Ent-labdane-type diterpene glycosides obtained from Rubus chingii Hu and their inhibitory effects on PDE5A activity.

In this study, 16 new ent-labdane-type diterpene glycosides, designated as goshonosides J1-J16 (1-16), along with nine previously known diterpene glycosides (17-25) were extracted from the fruits of Rubus chingii Hu. The structures of goshonosides J1-J16 were elucidated using various analytical techniques, such as nuclear magnetic resonance, electron capture detector ECD, high-resolution electrospray ionization mass spectrometry HREIMS, single-crystal X-ray diffraction, and hydrolysis. Furthermore, the isolates' efficacy in inhibiting the activity of phosphodiesterase type 5 A was evaluated. Goshonosides J1, J2, and G effectively inhibited the activity of the aforementioned enzyme (IC50 values: 6.15 ± 1.76, 3.27 ± 0.65, and 9.61 ± 2.36 µM, respectively). Our findings highlight the remarkable structural diversity of bioactive compounds in R. chingii Hu and offer insights into the use of this shrub.

MXSGD alleviates CsA-induced hypoimmunity lung injury by regulating microflora metabolism.

Context: Ma Xing Shi Gan Decoction (MXSGD) is a traditional remedy for treating lung injuries that was developed by the Typhoid and Fever School of Pharmaceutical Biology. It has antitussive and expectorant effects, anti-inflammatory, antiviral, regulates the body's immunity, etc. Aim: The aim of this study is to investigate whether MXSGD can ameliorate cyclosporine A (CsA)-induced hypoimmunity lung injury by regulating microflora metabolism. Methods: Establishment of a model for CsA-induced hypoimmunity lung injury. Using 16S rRNA high-throughput sequencing and LC-MS, the effects of MXSGD on gut flora and lung tissue microecology of mice with CsA-induced hypoimmunity were investigated. Results: MXSGD was able to preserve lung tissue morphology and structure, reduce serum inflammatory marker expression and protect against CsA-induced lung tissue damage. Compared to the model, MXSGD increased beneficial gut bacteria: Eubacterium ventriosum group and Eubacterium nodatum group; decreased intestinal pathogens: Rikenellaceae RC9 intestinal group; reduced the abundance of Chryseobacterium and Acinetobacter, promoted the production of Lactobacillus and Streptococcus, and then promoted the lung flora to produce short-chain fatty acids. MXSGD was able to enhance the expression of serum metabolites such as Americine, 2-hydroxyhexadecanoylcarnitine, Emetine, All-trans-decaprenyl diphosphate, Biliverdin-IX-alpha, Hordatin A and N-demethyl mifepristone in the CsA-induced hypoimmunity lung injury model. Conclusion: MXSGD can restore gut and lung microbiota diversity and serum metabolite changes to inhibit inflammation, ameliorate CsA-induced hypoimmunity lung injury.

The Effectiveness Comparison of Different Acupuncture-Related Therapies on Knee Osteoarthritis: A Meta-Analysis.

Objective: This meta-analysis aims to assess the efficacy of acupuncture-related therapy on knee osteoarthritis (KOA) patients. Method: We searched PubMed, Embase, and CNKI databases to screen eligible trials between 2017 and 2022. All trials that used acupuncture/moxibustion of KOA patients were included. Study selection and data extraction were performed by 2 researchers independently. The statistics was performed by using R 4.1.1. Results: A total of 17 trials were included in our meta-analysis. Meta-analysis results showed the evidence of the relation of several common acupunture/moxibustion treatments by network meta-analysis. In the fixed effect model, acupuncture/moxibustion has superior therapy efficacy than sham treatment (mean difference = -0.34, 95% confidence interval = (-0.52,-0.16), P=0.95). In fixed effect model, specific acupuncture/moxibustion has superior therapy efficacy than usual acupuncture/moxibustion (mean difference = -0.45, 95% confidence interval = (-0.62, -0.29), P < 0.01). Conclusion: Acupuncture/moxibustion has superior therapy efficacy than sham treatment. Specific acupuncture/moxibustion has superior therapy efficacy than usual acupuncture/moxibustion.

Magnesium implantation or supplementation ameliorates bone disorder in CFTR-mutant mice through an ATF4-dependent Wnt/ß-catenin signaling.

Magnesium metal and its alloys are being developed as effective orthopedic implants; however, the mechanisms underlying the actions of magnesium on bones remain unclear. Cystic fibrosis, the most common genetic disease in Caucasians caused by the mutation of CFTR, has shown bone disorder as a key clinical manifestation, which currently lacks effective therapeutic options. Here we report that implantation of magnesium-containing implant stimulates bone formation and improves bone fracture healing in CFTR-mutant mice. Wnt/ß-catenin signaling in the bone is enhanced by the magnesium implant, and inhibition of Wnt/ß-catenin by iCRT14 blocks the magnesium implant to improve fracture healing in CFTR-mutant mice. We further demonstrate that magnesium ion enters osteocytes, increases intracellular cAMP level and activates ATF4, a key transcription factor known to regulate Wnt/ß-catenin signaling. In vivo knockdown of ATF4 abolishes the magnesium implant-activated ß-catenin in bones and reverses the improved-fracture healing in CFTR-mutant mice. In addition, oral supplementation of magnesium activates ATF4 and ß-catenin as well as enhances bone volume and density in CFTR-mutant mice. Together, these results show that magnesium implantation or supplementation may serve as a potential anabolic therapy for cystic fibrosis-related bone disease. Activation of ATF4-dependent Wnt/ß-catenin signaling in osteocytes is identified as a previously undefined mechanism underlying the beneficial effect of magnesium on bone formation.

Involvement of kisspeptin in androgen-induced hypothalamic endoplasmic reticulum stress and its rescuing effect in PCOS rats.

Endoplasmic reticulum (ER) stress, with adaptive unfolded protein response (UPR), is a key link between obesity, insulin resistance and type 2 diabetes, all of which are often present in the most common endocrine-metabolic disorder in women of reproductive age, polycystic ovary syndrome (PCOS), which is characterized with hyperandrogenism. However, the link between excess androgen and endoplasmic reticulum (ER) stress/insulin resistance in patients with polycystic ovary syndrome (PCOS) is unknown. An unexpected role of kisspeptin was reported in the regulation of UPR pathways and its involvement in the androgen-induced ER stress in hypothalamic neuronal cells. To evaluate the relationship of kisspeptin and ER stress, we detected kisspeptin and other factors in blood plasm of PCOS patients, rat models and hypothalamic neuronal cells. We detected higher testosterone and lower kisspeptin levels in the plasma of PCOS than that in non-PCOS women. We established a PCOS rat model by dihydrotestosterone (DHT) chronic exposure, and observed significantly downregulated kisspeptin expression and activated UPR pathways in PCOS rat hypothalamus compared to that in controls. Inhibition or knockdown of kisspeptin completely mimicked the enhancing effect of DHT on UPR pathways in a hypothalamic neuronal cell line, GT1-7. Kp10, the most potent peptide of kisspeptin, effectively reversed or suppressed the activated UPR pathways induced by DHT or thapsigargin, an ER stress activator, in GT1-7 cells, as well as in the hypothalamus in PCOS rats. Similarly, kisspeptin attenuated thapsigargin-induced Ca2+ response and the DHT- induced insulin resistance in GT1-7 cells. Collectively, the present study has revealed an unexpected protective role of kisspeptin against ER stress and insulin resistance in the hypothalamus and has provided a new treatment strategy targeting hypothalamic ER stress and insulin resistance with kisspeptin as a potential therapeutic agent.

[Research advance in multi-component pharmacokinetics of Chinese herbal extracts in recent five years].

The multi-component pharmacokinetic study of Chinese herbal extracts elaborates the in vivo processes,including absorption,distribution,metabolism,and excretion,of multiple bioactive components,which is of significance in revealing pharmacodynamic material basis of Chinese herbal medicine. In recent years,with the innovation in ideas,and development of techniques and methods on traditional Chinese medicine( TCM) research,the pharmacokinetic studies of Chinese herbal extracts were extensively performed,and notable progress has been made. This paper reviewed the advancement of multi-component pharmacokinetics of Chinese herbal extracts in recent five years from analysis technology of biological sample,the pharmacokinetic characteristics of Chinese herbal medicine with complex system,and the impacts of processing and pathological state on pharmacokinetics of Chinese herbal extracts,aiming to provide a reference for quality control,product development and rational medication of Chinese herbal extracts.

Therapeutic effects of Yiqi Huoxue prescription on diabetic nephropathy: a meta-analysis and systematic review.

BACKGROUND: Traditional Chinese medicine (TCM) has demonstrated excellent effects in treating diabetic nephropathy, and Yiqi Huoxue prescription has been widely used clinically. In the study, its effects on the kidney function and blood glucose of patients were explored. METHODS: Chinese and English databases including PubMed, Medline, Embase, and Web of Sciences were used to retrieve articles comparing the treatment of diabetic nephropathy using Yiqi Huoxue prescription on the basis of conventional Western medicine treatment (experimental group) and conventional Western medicine treatment alone (control group) published from January 2000 to December 2020. The risk of bias assessment tool of the Cochrane System Review Manual 5.2.2 and the Jadad scale were used to evaluate the quality of the included literature. The outcome indexes were extracted, and the Review Manager 5.3 software was used for meta-analysis. RESULTS: A total of 13 articles that satisfied the inclusion/exclusion criteria were included in this study. After treatment, compared to the control group, the experimental group exhibited lower urine microalbumin excretion rate (UAER) [mean difference (MD) =-33.94, 95% confidence interval (CI), -42.60 to -25.28, P<0.00001], serum creatinine (SCr) (MD =-7.43, 95% CI, -11.50 to -3.36, P=0.0004), blood urea nitrogen (BUN) (SMD =-1.23, 95% CI, -2.49 to 0.03, P=0.04), blood glucose-related indexes [fasting blood glucose (FBG)] (MD =-0.43, 95% CI, -0.87 to 0.01, P=0.03), glycosylated hemoglobin (HbA1c) (MD =-0.38, 95% CI, -0.68 to -0.08, P=0.01), blood lipid-related indexes [triglycerides (TG)] (MD =-0.44, 95% CI, -0.76 to -0.13, P=0.006), and serum total cholesterol (TC) (MD =-0.37, 95% CI, -0.57 to -0.18, P=0.0002). Furthermore, the experimental group also showed higher effectiveness rate (odds ratio =3.81, 95% CI, 2.71 to 5.35, P<0.00001) after treatment. DISCUSSION: The included literature had low bias risk. Yiqi Huoxue prescription on the basis of conventional Western medicine can significantly improve the renal function and reduce the levels of blood glucose and blood lipids of patients with diabetic nephropathy.

Anti-SARS-CoV-2 activities in vitro of Shuanghuanglian preparations and bioactive ingredients.

Human infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes coronavirus disease 2019 (COVID-19) and there is no cure currently. The 3CL protease (3CLpro) is a highly conserved protease which is indispensable for CoVs replication, and is a promising target for development of broad-spectrum antiviral drugs. In this study we investigated the anti-SARS-CoV-2 potential of Shuanghuanglian preparation, a Chinese traditional patent medicine with a long history for treating respiratory tract infection in China. We showed that either the oral liquid of Shuanghuanglian, the lyophilized powder of Shuanghuanglian for injection or their bioactive components dose-dependently inhibited SARS-CoV-2 3CLpro as well as the replication of SARS-CoV-2 in Vero E6 cells. Baicalin and baicalein, two ingredients of Shuanghuanglian, were characterized as the first noncovalent, nonpeptidomimetic inhibitors of SARS-CoV-2 3CLpro and exhibited potent antiviral activities in a cell-based system. Remarkably, the binding mode of baicalein with SARS-CoV-2 3CLpro determined by X-ray protein crystallography was distinctly different from those of known 3CLpro inhibitors. Baicalein was productively ensconced in the core of the substrate-binding pocket by interacting with two catalytic residues, the crucial S1/S2 subsites and the oxyanion loop, acting as a "shield" in front of the catalytic dyad to effectively prevent substrate access to the catalytic dyad within the active site. Overall, this study provides an example for exploring the in vitro potency of Chinese traditional patent medicines and effectively identifying bioactive ingredients toward a specific target, and gains evidence supporting the in vivo studies of Shuanghuanglian oral liquid as well as two natural products for COVID-19 treatment.

Response of the nitrogen load and its driving forces in estuarine water to dam construction in Taihu Lake, China.

To regulate the water level and minimize the occurrence of water eutrophication in shallow lakes, dams and gates are often constructed in rivers. However, this practice may result in a deterioration of water quality in some estuaries. In the present study, using the correction of Nemerow pollution index (CNPI) and a redundancy analysis (RDA), water samples from different dammed rivers around Taihu Lake were compared to assess the pollution risk and identify the factors responsible for water eutrophication. The average total nitrogen (TN), total phosphorus (TP), total organic carbon (TOC) concentrations, and chemical oxygen demand (CODMn) were 2.45 ± 2.28, 0.08 ± 0.06, 43.01 ± 18.75, and 10.78 ± 4.86 mg L-1, respectively. The CNPI values indicated that approximately 76.47% of the estuarine water was moderately polluted (1 < CNPI < 7.28). A positive correlation was observed between dam construction and nutrient concentrations (e.g., rTN = 0.38, p < 0.05; rTP = 0.89, p < 0.01). Under the effects of dam construction, land use change, estuary shape, and meteorological conditions, there was a clear spatial variation of the TN concentrations. Dams that were closed all year round accelerated the TN accumulation in the water around them. The pollution risk in a trumpet-shaped estuary was higher than that in other regions (t = 2.92, p = 0.02). Endogenous release of pollutants was an important factor that may have a priming effect on algal blooms and should be given more attention. In Wuli Lake, exogenous pollution was the dominant pollutant source. A total of 74.49% of the nitrogen losses with the runoff into the estuarine water in 2018 were derived from urban domestic sewage and constructed land, with the load being 4.40 times higher than in 2000. The RDA results revealed that dam construction was the main factor (43.70%) affecting water quality, while meteorological conditions, land use types, estuary shape, and other factors contributed 56.30%. Scientific regulation and control of dam operation is important to protect the water environment of Taihu Lake.

Magnesium and vitamin C supplementation attenuates steroid-associated osteonecrosis in a rat model.

Magnesium (Mg)-based biometal attracts clinical applications due to its biodegradability and beneficial biological effects on tissue regeneration, especially in orthopaedics, yet the underlying anabolic mechanisms in relevant clinical disorders are lacking. The present study investigated the effect of magnesium (Mg) and vitamin C (VC) supplementation for preventing steroid-associated osteonecrosis (SAON) in a rat experimental model. In SAON rats, 50 mg/kg Mg, or 100 mg/kg VC, or combination, or water control was orally supplemented daily for 2 or 6 weeks respectively. Osteonecrosis was evaluated by histology. Serum Mg, VC, and bone turnover markers were measured. Microfil-perfused samples prepared for angiography and trabecular architecture were evaluated by micro-CT. Primary bone marrow cells were isolated from each group to evaluate their potentials in osteoblastogenesis and osteoclastogenesis. The mechanisms were tested in vitro. Histological evaluation showed SAON lesions in steroid treated groups. Mg and VC supplementation synergistically reduced the apoptosis of osteocytes and osteoclast number, and increased osteoblast surface. VC supplementation significantly increased the bone formation marker PINP, and the combination significantly decreased the bone resorption marker CTX. TNFα expression and oxidative injury were decreased in bone marrow in Mg/VC/combination group. Mg significantly increased the blood perfusion in proximal tibia and decreased the leakage particles in distal tibia 2 weeks after SAON induction. VC significantly elevated the osteoblast differentiation potential of marrow cells and improved the trabecular architecture. The combination supplementation significantly inhibited osteoclast differentiation potential of marrow cells. In vitro study showed promoting osteoblast differentiation effect of VC, and anti-inflammation and promoting angiogenesis effect of Mg with underlying mechanisms. Mg and VC supplementation could synergistically alleviate SAON in rats, indicating great translational potentials of metallic minerals for preventing SAON.

Degradation Characteristics of Phosphorus in Phytoplankton-Derived Particulate Organic Matter and Its Effects on the Growth of Phosphorus-Deficient Microcystis aeruginosa in Lake Taihu.

To illustrate the contribution of phytoplankton-derived particulate organic matter (PPOM) to endogenous phosphorus (P) cycling and its effects on cyanobacteria blooms, PPOM characteristics, the degradation mechanism, and the growth of P-deficient Microcystis aeruginosa were studied in Lake Taihu. Results showed that PPOM is the most important P pool in the water column during cyanobacteria bloom, accounting for more than 80% of the total P (TP) in the water. During PPOM degradation, the particulate orthophosphate (Ortho-P) is the main species of P release from PPOM in the early degradation stage. The variations of polyphosphate (Poly-P) and phosphodiesters (Diester-P) contents were most significant, which were degraded completely within four days and eight days. Cell density and growth rate of M. aeruginosa using PPOM as P source were similar to those growing on Na2HPO4. The above results show that P in PPOM can be converted into available P by degradation, thus promoting the growth of M. aeruginosa. Therefore, the contribution of P release from PPOM degradation needs to be paid attention to in lake eutrophication control in the future.

Characterization and phylogenetic analysis of the complete chloroplast genome of Curcuma longa (Zingiberaceae).

Curcuma longa, a well-known traditional medicinal plant in China, belongs to the genus Curcuma family Zingiberaceae. In this study, we firstly assembled the complete chloroplast genome of C. longa based on sequences from Illumina and PacBio sequencing platforms. We obtained the complete chloroplast genome with the total length of 162,176 bp. It consisted of a large single-copy region (LSC, 86,984 bp), a small single-copy region (SSC, 15,694 bp), and a pair of inverted repeats (IRs, 29,749 bp each). Sequence analyses indicated that the chloroplast genome contained 111 distinct genes including 79 protein-coding genes, 28 tRNA genes, and four rRNA genes. The nucleotide composition was asymmetric (31.62% A, 18.42% C, 17.79% G, 32.18% T) with an overall AT content of 63.80%. The AT contents of the LSC, SSC and IR regions were 66.00%, 70.35% and 58.85%, respectively. Sixteen genes owned a single intron, while another two genes had two introns. The phylogenetic analysis indicated that C. longa was closely related to species Curcuma roscoeana within the genus Curcuma in family Zingiberaceae.

[Study on mechanism of inducing apoptosis in human hepatoma SMMC-7721 cells by DMC, a chalcone from buds of Cleistocalyx operculatus].

OBJECTIVE: To study the in-vitro inducing apoptosis mechanism of human hepatoma SMMC-7721 cells by 2',4'-di- hydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), a chalcone compound from Cleistocalyx operculatus. METHOD: Quantitative DNA fragmentation assay was carried out to detect the effect of DMC of different concentrations on SMMC-7721 cells, according to the method of Sellins and Cohen with some modifications. Telomerase activities of the cells were determined by PCR-ELISA methods. The expression quantity of c-myc and hTERT mRNA were determined by semi-quantitative RT-PCR The effect of DMC on expression levels of cmyc and hTERT protein were measured by western blot. RESULT: The percentage of DNA fragmentation increased with notable concen- tration dependence, after treatment with DMC for 48 h. Compared with that of control group, the telomerase activity of the cells de- creased by (66.2 ± 2.1)% after 48 h treatment with 20 µmol x L(-1) DMC, the mRNA expression of c-myc and hTERT decreased by (67.3 ± 2.1)% and (64.4 ± 2.3)%, respectively, and the protein expression of c-myc and hTERT decreased by (69.6 ± 1.9)% and (71.3 ± 2.4)%, respectively. CONCLUSION: DMC can induce SMMC-7721 cell apoptosis and the apoptosis mechanism may be related to the decreased mRNA and protein expression of c-myc and hTERT.

The cytotoxic activities of cardiac glycosides from Streptocaulon juventas and the structure-activity relationships.

A series of cardiac glycosides were isolated and identified from the anti-tumor fraction of the root of Streptocaulon juventas in previous studies. In the present research, the cytotoxic activities of the 43 cardiac glycosides on three cell lines, human lung A549 adenocarcinoma cell, large cell lung cancer NCI-H460 cell and normal human fetal lung fibroblast MRC-5 cell, were evaluated in vitro. Most of the tested compounds showed potent inhibitory activities toward the three cell lines. Then, the structure-activity relationships were discussed in detail. It was indicated that hydroxyl and acetyl groups at C-16 increased the activity, whereas hydroxyl group at C-1 and C-5 can both increase and decrease the activity. Two glucosyl groups which were connected by C1'→C6' showed better inhibitory activity against cancer cell lines, while the C1'→C4' connection showed stronger inhibitory activity against the normal cell line. Also, this is the first report that the activities of these compounds exhibited different variation trends between A549 and NCI-H460 cell lines, which indicated that these compounds could selectively inhibit the cell growth. The results would lay a foundation for further research on new anti-tumor drug development.

Cytotoxic cardiac glycosides from the roots of Streptocaulon juventas.

Chemical investigation on the 75% ethanol extract of the roots of Streptocaulon juventas afforded two new cardiac glycosides, digitoxigenin 3-O-[O-ß-D-glucopyranosyl-(1 → 4)-2-O-acetyl-ß-D-digitalopyranoside] (1) and periplogenin 3-O-[O-ß-D-glucopyranosyl-(1 → 4)-O-ß-D-glucopyranosyl-(1 → 4)-ß-D-cymaropyranoside] (2), and thirteen known cardenolides. Structures were elucidated by spectral methods. This is the first report of the isolation of compounds 3, 10, 14, and 15 from plants of the Streptocaulon genus, while 4, 11, and 12 are hitherto unreported from Streptocaulon juventas. All the compounds were in vitro evaluated for their cytotoxic activities against the A549 cell line, and seven effective cardiac glycosides were screened against the PC-9 cell line by WST assay, which also showed strong antiproliferation activities. Moreover, the characteristic morphological changes in PC-9 cells treated with cardenolides indicated cell inhibition due to apoptosis. These results revealed that these compounds possessed potential antitumor activities.

[Nephro-protective effects of total triterpenoids from Psidium guajava leaves on type 2 diabetic rats].

OBJECTIVE: To investigate the nephro-protective effects of total triterpenoids from Psidium guajava leaves (TTPGL) on type 2 diabetic rats. METHODS: Diabetic rats were induced by intraperitoneal injection of streptozotocin (STZ, 35 mg/kg) and a high-fat diet. Diabetic rats were divided into five groups: diabetic model control, low-dose TTPGL-treated (60 mg/kg, L-TTPGL), medium-dose TTPGL-treated (120 mg/kg, M-TTPGL), high-dose TTPGL-treated (240 mg/kg, H-TTPGL) and rosiglitazone-treated (3 mg/kg, RSG). The rats received daily treatment for six weeks. At the end of the period,the levels of fasting blood glucose (FPG), fasting insulin (FINS), creatinine (Cr) and blood urea nitrogen (BUN) in serum were measured. Kidneys for histopathological evaluation were stained with Hematoxylin and Eosin (HE). RESULTS: Compared with normal control group, the level of FPG was increased, the insulin and insulin sensitivity index were decreased in the model group; The levels of BUN and Cr were increased with histopathological changes related to diabetic nephropathy in the kidney, which were the glomerular endothelium and mesangial cell proliferation, capillary narrowed, the base-membrane incrassation, glomerular swelling, cysts narrowed and tubules edema. Compared with the model group, the levels of FPG were decreased, serum insulin and insulin sensitivity index were increased significantly in M-TTPGL and H-TTPGL groups (P<0.01 or P<0.05); The levels of BUN and Cr were decreased significantly (P<0.01 or P<0.05) and the renal structural damages were improved significantly. CONCLUSION: TTPGL could decrease the level of blood glucose of diabetic rat effectively, increase the insulin sensitivity index and protect renal lesions in diabetic rats.

Decreased accumulation of subcellular amyloid-ß with improved mitochondrial function mediates the neuroprotective effect of huperzine A.

A number of recent discoveries indicate that huperzine A, an active herbal medicine employed for the treatment of Alzheimer's disease (AD) in China, can afford neuroprotection on in vitro and in vivo models related to mitochondrial dysfunction. However, it is an intricate and highly debated research topic about whether another pharmacological mechanism is involved in the beneficial profiles of huperzine A, independent of its well-recognized potent acetycholinesterase (AChE) inhibitory effect. As an extension, this study for the first time verified the co-occurrence of the beneficial effects of huperzine A on mitochondrial dysfunction and memory deficits in AßPP/PS1 double transgenic mice, at a time point that AChE was not inhibited. Moreover, using isolated brain cortical mitochondria, we confirmed the ameliorating effect of huperzine A on oligomeric Aß1-42-induced ATP reduction and mitochondrial swelling, as well as a decrease in the enzymatic activities of respiratory chain complexes, especially complex II-III and complex IV, which may be attributed to the blockage of oligomeric Aß1-42 from penetrating into mitochondria. These results shed more light on a potential direct target of huperzine A on isolated mitochondria, which may be largely different from its specific inhibition on AChE. This work describes a novel mechanism of neuroprotection by huperzine A and provides important clues for discovering novel therapeutic strategy for AD.

Antithrombotic activity of fractions and components obtained from raspberry leaves (Rubus chingii).

The 70% ethanol fraction from an aqueous extract of raspberry leaves was shown to be the most antithrombotic fraction in in vitro and in vivo tests. The total flavonoids and phenolics in this fraction were 0.286g/g and 0.518g/g by colorimetry. Six compounds, including salicylic acid, kaempferol, quercetin, tiliroside, quercetin 3-O-ß-d-glucopyranoside and kaempferol 3-O-ß-d-glucopyranoside, were isolated from the active fraction. Among them, kaempferol, quercetin and tiliroside obviously delayed plasma recalcification time (PRT) in blood.

Extraction of polysaccharides from herbal Scutellaria barbata D. Don (Ban-Zhi-Lian) and their antioxidant activity.

The response surface methodology was employed to study the extraction of polysaccharides from Scutellaria barbata D. Don. The quantitative effects of extraction temperature, time, number and ratio of water to raw material on yield of polysaccharides were investigated with Box-Behnken design. The experimental data were fitted to a second-order polynomial equation using multiple regression analysis and also analyzed using the appropriate statistical methods. By solving the regression equation and analyzing 3D plots, the optimum condition was at extraction temperature 70 °C, time 3h, numbers 3 and ratio of water to raw material 18.5 mL/g. Under these conditions, the experimental polysaccharides yield was 2.43±0.11%, which was in good agreement with the predicted value. The antioxidant activities of the polysaccharides were evaluated in vitro. A potential antioxidant activity of S. barbata polysaccharides provides a scientific basis for the use of this herb in traditional medicine as an antioxidant.

[Effects of extracts of Ginkgo biloba leaves on apelin concentration and expressions in plasma and myocardium of rats with myocardial ischemia injury].

OBJECTIVE: To investigate the changes of apelin in plasma and myocardium of model rats and the protective mechanisms of Extracts of Ginkgo biloba leaves (EGb) on myocardial ischemia injury induced by isoproterenol. METHODS: The model of myocardial ischemia injury was induced by subcutaneous injection of high dose isoproterenol. ELISA (enzyme linked immunosorbent assay) was used to measure the apelin concentration in plasma and myocardium. Semi-Quantitative RT-PCR was used to measure the apelin mRNA level in myocardium. The pathomorphology changes of myocardium was observed with light microscope. EGb was administered for 7 weeks. RESULTS: Compared with the normal control group, the apelin concentration in plasma and myocardium and the apelin mRNA level in myocardium significantly decreased in the model group (P < 0.01). Compared with the model group, the apelin concentration in plasma and myocardium and the apelin mRNA level in myocardium obviously increased in the EGb group (P < 0.01). Meanwhile, the NO content in serum also obviously increased and the pathological damage of myocardium was obviously improved. CONCLUSION: The protective mechanisms of EGb on myocardial ischemia injury may be related to the elevation of apelin contents and apelin mRNA level.