Phytochemical Profile of Alkaloid Extract from Dendrobium huoshanense and Inhibitory Effects against Oxidative Stress in H2 O2 -Induced PC12 Cells.

This study aimed to explore the alkaloid profile of Dendrobium huoshanense and determine the potential protective effect against oxidative damage. The crude D. huoshanense alkaloid extract (DHAE) was obtained by 70 % ethanol extraction and liquid-liquid partition. DHAE contained specific alkaloid components with abundant 6-hydroxynobiline (58.15 %) and trace dendrobine (3.23 %) in the preliminary HPLC fingerprint and GC-MS analysis, which was distinguished from D. officinale or D. nobile. Subsequently, six alkaloids including 6-hydroxynobiline, 2-hydroxy dendrobine, nobilonine, dendrobine, Findlayines D and trans-dendrochrysanine were identified in the purified DHAE (namely DHSAE-3, DHSAE-3') via further solid phase extraction coupled with UPLC-MS/MS analysis. Meanwhile, pretreatment with DHAE or DHSAE (0.5, 5 µg/mL) increased cell viability by 14.0-57.4 % compared to that of H2 O2 -induced PC12 Model cells. Among them, 5 µg/mL DHSAE-3-treated cells displayed a pronounced reversion than the positive vitamin E (p<0.01). Furthermore, a clear cellular morphological restoration and 38.4 % reduction in intracellular reactive oxidative species level were achieved. Our findings suggest that D. huoshanense has a characteristic alkaloid profile represented by abundant 6-hydroxynobiline, and DHAEs exhibit obvious protection against oxidative neuronal damage. Overall, this study indicates that DHAEs might be used to inhibit oxidative stress and provide a source to develop novel neuroprotective drugs.

A comparative study of pectic polysaccharides from fresh and dried Dendrobium officinale based on their structural properties and hepatoprotection in alcoholic liver damaged mice.

In this study, two pectic polysaccharides from fresh and dried Dendrobium officinale, namely FDP and DDP, were obtained by sour-water extraction, ethanol precipitation and further purification with DEAE cellulose-52 and Sephadex G-100 column chromatography. FDP/DDP had eight similar glycosidic linkages including 1,4-linked-GlcAp, 1,4- and 1,3,4-linked-GalAp, 1,3,4- and T-linked-Glcp, 1,6- and T-linked-Galp, T-linked-Galp and T-linked-Xylp. Besides, FDP was marked by 1,6-, 1,2,6-linked-Manp and 1,2,4-, 1,2-linked-Rhap, and DDP consisted of unique 1,6-linked-GlcAp and 1,3,6-Manp. FDP with a molecular weight of 14.8 kDa generally showed stronger scavenging capacity against DPPH, ABTS and hydroxyl radicals than DDP (p < 0.05). Pretreatment with FDP/DDP alleviated the alcohol-induced liver injury in mice, and their serum aminotransferase and triglyceride levels were 10.3%-57.8% lower than those of the model group (MG). Meanwhile, the FDP/DDP-M and FDP/DDP-H groups (200 and 300 mg kg-1) displayed a remarkable increase in antioxidant enzyme activities and significant reduction in inflammatory cytokine levels in comparison with the MG. Further analysis revealed that FDP-treated mice generally exhibited lower transaminase levels and inflammatory cytokine expression as well as higher antioxidant enzyme activities than DDP-treated ones. The FDP-H group showed significant restoration, which was slightly less than or almost comparable to that of the bifendate-fed positive control. The above results indicate that D. officinale pectin can attenuate oxidative stress and inflammatory cytokine response, and ultimately ameliorate liver injury, and "fresh" pectin with specific structural characteristics is expected to be more promising as hepatoprotective food.

Preparation, characterization, antioxidant and anti-inflammatory activities of acid-soluble pectin from okra (Abelmoschus esculentus L.).

Currently, there are few studies on acid-soluble pectin from okra, especially in biological activity for antioxidant and anti-inflammatory. In this study, the antioxidant properties of acid-soluble okra pectin components and their anti-inflammatory were explored. Firstly, two acid-soluble okra pectic fractions, namely crude acid-soluble okra pectin (CAOP) and acid-soluble okra pectin (AOP), were obtained and exhibited structural and compositional variation. The two pectic fractions contained a low degree of esterification (42.0-46.5%) and a relatively high uronic acid content (31.6-37.3%). AOP was composed of galacturonic acid (79.1 mol/%), galactose (4.3 mol/%), rhamnose (14.5 mol/%) and xylose (2.1 mol/%), and the molecular weight was 92.8 kDa. Morphological and thermal properties of acid-soluble okra pectin components were also investigated. Compared to CAOP, AOP expressed better antioxidant activity, and suppressed the NO production in LPS-induced RAW 264.7 macrophages. All the above results indicated that AOP had the potential to act as a natural antioxidant or a functional anti-inflammatory food, which would broaden the development and utilization of okra resources.

Okra pectin relieves inflammatory response and protects damaged intestinal barrier in caerulein-induced acute pancreatic model.

BACKGROUND: Protecting the intestinal mucosa from being destroyed helps reduce the inflammation caused by acute pancreatitis (AP). In this study, whether okra pectin (OP) could attenuate the inflammation of AP through protecting the intestinal barrier was investigated. RESULTS: OP was obtained from crude okra pectin (COP) through the purification by DEAE cellulose 52 column. Supplementation with OP or COP in advance reduced the severity of AP, as revealed by lower serum amylase and lipase levels, abated pancreatic edema, attenuated myeloperoxidase activity and pancreas histology. OP or COP inhibited the production of pancreatic proinflammatory cytokines, including tumor necrosis factor-α and interleukin-6. In addition, the upregulation of AP-related proteins including ZO-1, occludin, the antibacterial peptide-defensin-1 (DEFB1) and cathelicidin-related antimicrobial peptide (CRAMP), as well as the histological examination of colon injuries, demonstrated that OP or COP provision could effectively maintain intestinal barrier function. Ultimately, dietary OP or COP supplementation could inhibit AP-induced intestinal inflammation. For the above, the effect of OP was better than COP. CONCLUSION: Dietary OP supplementation could be considered as a preventive method that effectively interferes with intestinal damage and attenuates inflammatory responses trigged by AP. © 2020 Society of Chemical Industry.

Two macamide extracts relieve physical fatigue by attenuating muscle damage in mice.

BACKGROUND: Macamides, the main active components contained in maca, have attracted increasing attention due to their various bioactivities. In this study, crude macamide extract (CME) and purified macamide extract (PME) were prepared by enzyme-assisted extraction and macroporous resin separation, and the anti-fatigue effects of CME and PME were evaluated in a forced swimming model. RESULTS: The composition analysis results revealed that both CME and PME mainly contain eight kinds of macamide. Based on the results of a weight-loaded forced swimming test, compared with a control group, CME and and PME groups could prolong exhaustive swimming time, increase levels of liver glycogen (LG) and muscle glycogen (MG), accelerate fatty acid oxidation in serum to provide energy, eliminate the accumulation of blood lactic acid (BLA) and blood urea nitrogen (BUN), and decrease the serum biomarkers for muscle damage, such as lactate dehydrogenase (LDH) and creatine kinase (CK). Histological analysis also indicated that CME and PME attenuated damage to skeletal muscle and the myocardium in mice during exercise. CONCLUSION: Two macamide extracts have a beneficial effect on relieving physical fatigue by attenuating the damage of skeletal muscle and myocardium during exercise, and a better effect was observed in the PME group. © 2018 Society of Chemical Industry.

Optimization on conditions of podophyllotoxin-loaded liposomes using response surface methodology and its activity on PC3 cells.

The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106 nm and a zeta potential of -10.1 mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24 h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.

Purification, characterization and anti-fatigue activity of polysaccharide fractions from okra (Abelmoschus esculentus (L.) Moench).

The aim of this study was to investigate the anti-fatigue activity of polysaccharide fractions from Abelmoschus esculentus (L.) Moench (AE) in mice. After crude polysaccharide (CAEP) was extracted from AE and purified by DEAE cellulose-52 column, two polysaccharide fractions (AEP-1 and AEP-2) were obtained. The structural analysis suggested that AEP-1 and AEP-2 were a RG-I polysaccharide and an AG-II polysaccharide, respectively. According to the results of the weight-loaded swimming test, compared with the negative control group, the CAEP, AEP-1 and AEP-2 treatment groups could prolong the swimming time, decrease serum urea nitrogen (SUN) and blood lactic acid (BLA), and increase hepatic glycogen (HG) and muscle glycogen (MG), which indicated that okra polysaccharides have an effective anti-fatigue activity. Furthermore, our study exhibited the anti-fatigue mechanism of okra polysaccharide was correlated with retarding the accumulation of creatine kinase (CK) and lactate dehydrogenase (LDH) in serum, and enhancing succinate dehydrogenase (SDH), adenosine triphosphate (ATP) and adenosine triphosphatase (ATPase) levels. In addition, the anti-fatigue activity of AEP-1 was stronger than that of AEP-2, and significantly better than that of CAEP. Therefore, AEP-1 and AEP-2 may be the main active anti-fatigue functional substances of AE.

Synthesis, in silico and in vivo blood brain barrier permeability of ginkgolide B cinnamate.

Ginkgolide B, one of the important components of Ginkgo biloba extracts, has been revealed to exhibit great potential in therapy of cerebrovascular diseases. However the lack of permeability greatly limited it from further clinical application. Based on the prediction model for blood brain barrier (BBB) permeation, herein a potential brain-targeting analog ginkgolide B cinnamate (GBC) was successfully synthesized and characterized. After intravenous administration of GBC or GB, liquid chromatography tandem mass spectrometry (LC-MS/MS) was conducted to determine the analog in rat plasma and brain. The results showed that GBC had a significant increase in BBB permeability. A significant 1.61-times increase in half-life was observed for GBC and the drug targeting index (DTI) value was calculated to be 9.91. The experiment results matched well with the predicted one, which revealed that BBB permeability prediction model combined with in vivo study could be used as a quick, feasible and efficient tool for brain-targeting drug design.