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Triterpenoid saponins are structurally diverse secondary metabolites. They are the main active ingredient of many medicinal plants and have a wide range of pharmacological effects. Traditional production of triterpenoid saponins, directly extracted from cultivated plants, cannot meet the rapidly growing demand of pharmaceutical industry. Microorganisms with triterpenoid saponins production ability (especially Agrobacterium genus) and biotransformation ability, such as fungal species in Armillaria and Aspergillus genera and bacterial species in Bacillus and Intestinal microflora, represent a valuable source of active metabolites. With the development of synthetic biology, engineering microorganisms acquired more potential in terms of triterpenoid saponins production. This review focusses on potential mechanisms and the high yield strategies of microorganisms with inherent production or biotransformation ability of triterpenoid saponins. Advances in the engineering of microorganisms, such as Saccharomyces cerevisiae, Yarrowia lipolytica, and Escherichia coli, for the biosynthesis triterpenoid saponins de novo have also been reported. Strategies to increase the yield of triterpenoid saponins in engineering microorganisms are summarized following four aspects, that is, introduction of high efficient gene, optimization of enzyme activity, enhancement of metabolic flux to target compounds, and optimization of fermentation conditions. Furthermore, the challenges and future directions for improving the yield of triterpenoid saponins biosynthesis in engineering microorganisms are discussed.

The aim of this study was to investigate the anti-fatigue activity of Chinese Yam polysaccharides (CYPs). The structural characterization of CYPs was conducted using Fourier transform-infrared spectroscopy, nuclear magnetic resonance spectroscopy, gel permeation chromatography-light scattering-refractive index, and ion chromatography. The weight-loaded swimming capability, behavior performance, tumor growth, content of adenosine triphosphate (ATP), and biochemical markers of CYP in a cancer-related fatigue mouse model were tested. The results showed that CYP is a mixture with an average Mw of 75.57 kDa and is mainly composed of rhamnose, glucuronic acid, glucose, galactose, and arabinose with a molar ratio of 0.01 : 0.06 : 1.00 : 0.17 : 0.01. CYP increased the exhausting swimming time, which was decreased in the cisplatin (DDP) control group and the model group. CYP also increased the content of ATP in musculus gastrocnemius, which was down-regulated by DDP; the DDP had significantly enhanced the contents of interleukin-1β (IL-lβ), malondialdehyde (MDA), blood urea nitrogen (BUN) and lactic dehydrogenase (LDH) and inhibited the activity of superoxide dismutase (SOD) in the muscle. Administration of CYP decreased the levels of IL-lβ, MDA, BUN and LDH, and up-regulated the SOD activity. The DDP + CYP group presented a decreased tumor volume and a lower tumor weight as compared with the model group. Moreover, the mice in the CYP or DDP + CYP groups had heavier body weights than the mice in the model group and DDP group. These results suggest that CYP should improve cancer-related fatigue via the regulation of inflammatory responses, oxidative stress and increase in energy supplementation.

Objective Fusarium oxysporum is a common pathogenic fungus in ginseng cultivation. Both pathogens and antagonistic fungi have been reported to induce plant resistance responses, thereby promoting the accumulation of secondary metabolites. The purpose of this experiment is to compare the advantages of one of the two fungi, in order to screen out more effective elicitors. The mechanism of fungal elicitor-induced plant resistance response is supplemented. Methods A gradient dilution and the dural culture were carried out to screen strains. The test strain was identified by morphology and 18 s rDNA. The effect of different concentrations (0, 50, 100, 200, 400 mg/L) of Penicillium sp. YJM-2013 and F. oxysporum on fresh weight and ginsenosides accumulation were tested. Signal molecules transduction, expression of transcription factors and functional genes were investigated to study the induction mechanism of fungal elicitors. Results Antagonistic fungi of F. oxysporum was identified as Penicillium sp. YJM-2013, which reduced root biomass. The total ginsenosides content of Panax ginseng adventitious roots reached the maximum (48.95 ± 0.97 mg/g) treated with Penicillium sp. YJM-2013 at 200 mg/L, higher than control by 2.59-fold, in which protopanoxadiol-type ginsenosides (PPD) were increased by 4.57 times. Moreover, Penicillium sp. YJM-2013 activated defense signaling molecules, up-regulated the expression of PgWRKY 1, 2, 3, 5, 7, 9 and functional genes in ginsenosides synthesis. Conclusion Compared with the pathogenic fungi F. oxysporum, antagonistic fungi Penicillium sp. YJM-2013 was more conducive to the accumulation of ginsenosides in P. ginseng adventitious roots. Penicillium sp. YJM-2013 promoted the accumulation of ginsenosides by intensifying the generation of signal molecules, activating the expression of transcription factors and functional genes.

A biosimilar needs to demonstrate its similarity to the originator reference product (RP) in terms of structural and functional properties as well as nonclinical and clinical outcomes. The aim was to assess the analytical similarity between the trastuzumab biosimilar HLX02 and Europe-sourced Herceptin® (EU-Herceptin®) and China-sourced Herceptin® (CN-Herceptin®) following a quality-by-design (QbD) quality study and tier-based quality attribute evaluation. A panel of highly sensitive and orthogonal methods, including a novel Fc gamma receptor IIIa (FcγRIIIa) affinity chromatography technique that enables quantitative comparison of glycan effects on effector function, was developed for the assessment. To ensure the full product variability was captured, ten batches of HLX02 were compared with 39 RP batches with expiry dates from August 2017 to March 2021. The extensive three-way similarity assessment demonstrated that HLX02 is highly similar to the RPs. Furthermore, the %afucose, %galactose, and FcγRIIIa affinity of the RPs were observed to first decrease and then return to the original level in relation to their expiry dates, and the RP batches can be subgrouped by their FcγRIIIa affinity chromatograms. HLX02 is demonstrated to be more similar to the RPs of the high FcγRIIIa affinity group. Besides having an overall high analytical similarity to both EU-Herceptin® and CN-Herceptin®, HLX02 is more similar to Herceptin® with high FcγRIIIa affinity, a result that demonstrates the power of the novel FcγRIIIa affinity chromatography technology in biosimilarity evaluation.

A novel photocatalyst Tm3+/Yb3+–co-doped bismuth molybdate (Bi2MoO6) were synthesized via the hydrothermal method. The samples were characterized through X-ray diffraction, field emission scanning electron microscopy, transmission electron microscopy, X-ray photoelectron spectroscopy (XPS), UV-vis diffuse reflectance spectra, and photoluminescence. XPS characterization confirmed the doped rare earth elements. Analysis of the optical properties explained the up-conversion process and its effect on the photocatalytic performance. The as-synthesized samples were employed to decompose Rhodamine B to value its photocatalytic activities under visible light irradiation. The doped samples showed an enhanced photocatalytic activity compared with the bare Bi2MoO6. When the ratio of Tm3+ and Yb3+ was 0.5:5, the degradation efficiency was the highest of 96.1% within 25 min, which was higher than that (74.9%) of pure Bi2MoO6. Moreover, the photocatalytic mechanism of improving the photocatalytic properties was discussed. Besides, the sample showed a super stability in photocatalytic activity. A novel catalyst for industrial pollutant degradation was proposed.

Huashanshen dripping pill (HSS), a commonly used traditional Chinese medicine, has been widely used in China due to its properties of antiasthma, expectorant, and antitussive. However, it was less in-depth understanding of the chemical composition, their absorption in plasma and potential biological mechanism. In this research, ultra performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry was developed to simultaneously identify the chemical constituents and absorption in rat plasma after oral administration of HSS. IgE-sensitized to ovalbumin was induced in BALB/c mice. ELISA and molecular docking analysis were carried out to identify their antiasthmatic mechanisms. As a result, 11 compounds were tentatively characterized by comparing the retention time, ion fragments, and the accurate mass measurement of [M + H]+ ions in the HSS. Two alkaloids including d-anisodamine and l-anisodamine were identified in the rat plasma after oral administration of HSS. The pills alleviated airway inflammation in lung tissues, and inhibited IgE, IL-4, and IL-5 in the serum. Furthermore, there were several amino acid residues involved in anisodamine-targeting receptors of hydrogen bonds and hydrophobic interactions via molecular docking indication. All in all, anisodamine would be the main component in the HSS whose antiasthmatic effects based on the inhibition of IgE, IL-4, and IL-5 production.

The investigation of the constituents of the rhizomes of Dioscorea collettii afforded one new dihydroisocoumarin, named (−)-montroumarin (1a), along with five known compounds—montroumarin (1b), 1,1′-oxybis(2,4-di-tert-butylbenzene) (2), (3R)-3′-O-methylviolanone (3a), (3S)-3′-O-methylviolanone (3b), and (RS)-sativanone (4). Their structures were elucidated using extensive spectroscopic methods. To the best of our knowledge, compound 1a is a new enantiomer of compound 1b. The NMR data of compound 2 had been reported but its structure was erroneous. The structure of compound 2 was revised on the basis of a reinterpretation of its NMR data (1D and 2D) and the assignment of the 1H and 13C NMR data was given rightly for the first time. Compounds 3a–4, three dihydroisoflavones, were reported from the Dioscoreaceae family for the first time. The cytotoxic activities of all the compounds were tested against the NCI-H460 cell line. Two dihydroisocoumarins, compounds 1a and 1b, displayed moderate cytotoxic activities, while the other compounds showed no cytotoxicity.

Yiqi Fumai lyophilized injection (YQFM) is the recombination of Sheng mai san (SMS).YQFM has been applied clinically to efficaciously and safely treat chronic heart failure (CHF). However, the mechanism of YQFM is still not fully elucidated. The purpose of our study was to investigate the protective mechanism of YQFM against abdominal aortic coarctation (AAC) in rats by proteomic methods. After YQFM treatment, the cardiac function were obviously meliorated. One hundred and fifty-seven important differentially expressed proteins (DEPs) were identified, including 109 in model rat compared with that in control rat (M:C) and 48 in YQFM-treated rat compared with that in model rat (T:M) by iTRAQ technology to analyze the proteomic characteristics of heart tissue. Bioinformatics analysis showed that DEPs was mainly involved in the body’s energy metabolism and was closely related to oxidative phosphorylation. YQFM had also displayed efficient mitochondrial dysfunction alleviation properties in hydrogen peroxide (H2O2)-induced cardiomyocyte damage by Transmission Electron Microscope (TEM), Metabolic assay, and Mitotracker staining. What’s more, the levels of total cardiomyocyte apoptosis were markedly reduced following YQFM treatment. Furthermore, Western blot analysis showed that the expressions of peroxisome proliferator activated receptor co-activator-1α(PGC-1α) (p < 0.01 or p < 0.001), perixisome proliferation-activated receptor alpha (PPAR-α) (p < 0.001)and retinoid X receptor alpha (RXR-α) were upregulated (p < 0.001), PGC-1α as well as its downstream effectors were also found to be upregulated in cardiomyocytes after YQFM treatment(p < 0.001).These results provided evidence that YQFM could enhance mitochondrial function of cardiomyocytes to play a role in the treatment of CHF by regulating mitochondrial biogenesis-related proteins.

Contents of total flavonoids (TFc), total phenolics (TPc), and total crude polysaccharide (TCPc) in licorice from different origins were determined by optimized colorimetric methods, whereas five monomer ingredients (liquiritin [LQ], isoliquiritin [ILQ], liquiritigenin [LQG], isoliquiritigenin [ILQG], and glycyrrhizic acid [GA]) were simultaneously identified and quantified by HPLC-MS and HPLC. The results indicated that the contents of chemical compounds in licorice showed significant difference in different origins. Hierarchical cluster analysis and principal component analysis further proved that producing area indeed affected the quality including compounds and pharmacological activity in licorice. Licorice from Inner Mongolia exhibited the excellent DPPH assay, whereas samples from Gansu and Xinjiang showed high scavenging capacity to OH and ABTS free radicals. Meanwhile, α-Glu inhibitory activity of licorice samples was four times higher than the antioxidant activity. Correlation analysis made clear that TFc and TCPc both strongly contribute to DPPH scavenge capacity at P < 0.01 level, whereas TCPc contributed to α-Glu inhibitory activity at P < 0.05 level. This study would contribute to the comprehensive quality evaluation based on the compounds and pharmacological activity of licorice, and provide a reference for the choice of producing area to ensure the quality of licorice as a medicine.

Inflammatory bowel disease (IBD) is a long-term chronic disease, about 20% of IBD patients deteriorate to colorectal cancer. Currently, there is no radical cure for IBD. Natural plant polysaccharides (NPP) have low toxic and side effects, which have immune and prebiotic activities and possesses positive effect on alleviating IBD. In this review, we will focus on the alleviating effect of NPP on IBD in vitro and in vivo from three aspects: regulating intestinal flora imbalance, repairing intestinal barrier injury and improving immunity. The relationship between the chemical structure of natural plant polysaccharides and the therapeutic effect of IBD are highlighted. Finally, the synergistic role of NPP as a carrier of drugs or active molecules to reduce side effects and enhance targeting function are discussed, especially pectic polysaccharides. Broadly, this review provides a valuable reference for NPP to be developed as functional food or health products to alleviate IBD.

Postharvest processing plays a very important role in improving the quality of traditional Chinese medicine. According to previous studies, smoke-drying could significantly promote the accumulation of the bioactive components and pharmacological activities of rhubarb, but so far, the molecular mechanism has not been studied yet. In this research, to study the molecular mechanisms of postharvest processing for rhubarb during shade-drying and smoke-drying, label-free proteomic analyses were conducted. In total, 1,927 differentially abundant proteins (DAPs) were identified from rhubarb samples treated by different drying methods. These DAPs were mainly involved in response and defense, signal transduction, starch, carbohydrate and energy metabolism, and anthraquinone and phenolic acid biosynthesis. Smoke-drying significantly enhanced the expression of proteins involved in these metabolic pathways. Accordingly, the molecular mechanism of the accumulation of effective ingredients of rhubarb was clarified, which provided a novel insight into the biosynthesis of active ingredients that occur during the rhubarb dry process.

Diosgenin and diosgenyl saponins as the major bioactive compounds isolated from dietary fenugreek seeds, yam roots, etc. possessed strong antitumor effects. To understand their detailed antitumor mechanisms, a fluorophore-appended derivative of diosgenin [Glc/CNHphth-diosgenin (GND)] was synthesized, starting from diosgenin and glucosamine hydrochloride in overall yields of 7-12% over 7-10 steps. Co-localization of GND with organelle-specific stains, transmission electron microscopy, and relative protein analyses demonstrated that GND crossed the plasma membrane through organic anion-transporting polypeptide 1B1 and distributed in the endoplasmic reticulum (ER), lysosome, and mitochondria. In this process, GND induced ER swelling, mitochondrial damage, and autophagosome and upregulating IRE-1α to induce autophagy and apoptosis. Furthermore, autophagy inhibitor chloroquine delayed the appearance of cleaved poly(ADP-ribose) polymerase and inhibited cleaved caspase 8, which indicated that GND induced autophagy to activate caspase-8-dependent apoptosis. These observations suggested that diosgenyl saponin was a potent anticancer agent that elicited ER stress and mitochondria-mediated apoptotic pathways in liver cancer.

Novel composite sub-micron fibers materials, consisting of superfine powdered diatomite (SPD) and fibrous poly(vinyl alcohol) (PVA), were fabricated by electrospinning. SPD was obtained after high energy ball milling for 6h high energy ball milling with 10% (wt%) Polyvinyl pyrrolidone (PVP) as dispersant. The diameters of SPD (400 nm–1000 nm) were 30 times less than that of the normal powdered diatomite particles, and SPD also had pores inside based on Rhodamine B (RhB) micro-pollutant. The composite sub-micron fibers were composed by three dimensional networks from PVA sub-micron fibers, on which SPD particles were randomly attached on. The composite sub-micron fibers exhibited excellent mechanical behavior and stable thermal decomposition property in the temperature from 275 °C to 300 °C. Comparing with PVA sub-micron fibers, SPD-PVA composite sub-micron fibers possess extra 36% adsorption capacity to RhB, which was due to 48.5% (wt%) of SPD in fibers. Conserving the adsorptive functionality of SPD particles in electrospinning non-woven polymeric fiber, could enable them to be used in the fields of adsorbants.

This study aims at presenting a comprehensive perusal on polysaccharides from Angelica Sinensis Radix (ASPs) processing with Chinese rice wine (18, 20, 22, 24 min at 120 °C) through investigating the structural characterizations, antioxidant activity, invigorating blood circulation activity, and inhibitory activity on alkaline phosphatase. The results of high-performance gel permeation chromatography (HPGPC) and scanning electron microscope (SEM) indicated that certain aggregation and disaggregation would happen owing to the wine processing. While they all had the typical fourier transform-infrared spectroscopy (FTIR) spectra characteristic of polysaccharides. Monosaccharide composition analysis combined with 1H NMR spectroscopic analysis demonstrated that all samples are of the same monosaccharide composition, but the ratios and types were varied diversely. The structure differences mainly focused on the chemical compositions, the monosaccharide ratios, types, and apparent structure. Wine processing, especially stir-frying 20 min, caused higher antioxidant abilities, stronger inhibitory activities on thrombin and alkaline phosphatase. In conclusion, stir-frying 20 min was a good choice for the preparation of wine-processed A. Sinensis, for which polysaccharides owned the highest content of neutral sugar and GalA, as well as the best antioxidant and alkaline phosphatase inhibitory activity.

Two neutral polysaccharides named POP-1 and PCP-1 were purified from Polygonatum odoratum and P. cyrtonema, respectively. Results showed that both of them were composed of fructose and glucose, and the average molecular weights of them were about 5 kDa. FT-IR, 1D- and 2D-NMR analyses revealed that both POP-1 and PCP-1 contained a (2→1)-linked β- d -fructofuranose (Fruf) backbone and (2→6)-linked β- d -Fruf side chains with an internal α- d -glucopyranose (Glcp) in neokestose form. The difference between these two purified polysaccharides were that PCP-1 possessed of an acetyl group attached at O-3 of α- d -Glcp residue. In addition, PCP-1 exhibited a little better immune stimulating activity than POP-1 on cell viability and IL-6 production of RAW 264.7 macrophages. These results indicated that the acetyl group might affect the immunoregulatory activity and PCP-1 have more potential to be explored as an immunomodulatory agent.

The effect of drying methods were evaluated including hot air drying (HD), blanching-hot air drying (BHD), shade drying, microwave-hot air drying (MHD), freeze drying (FD), and vacuum-hot air drying (VHD) on the quality and bioactivities of chrysanthemum flowers. HD had the lowest total flavonoid values due to the reaction between flavonoids and oxidase during drying. Reduced activities of polyphenol oxidase and peroxidase in samples from MHD and BHD suggested that they are effective at inhibiting enzymatic browning, while the BHD could lead to the loss of some water-soluble components. Microwave treatment for 30 s combined with 75 °C hot air drying was the most effective treatment in preserving biologically active compounds, resulting in higher antioxidant capacity and greater inhibition of the enzyme acetylcholinesterase (AChE). FT-IR showed that the BHD, microwave treatment for 90 s, and VHD led to loss of more compounds than FD. This study also found that 3,5-di-caffeoylquinic acid (3,5-DCQA), luteolin-7-O-glucoside (LuG), luteolin, and kaempferol were the key bioactive substances inhibiting AChE. Furthermore, molecular docking studies showed that a high inhibition of AChE by 3,5-DCQA and LuG could be attributed to the formation of strong hydrogen bonds. The study may be beneficial for understanding C. morifolium's nutritional value and the effects of drying methods on the quality of the final product.

The starch-palmitic acid complex was prepared by the reaction of different concentrations (0.1%–5.0%) of palmitic acid and yam starch. In order to find out the effects of concentration of palmitic acid on the properties of the complex, the physicochemical properties, morphological properties, freeze-thaw stability, antioxidant activity and bile acid binding capacity of complexes were studied. It was found that with the increase of palmitic acid concentration, the complex index of starch-fatty acid increased first and then decreased. When the concentration of palmitic acid was 2%, the complex index was the highest (26.39%). The crystal type has gradually changed from Ca type into mixtures of V-type pattern and B-type pattern when introduced palmitic acid. The water binding capacity, solubility, swelling power and paste clarity were decreased, while the content of resistant starch and freeze-thaw stability were obviously increased. Compared with the native starch, the antioxidant activity and bile acid binding capacity of the complex were significantly increased. All the result showed that the concentration of palmitic acid has a great influence on the physicochemical properties of modified starch and the starch-palmitic acid complexes have higher ability of controlling cholesterol and improving the anti-oxidant activity than native yam.

Development of bio-therapeutics has exhibited exponential growth in China over the past decade. However, no biosimilar drug has been approved in China (CN) due to the lack of a national biosimilar regulatory guidance. HLX01, a rituximab biosimilar developed in China under European Medicines Agency biosimilar guidelines and requirements, was the first such drug submitted for regulatory review in China, and it is expected to receive approval there as a biosimilar product. To demonstrate the analytical similarities of HLX01, CN-rituximab (sourced in China but manufactured in Europe) and EU-rituximab (sourced and manufactured in Europe), an extensive 3-way physicochemical and functional similarity assessment using a series of orthogonal and state-of-the-art techniques was conducted, following the similarity requirement guidelines recently published by China’s Center for Drug Evaluation. The results of the similarity study showed an identical protein amino acid sequence and highly similar primary structures between HLX01 and the reference product (RP) MabThera®, along with high similarities in higher order structures, potency, integrity, purity and impurity profiles, biological and immunological binding functions, as well as degradation behaviors under stress conditions. In addition, HLX01 presented slightly lower aggregates and better photostability compared with the RP. Despite slight changes in relative abundance of glycan moieties and heavy chain C-terminal lysine modification, no differences in biological activities and immunological properties were observed between the RP and HLX01. In conclusion, HLX01 is highly similar to CN- and EU-sourced RP in terms of physicochemical properties and biological activities, suggesting similar product quality, efficacy, and safety. The regulatory requirements interpreted and applied towards the HLX01 marketing application sets a precedent for analytical similarity assessment of biosimilar products in China.

Polysaccharides (ASP) were extracted from Angelica Sinensis Radix (ASR) and were subjected to freeze drying (ASP-FD), vacuum drying (ASP-VD), and hot air drying (ASP-HD). Structural characteristics, rheological and emulsifying properties, antioxidant, anticoagulant and alkaline phosphatase inhibitory activities of ASPs were firstly investigated. ASP-FD owned higher thermostability, unique morphological structure, uniform and the lowest molecular weight, which is suitable for using as a raw material for polysaccharide derivatives. Smaller viscosity of ASP-FD supplied a better appearance that consumers preferred and the smallest particle size was benefit to manufacture instant soluble products. ASP-VD behaved the highest neutral sugar content, protein content, intrinsic viscosities, and the best emulsifying activity, being a candidate for cosmetics additive. ASP-HD exhibited the highest apparent viscosities, higher thermostability, loose structure, and better bioactivities. Drying conditions had significant effect on the physicochemical properties and bioactivities of ASPs. ASPs with specific characteristics may meet the requirements for diverse applications.

Physicochemical properties and gastroprotection of four types of resistant starch (RS) including native (RS2), retrograded (RS3), cross-linked with sodium trimetaphosphate/sodium tripolyphosphate (RS4) and complexed with palmitic acid (RS5) resistant starches were investigated and compared. After modification, there was no significant change in RS content in addition to the decline in the RS3. The crystal type of RS2 was B-type pattern. During modification, RS3 and RS5 lost their granular shape and crystalline structure collapsed, while RS4's granular structure was not destroyed and maintained the B-type crystalline pattern. In addition, gastroprotective effect of the four types of RS on gastric ulcer induced by ethanol in mice was investigated. Pretreatment with the four types of RS had an obvious gastroprotection compared to ethanol group that significantly attenuated the level of histopathological injury and ulcerative lesion index (ULI). Also, the excess malondialdehyde (MDA) and the reduced superoxide dismutase (SOD) induced by ethanol can be effectively inhibited. Furthermore, there were more SCFAs (short chain fatty acids) generated in colon with the four starches when compared with ethanol group. The results demonstrated that the four types of RS were proved to be effective on ethanol-induced gastric injure probably by ameliorating oxidative stress, generating more SCFAs and promoting gastric emptying. Of the four RS samples tested, the high dose groups of RS3 and RS5 showed the best activity. This study reported four kinds of gastro-protection starches and provided useful information for functional food and pharmaceutical industries.

Context: Aquilariae Lignum Resinatum (ALR), the dry rhizome of Aquilaria agallocha R. (Thymelaeaeeae), has been widely used to treat emesis, stomachache and gastrointestinal dysfunction. Objective: This study evaluates the effects of ALR methanol extract on gastrointestinal motility (GIM) and possible mechanisms of the action involved. Materials and methods: In vivo, the study evaluated the effects of ALR (200–800 mg/kg) on gastric emptying and small intestinal motility in normal and neostigmine-induced adult KM mice. The in vitro effects of ALR (0.2–1.6 mg/mL) on GIM were performed on isolated jejunum of Wistar rats, pretreated with acetylcholine (ACh), KCl, CaCl2, and pre-incubation with l-NAME (a selective inhibitor of the nitric oxide synthase). Results: In vivo, ALR (800 mg/kg) decreased gastric emptying (70.82 ± 9.81%, p

More than 90% of the cancer-associated mortality is attributed to its metastasis. Numerous studies demonstrated that natural steroidal saponins from plants had the capacity to inhibit lung cancer metastasis. Dioscin-6’-O-acetate (DA) was a novel steroidal saponin first obtained from the rhizomes of Dioscorea althaeoides R. Knuth. Our previous study indicated that it suppressed lung cancer cell proliferation via inducing cell-cycle arrest and enhancing caspase-dependent apoptosis. Until now, there were still no reports on its anti-migration activity. In the present study, we further verified the anti-proliferation and apoptosis-inducing effects and investigated the anti-migration effects of DA on human NSCLC (NCI-H460, NCI-H1299, NCI-H520) and SCLC (NCI-H446) cells for the first time. To clarify the possible mechanisms, western blot and/or RT-PCR analysis were used. The results revealed that DA treatment increased the levels of caspase 3, 8, 9, and Bax and markedly decreased the expression of bcl-2, PCNA, MMP-2, MMP-9, and NF-κB. Docking study indicated that DA presented strong affinity with the key metastasis-related proteins, such as MMP-2, MMP-9, and NF-κB. We proposed that DA might suppress lung cancer proliferation by downregulating PCNA, induce lung cancer apoptosis via activation of caspase-dependent apoptosis pathways, and inhibit lung cancer migration possibly by targeting MMP-2/9 through NF-κB signaling suppression. The findings would provide the foundation for the clinical use of DA in future.

Liver cancer most commonly develops in patients with chronic liver disease, the etiology of which includes viral hepatitis (B and C), alcohol, obesity, dietary carcinogens, and so forth. The current treatment modalities, including surgical resection and liver transplantation, have been found far from effective. Hence, there is an obvious critical need to develop alternative strategies for the treatment of it. In this review, we discuss the formation process and therapeutic targets of liver cancer. Currently, targeted therapy is limited to sorafenib, lenvatinib, regorafenib, ramucirumab and cabozantinib which leads to a survival benefit in patients, but on the other hand is hampered by the occurrence of drug resistance. Pleasingly and importantly, there are multiple natural products undergoing clinical evaluation in liver cancer, such as polyphenols like icaritin, resveratrol, and silybin, saponins including ginsenoside Rg3 and glycyrrhizinate, alkaloid containing irinotecan and berberine and inorganic compound arsenic trioxide at present. Preclinical and clinical studies have shown that these compounds inhibit liver cancer formation owing to the influence on the anti-viral, anti-inflammation, anti-oxidant, anti-angiogenesis and anti-metastasis activity. Furthermore, a series of small molecule derivatives inspired by the aforementioned compounds are designed and synthesized according to structure-activity relationship studies. Drug combination and novel type of drug-targeted delivery system thereof have been well developed. This article is ended by a perspective remark of futuristic development of natural product-based therapeutic regimen for liver cancer treatment. We expect that this review is an account for current status of natural products as promising anti-liver cancer treatments and should contribute to its understanding.

Polyphyllin II (PII) and polyphyllin VII (PVII) were the main active ingredients in Paris Polyphylla with an excellent antitumor effect in vitro and in vivo. In this study, a rapid and precise LC-MS/MS method was developed and validated for the separation and simultaneous determination of PII and PVII in rat plasma, tissues, feces and urine using ginsenoside Rg3 as the internal standard. A positive linearity ranged from 1 to 1000 ng/mL in samples. At the same time, intra- and inter-day precision were in range of 1.8% to 12.0%. The accuracy was ranged from 95.9% to 100.8%. Mean extraction recovery of PII and PVII were ranged from 86.6% to 96.4%. The analytical method has been successfully applied to the pharmacokinetic studies of PII and PVII in rats after their intravenous administration. After entering systemic circulation, PII and PVII were rapidly distributed in organs, mainly including liver, lung and spleen. Their elimination rate was slow. All these data provided a theoretical basis for the application of PII and PVII in the treatment of liver and lung related diseases.

The aim of this study was to investigate and compare the structural and physicochemical properties of native Banxia starch (BXS) and autoclaving-cooling treated Banxia starch (CTBXS) and its related impacts on production of short chain fatty acids (SCFAs) and human gut microbiota by in vitro fecal fermentation. BXS had semicircle to spherical granules, whereas CTBXS exhibited block-shape. According to XRD and TGA, BXS had a C-type crystalline pattern, while CTBXS had a B-type crystalline pattern. CTBXS had better thermal stability than BXS. In addition, BXS exhibited significantly higher solubility and swelling power than CTBXS, and CTBXS had higher content of SDS than BXS. Moreover, BXS and CTBXS could change the composition and abundance of gut microbiota, could also promote the production of SCFAs. This study is beneficial to well understand the in vitro digestion and fecal fermentation behaviors of BXS and CTBXS, and can be developed as a potential functional food with the aim of improving colonic health.

Many free-living saprobic fungi are nature recruited organisms for the degradation of wastes, ranging from lignocellulose biomass to organic/inorganic chemicals, aided by their production of enzymes. In this study, fungal strains were isolated from contaminated crude-oil fields in Nigeria. The dominant fungi were selected from each site and identified as Aspergillus oryzae and Mucor irregularis based on morphological and molecular characterization, with site percentage incidences of 56.67% and 66.70%, respectively. Selected strains response/tolerance to complex hydrocarbon (used engine oil) was studied by growing them on Bushnell Haas (BH) mineral agar supplemented with the hydrocarbon at different concentrations, i.e., 5%, 10%, 15%, and 20%, with a control having dextrose. Hydrocarbon degradation potentials of these fungi were confirmed in BH broth culture filtrates pre-supplemented with 1% engine oil after 15 days of incubation using GC/MS. In addition, the presence of putative enzymes, laccase (Lac), manganese peroxidase (MnP), and lignin peroxidase (LiP) was confirmed in culture filtrates using appropriate substrates. The analyzed fungi grew in hydrocarbon supplemented medium with no other carbon source and exhibited 39.40% and 45.85% dose inhibition response (DIR) respectively at 20% hydrocarbon concentration. An enzyme activity test revealed that these two fungi produced more Lac than MnP and LiP. It was also observed through the GC/MS analyses that while A. oryzae acted on all hydrocarbon components in the used engine oil, M. irregularis only degraded the long-chain hydrocarbons and BTEX. This study confirms that A. oryzae and M. irregularis have the potential to be exploited in the bio-treatment and removal of hydrocarbons from polluted soils.

Fungi, organisms of high nutritional value with significant bioactive compound content, are considered to be nutraceuticals, mycotherapeutics, cosmeceuticals and useful for the production of functional foods. Their cultivation allows the sustainable management of agro-industrial wastes and generates good income with low inputs, constituting a good opportunity for the development of economically depressed rural areas. There are also many possible uses for the spent substrate in various sectors. provide an overview of the nutritional value of mushrooms and the cultivation of edible and medicinal mushrooms cultivation and uses in Italy.

In this work, a series of In2O3/NiO composites with hierarchical structure were prepared through an efficient synthesis method based on electrospinning technique and ion exchange reaction. Material characterization confirmed that the composite was composed by one-dimensionally aligned NiO nanosheets with In2O3 nanoparticles evenly attached to them. Gas sensing properties of the In2O3/NiO series composites were systematically investigated, accompanying with pristine NiO sample for comparison. An obvious enhancement in ethanol sensing performance was discovered for the NiO based sensor via decoration with In2O3 nanoparticles. The gas sensing mechanism of In2O3/NiO composite towards ethanol based on the formation of nanoscale p-n heterojunction structure was discussed. Besides, gas response properties of the In2O3/NiO series sensors to some harmful gases (including ethanol, DMF, acetone and ammonia) were found out to be highly dependent on the component content within the composites. The different gas sensing patterns of In2O3/NiO series sensors could be utilized to discriminate among these target gases.

Ferroptosis is a type of lipid peroxidation-induced cell death that can be regulated in various ways, from changing the activity of antioxidant enzymes to the levels of transcription factors. The p53 tumor suppressor gene is the "guardian of the genome" and is involved in controlling cell survival and division under various pressures. In addition to its effects on apoptosis, autophagy, and cell cycle, p53, through the way of transcription dependent or independent two-way, also regulates the biological processes of tumor cell sensitivity to ferroptosis, including the metabolism of amino acids, nicotinamide adenine dinucleotide phosphate, and lipid peroxidation, as well as the biosynthesis of glutathione, phospholipids, NADPH and coenzyme Q10.As reviewed here, we summarized the metabolic network of p53 and its signaling pathway in regulating ferroptosis and elucidated possible factors and potential clinical application of p53 regulating ferroptosis. This review will provide a basis for further understanding the role of p53 in tumor ferroptosis and new strategies for cancer therapeutic avenues.

Ethnopharmacological relevance Paris polyphylla var yunnanensis as a traditional Chinese medicine has been used in the treatment of liver disease for thousands of years. Rhizoma Paridis saponins (RPS) were the main active ingredients in Paris polyphylla with an excellent antitumor effect. However, metabolic and distribution of RPS has not been known. Aim of the study: The objective of this study was to research metabolic and distribution of RPS. Materials and methods In this study, the separation and simultaneous determination of RPS in rat plasma and tissues were developed and validated by LC–MS/MS. The permeability and recovery of RPS were tested by Caco-2. S9 assay suggested the metabolic mode of RPS in rats. Results After oral administration of RPS, the metabolic compound like diosgenin was detected in different tissues although there was none in RPS. The concentration of PI, PII, PVI, PVII, PH and gracillin in the spleen was the highest among these organs. The content of diosgenin were the highest in lung and brain. Caco-2 test indicated that PI, PII, PVI and PVII were low permeability and low recovery. Efflux ratio indicated that PVI should be a potential P-gp substrate. Potential P-gp substrate may be PVI. S9 assay suggested that RPS possess slow metabolic and moderate metabolic compounds. Conclusions Integrated LC–MS/MS analysis of serum samples, together with Caco-2 and S9 assays provided a theoretical basis for the application of RPS in the future.

Red clover consists of the overground parts and inflorescence of Trifolium pratense L., a leguminous plant belonging to the genus Trifolium. It is widely distributed worldwide and has long been used in traditional medicine. In this study, a combination approach using UPLC-MS and network pharmacology was applied to explore the quality control markers for the quality assessments of red clover. Firstly, UPLC-MS was used to identify the compounds in different parts of red clover. Twenty-eight compounds were totally identified. According to the traditional clinical efficacy of red clover, a compound-target-function network was constructed by network pharmacology to discover the main active compounds based on the identified compounds. Nine compounds of chlorogenic acid, daidzin, calycosin-7-O-&beta, d-glucoside, genistin, ononin, daidzein, genistein, formononetin, and biochanin A were filtrated and further confirmed in rat plasma in view of the blood-absorbed components taking effects. Finally, a novel method for simultaneously detecting the nine quality control markers was developed by UPLC-QQQ-MS in an effort to assess the quality of red clover. For all samples, the average contents of the nine compounds measured from high to low consist of formononetin, ononin, biochanin A, genistin, daidzin, calycosin-7-O-&beta, d-glucoside, genistein, daidzein, and chlorogenic acid. The samples from Gansu province showed the best quality in the three producing areas This study provides new strategies to explore the quality control markers and develops a novel method for the quality assessment of red clover.

Introduction According to previous reports, hypertension has become the most common chronic disease in the world. Captopril, an angiotensin-converting enzyme inhibitor, has been widely used for the therapy of arterial hypertension and cardiovascular diseases therapy. Besides, Shunaoxin pill (SNX) as a traditional Chinese prescription showed antihypertensive effect in our previous research. Objective This study means to investigate whether SNX combining with captopril could show antihypertensive and renal protective effects on spontaneous hypertension rats (SHRs). Methods SHRs were randomly assigned to four treatment groups, including non-treated group, captopril, SNX, and captopril + SNX-treated groups. Their body weight and systolic blood pressure (SBP) were measured weekly. Histopathological examination was analyzed through Masson staining and hematoxylin and eosin staining. Biochemical analyses, ELISA, and western blot were used to analyze their combining mechanism. Results In this experiment, this combinatorial therapy significantly reduced aortic wall thickness, increased the content of NO, NOS and eNOS, decreased the content of bradykinin and endothelin 1(ET-1), and regulated the levels of TG, TC and HDLC back to normal, which suggested they could induce vasodilation and lower blood pressure. Meanwhile, histological examination alleviated that captopril + SNX remarkably inhibited renal injury, including tubular disorder, inflammatory cell infiltration and fibrosis. They down-regulated the serum levels of BUN and Cr, protein expression of IL-1β, NF-κB, Bax, Cyt c, caspase 3, 8 and 9 in kidney tissues and significantly increased the levels of Bcl-2 in kidney tissues compared with monotherapy group. Conclusion The combinatorial treatment of SNX and captopril lowered blood pressure through adjusting NO/NOS, ET-1 and dyslipidemia profile. Furthermore, this treatment alleviated the kidney damage via reducing the release of inflammatory factors and the expression of apoptotic markers. Therefore, these results provided a rationale for future clinical use of SNX combined with captopril in antihypertensive and protecting renal functions in hypertension.

Spinel exsolution is widespread in titanomagnetite from the Fe‐Ti oxide gabbro of the Panzhihua intrusion, Emeishan Large Igneous Province, SW China. However, little research has been conducted into the implications of patterns in the mineralogical characteristics of the spinel for spatial variation in the controls on the exsolution mechanism and, hence, the formation process of the ore deposit. This study selected the Lanjiahuoshan Ore Block in the Panzhihua V‐Ti magnetite deposit to explore this issue, systematically studying exsolution textures in the titanomagnetite through petrographic observation and the integrated use of in‐situ microanalysis. The results show that the exsolved spinel gradually becomes finer‐grained and less abundant from the center to edge and the bottom to top of the ore bodies. Compositionally, there is an inverse correlation between the size of exsolved spinel grains and their Mg# value. In addition, there is compositional zonation in the spinel interiors, with a gradual increase in the Mg content and decrease in Fe content from the core to the rim. The analysis suggests that fractional crystallization of ferrotitanium magma with a high oxygen fugacity in a shallow magma chamber caused compositional differences in the primary magnetite solid solution in different parts of the Panzhihua intrusion. Additionally, the thermal evolution of the magnetite solid solution differed in different parts of orebody, bringing about variations in spinel development. Together, these effects resulted in spatial variation in the abundance, grain size, and morphology of spinel in different parts of the orebody and intrusion that follows an identifiable distribution law. Furthermore, the compositional zonation of exsolved spinels reflects the rapid growth of exsolution features in a high‐temperature environment. Thus, the size, morphology, abundance, and composition of spinel exsolution features in titanomagnetite provide a valuable petrogenetic tool for estimating the maturity and formational environment of the deposit.

Ginsenosides attract great attention for their bioactivities. However, their contents are low, and many UDP-glycosyltransferases (UGTs) that play crucial roles in the ginsenoside biosynthesis pathways have not been identified, which hinders the biosynthesis of ginsenosides. In this study, we reported that one UDP-glycosyltransferase, UGTPg71A29, from Panax ginseng could glycosylate C20-OH of Rh1 and transfer a glucose moiety to Rd, producing ginsenosides Rg1 and Rb1, respectively. Ectopic expression of UGTPg71A29 in Saccharomyces cerevisiae stably generated Rg1 and Rb1 under its corresponding substrate. Overexpression of UGTPg71A29 in transgenic cells of P. ginseng could significantly enhance the accumulation of Rg1 and Rb1, with their contents of 3.2- and 3.5-fold higher than those in the control, respectively. Homology modeling, molecular dynamics, and mutational analysis revealed the key catalytic site, Gln283, which provided insights into the catalytic mechanism of UGTPg71A29. These results not only provide an efficient enzymatic tool for the synthesis of glycosides but also help achieve large-scale industrial production of glycosides.

Formononetin (MBHS) and its glycosylated derivative ononin (MBHG), as the major isoflavones, have exhibited the anti-inflammatory impacts on the lipopolysaccharide (LPS)-induced inflammation. Although various researches have focused on interpreting the pharmaceutical activities of MBHG and MBHS, the molecular mechanisms in zebrafish models are still unclear. The purpose of the present work is to investigate the molecular mechanisms of the anti-inflammatory effects of MGHG and MBHS based on lipidomics and targeted transcriptomics. UHPLC-MS was applied for the lipid analyses and RT-PCR was adopted for the mRNA analyses, and the results of different groups were compared for exploring the significantly changed lipids and mRNAs. The results of lipidomics revealed that phosphatidylcholines (PCs) were drastically down-regulated in the MBHG or MBHS treated LPS-induced inflammatory zebrafish models. Besides, MBHS can also decrease the levels of triacylglycerols (TAGs). For the targeted transcriptomics analyses, 4 cytokines (TNF-α, IL-1β, IL-6 and IFN-γ) and 3 mRNA (JNK1, ERK1 and p38a) involved in the MAPK pathway were down-regulated and IL-10 was up-regulated under the treatment of MBHG or MBHS. Combining the results of lipidomics and targeted transcriptomics, we indicated that MBHG and MBHS exerted potent anti-inflammatory effects on the LPS-induced zebrafish models through the MyD88 or TRIF MAPK/ERK and MAPK/JNK pathways and the glycerophospholipid, glycosylphosphatidylinositol (GPI)-anchor biosynthesis and glycerolipid metabolisms. Our results provided new insights into the anti-inflammatory mechanisms of MBHG or MBHS and supplied an effective method to interpret the pharmacological mechanisms of drugs.

Glycyrrhiza uralensis Fisch (G. uralensis) is gradually declining from the nature due to the plant high demand and over exploited. Glycyrrhizic acid, glycyrrhetinic acid and total flavonoid are the most important active compounds in G. uralensis. Adventitious root culture has been exploited as a biotechnological alternative for more efficient and controllable production of active metabolites. In this study, four adventitious root (AR) lines (AR-leaf, AR-stem, AR-root, AR-indirect) of G. uralensis have been successfully established. Histological analysis showed that the fibers, crystalline calcium oxalate, vessels and cork cells of G. uralensis AR lines were smaller than that in native root in size. The contents of total flavonoid, glycyrrhizic acid and glycyrrhetinic acid peaked at native G. uralensis and followed by AR-indirect. The contents of polysaccharide in AR lines were higher than that in native roots. Compared to native root, the principal component analysis (PCA) indicated that the accumulation pattern of metabolites is distinct in AR lines. The expression levels of 8 genes were consistent with production of glycyrrhizic acid and glycyrrhetinic acid. In addition, the correlation analysis revealed that the glycyrrhizic acid biosynthesis was significantly correlated with the gene expression of 3-hydroxy-3-methylglutaryl CoA reductase (HMGR) and β-amyrin synthase (β-AS) and showed the positive correlation.

Chaenomeles is an important source for food industry in China, and its planting area is expanding year by year. This study was conducted to evaluate different varieties of Chaenomeles by comparing the chemical compositions, antioxidant activity and α-glucosidase inhibitory activity of peels and fleshes from twelve varieties of Chaenomeles. In the results, peels of Chaenomeles contain more phenolics, flavonoids and triterpenes, and show better antioxidant activity and α-glucosidase inhibitory activity than their fleshes. All varieties of Chaenomeles perform different depend on cultivar and climatic conditions. Oleanolic acid, ursolic acid, protocatechuic acid, rutin, catechin, caffeic acid, syringic acid, epicatechin, hyperin, quercetin, kaempferol and chlorogenic acid are main active compounds in Chaenomeles. Zheng'an, Liufu, Zimugua1, Qijiang and Changjun get Top five scores. This is the first study on the peels and fleshes of twelve varieties of Chaenomeles, and it gives insights into variety selection in the planting and production of Chaenomeles.

In this paper, we reviewed the advances in ginsenoside biosynthesis and metabolic regulation. To begin with, the application of elicitors in the ginsenoside biosynthesis was discussed. Methyl jasmonate (MJ) and analogues have the best effect on accumulation of ginsenoside compared with other elicitors, and few biotic elicitors are applied in Panax genus plants tissue culture. In addition, so far, more than 40 genes encoding ginsenoside biosynthesis related enzymes have been cloned and identified from Panax genus, such as UDP-glycosyltransferases (UGT) genes UDPG, UGTAE2, UGT94Q2, UGTPg100, and UGTPg1. However, the downstream pathway of the ginsenoside biosynthesis is still not clear. Moreover, some methods have been used to increase the expression of functional genes and ginsenoside content in the ginsenoside synthesis pathway, including elicitors, overexpression, RNAi, and transcription factors. The ginsenoside biosynthesis pathway should be revealed so that ginsenoside contents can be regulated.

Formononetin and its glycoside ononin are bioactive isoflavones widely present in legumes. The present study investigated the pharmacokinetics, bioavailability, and in vitro absorption of formononetin and ononin. After an oral administration to rats, formononetin showed a higher systemic exposure over ononin. The oral bioavailability of formononetin and ononin were 21.8% and 7.3%, respectively. Ononin was more bioavailable than perceived, and its bioavailability reached 21.7% when its metabolite formononetin was taken into account. Both formononetin and ononin exhibited better absorption in large intestine segments than that in small intestine segments. Formononetin displayed a better permeability in all intestinal segments over ononin. Transport of formononetin across Caco-2 cell monolayer was mainly through passive diffusion, while ononin was actively pumped out by MRP2 but not P-gp. The results provide evidence for better understanding of the pharmacological actions of formononetin and ononin, which advocates more in vivo evaluations or human trials.

Raw rhubarb samples that have been subjected to different drying procedures will have different therapeutic effects, possibly due to processing-induced variations in the chemical composition. In the present work, the fresh materials were processed by smoking, sun-drying, shade-drying and oven-drying at low, moderate and high temperatures. To facilitate the selection of a suitable drying method for rhubarb, the quality of rhubarb processed under various drying conditions was evaluated based on the simultaneous determination of multiple bioactive constituents in combination with bioactivity assays.; Results: The total concentrations of 12 compounds in smoked rhubarb were higher than the concentrations of the same components in raw rhubarb and rhubarb products processed using other drying techniques. Smoked rhubarb was found to substantially inhibit Na+ /K+ -ATPase and thrombin. In addition, higher content of anthraquinones led to higher Na+ /K+ -ATPase inhibitory activities, and higher gallic acid content increased the antithrombin capacity.; Conclusion: The results confirmed that post-harvest fresh plant materials, especially roots, were still physiologically active organs that could undergo series of anti-dehydration mechanisms, including the production of related secondary metabolites during the early stages of dehydration. Therefore, the proper design of drying processes could enhance the quality of rhubarb as well as other similar medicinal plants. © 2018 Society of Chemical Industry.; © 2018 Society of Chemical Industry.

CTAB-Surface-Modified-TiO2 nanocatalysts were synthesized via a microemulsion combine hydrothermal method. The experimental result showed that the nitric acid concentration and hydrothermal temperature had important influence on the photocatalytic activity of samples. When the nitric acid concentration was 2 M and hydrothermal temperature was 120 °C, photocatalytic activity of sample was highest. It could achieve 99.99% degradation rate of rhodamine B (RhB) within 60 min visible light irradiation. The superior photocatalytic activity was mainly ascribed to that the CTAB molecule groups could abound the surface state of TiO2 and the abundant surface state could generate shallow trap levels to trap electron and thus enhanced light absorption as well as reduced electron-hole pair recombination.

The Shunaoxin dropping pill (SNX) is derived from a traditional recipe. It has been used to treat cerebrovascular diseases in China since 2005 (approval number Z20050041). In this study, we used an in vitro H2O2-induced PC12 cell oxidative damage model and an in vivo D-gal-induced mouse memory impairment model to investigate whether SNX had neuroprotective effects. In vitro, prior to exposure to 100 μM H2O2 for 2 h, PC12 cells were pre-treated with SNX 50 μg mL−1 for 24 h. Hoechst 33258 staining was used to confirm the effect of SNX on apoptosis in the PC12 cells. Our results demonstrate that H2O2 suppresses the proliferation of PC12 cells and induces cell death. Pretreatment with SNX attenuates H2O2-induced apoptosis in PC12 cells. In vivo, D-gal was administered (100 mg kg−1, subcutaneously (s.c.)) once daily for 8 weeks to induce memory deficit and neurotoxicity in the brain of an aging mouse. Then, SNX (320 mg kg−1) was simultaneously administered orally. The present study demonstrates that SNX can alleviate aging in the mouse brain induced by D-gal via improving behavioral performance, alleviating oxidative stress, inhibiting neuroinflammation, and reducing brain cell damage in the hippocampus. Overall, these data clearly demonstrate the neuroprotective effect of SNX from the in vitro and in vivo results. SNX may be considered a novel agent for easing aging and/or age-related neurodegenerative diseases.

Doxorubicin (DOX) is one of the most effective antineoplastic drugs, however, its organ toxicity inhibits the clinical utility. This study was aimed at investigating the protective effects of Yiqi Fumai lyophilized injection (YQFM) against DOX-induced tissue injury and exploring the mechanisms which mediated reactive oxygen species (ROS), inflammation and apoptosis. The experiment was as follows: rats were subjected to an intraperitoneal injection (i.p.) of YQFM (0.481 g kg−1, i.p.) for 12 days; DOX (5 mg kg−1, i.p.) was administered on the 4th, 8th and 12th days to achieve a cumulative dose of 15 mg kg−1. Pretreatment of YQFM significantly ameliorated intracellular damage and dysfunction of the heart, liver and kidneys via decreasing activities of injury indexes. The levels of lipid peroxidation and glutathione depletion were clearly reduced following YQFM pretreatment, meanwhile the activities of glutathione peroxidase, superoxide dismutase, and catalase were elevated. Additionally administering YQFM could mitigate the cardiotoxicity, hepatotoxicity and nephrotoxicity via reducing levels of inflammatory factors and decreasing apoptosis. Accordingly, this study indicated that YQFM attenuated DOX-induced toxicity by ameliorating organ function, decreasing ROS production, and preventing excessive inflammation and apoptosis.

Solvents effect of water, methanol aqueous, and ethanol aqueous on the active compositions (TFc, TPc, TTc, TCc, TPs and contents of eleven selected compounds) in Chaenomeles speciosa were studied, as well as effects on antioxidant activity, anti-α-glucosidase activity, and inhibit effect on Ach induced smooth muscle contraction of isolated rat jejunum. The results indicate that compositions and activities of extracts prepared with different solvents vary, and methanol, 60% methanol, 40% methanol, 20% methanol and 60% ethanol would be good choices for the industrial production of Chaenomeles speciosa extracts. Water extract displays the highest inhibit activity on the contraction of smooth muscle of isolated rat jejunum, and the result also indicates that condensed tannin is responsible for the inhibit activity. In summary, our study presents the solvents effect on chemical compositions and biological activities of Chaenomeles speciosa, and gives an insight into the potential application of Chaenomeles speciosa.

Using endophytic fungi elicitors to enhance the yield of valuable secondary metabolites in plant tissue culture is an effective biotechnology strategy. In this study, we isolated an endophytic fungus Chaetomium sp. from cultivated Panax ginseng root and detected a high concentration of Rg3 in its mycelium. By comparing the effects of different treatments of Chaetomium sp. on ginsenoside production in Panax ginseng adventitious roots (PGARs), the immobilized spores of Chaetomium sp. (ISC) were proved to be the best elicitor. An initial pH of 6.5 and cocultivation time of 24 h yielded the highest ginsenosides content (56.29 ± 0.62 mg/g) in ISC-treated PGARs, increasing ginsenosides production by 3.2-fold compared with the blank group (17.56 ± 0.49 mg/g). Moreover, we show that ISC could stimulate the temporary accumulation of defense-related signal molecules, intensify the expression of defense genes in PGARs, and upregulate biosynthetic genes involved in the biosynthetic pathway of ginsenosides. Besides, the expression of the biosynthetic gene FPS (farnesyl diphosphate synthase) was deemed the most relevant factor for ginsenosides production during the elicitation period, and the L -aspartic acid secreted by Chaetomium sp. was proven to play a key role in the elicitation process. In conclusion, this study provides an accessible way of improving pharmacologically active compounds production in medicinal plants.

Background Cardiac fibrosis occurs in ischemic and non-ischemic heart failure, hereditary cardiomyopathy, diabetes and aging. Energy metabolism, which serves a crucial function in the course and treatment of cardiovascular diseases, might have therapeutic benefits for myocardial fibrosis. Ginsenoside Rb3 (G-Rb3) is one of the main components of Ginseng and exhibits poor oral bioavailability but still exerts regulate energy metabolism effects in some diseases. Therefore, the study investigated the effect of chitosan (CS) @ sodium tripolyphosphate (TPP) nanoparticles conjugation with ginsenoside Rb3 (NpRb3) on myocardial fibrosis and studied its possible mechanisms. The results showed that NpRb3 directly participates in the remodeling of myocardial energy metabolism and the regulation of perixisome proliferation-activated receptor alpha (PPARα), thereby improving the degree of myocardial fibrosis. The study also verifies the protective effect of NpRb3 on energy metabolism and mitochondrial function by targeting the PPARα pathway. Therefore, the prepared nanodrug carrier may be a potential solution for the delivery of G-Rb3, which is a promising platform for oral treatment of myocardial fibrosis.