositions, pharmacological applications, biological activities, biosynthesis, and prospects of PSP, providing a basis for further study of PS and PSP.

Maca polysaccharides: Extraction optimization, structural features and anti-fatigue activities.

The maca polysaccharides optimal extraction conditions were obtained by using response surface methodology (RSM) method and the anti-fatigue activity of maca polysaccharides (MCP) was explored. The maca polysaccharides extract yield of RSM could reach 9.97 mg/g by using the model predicts, and the total sugar and protein purity were 61.00% and 4.46% with the further isolation process, respectively. And the monosaccharide compositions obtained by gas chromatograph (GC) were composed of rhamnose (rha), glucose (glc), galactose (gal) with the ratio of 2.34:10.21:1.00. Furthermore, the anti-fatigue activity was evaluated by the swimming parameter, biochemistry parameters (liver glycogen (LG), blood urea nitrogen (BUN), and lactic acid (LD)), the result indicated that the low-dose maca polysaccharides group had the significant anti-fatigue activity.

Yield enhancement strategies of rare pharmaceutical metabolites from endophytes.

Endophytes are barely untapped as vital sources in the medicine. They are microorganisms which mostly exist in plants. As they are exploited, it is accepted that endophytes can produce active metabolites that possess same function as their hosts such as taxol, podophyllotoxin, hypericin, and azadirachtin. These metabolites have been promising potential usefulness in safety and human health concerns. We are supposed to adopt measures to raise production for the low yield of metabolites. This paper summarizes the latest advances in various bioprocess optimization strategies. These techniques can overcome the limitations associated with rare pharmaceutical metabolite-producing endophytic fungi. These strategies include strain improvement, genome shuffling, medium optimization, fermentation conditions optimization, addition of specific factor, addition of solid sorbent, and co-culturing. It will enable endophytes to produce high and sustainable production of rare pharmaceutical metabolites.

Maca polysaccharides: A review of compositions, isolation, therapeutics and prospects.

Maca polysaccharides, some of the major bioactive substances in Lepidium meyenii (Walp.) (Maca), have various biological properties, including anti-oxidant, anti-fatigue, anti-tumor, and immunomodulatory effects, as well as hepatoprotective activity and regulation function. Although many therapeutics depend on multiple structures of maca polysaccharides in addition to providing sufficient foundations for maca polysaccharide products in industrial applications, the relationships between the pharmacological effects and structures have not been established. Therefore, this article summarizes the extraction and purification methods, compositions, pharmacological effects, prospects and industrial applications of maca polysaccharides.

Optimization of Submerged Fermentation Medium for Matrine Production by Aspergillus terreus, an Endophytic Fungus Harboring Seeds of Sophora flavescens, Using Response Surface Methodology.

Different endophytes isolated from the seeds of Sophora flavescens were tested for their ability to produce matrine production. Response surface methodology (RSM) was applied to optimize the medium components for the endophytic fungus. Results indicated that endophyte Aspergillus terreus had the ability to produce matrine. The single factor tests demonstrated that potato starch was the best carbon source and the combination of peptone and NH4NO3 was the optimal nitrogen source for A. terreus. The model of RSM predicted to gain the maximal matrine production at 20.67 µg/L, when the potato starch was 160.68 g/L, peptone was 24.96 g/L and NH4NO3 was 2.11 g/L. When cultured in the optimal medium, the matrine yield was an average of 20.63 ± 0.11 µg/L, which was consistent with the model prediction. This study offered an alternative source for the matrine production by endophytic fungus fermentation and may have far-reaching prospect and value.

Study on Transformation of Ginsenosides in Different Methods.

Ginseng is a traditional Chinese medicine and has the extensive pharmacological activity. Ginsenosides are the major constituent in ginseng and have the unique biological activity and medicinal value. Ginsenosides have the good effects on antitumor, anti-inflammatory, antioxidative and inhibition of the cell apoptosis. Studies have showed that the major ginsenosides could be converted into rare ginsenosides, which played a significant role in exerting pharmacological activity. However, the contents of some rare ginsenosides are very little. So it is very important to find the effective way to translate the main ginsenosides to rare ginsenosides. In order to provide the theoretical foundation for the transformation of ginsenoside in vitro, in this paper, many methods of the transformation of ginsenoside were summarized, mainly including physical methods, chemical methods, and biotransformation methods.