Preparation and polarization activity research of astragalus polysaccharide-superparamagnetic iron oxide nanocomposite / 药学学报

Size and surface modification are the two key factors affecting the effect of macrophages polarization induced by superparamagnetic iron oxide nanoparticles (SPIONs). The smaller the particle size, the better the polarization effect of SPIONs. Besides, the reasonable SPIONs surface modification method can also be used to enhance the polarization effect. In this study, SPIONs was prepared by solvothermal method and optimized by Box-Benhnken center combination design and response surface method. Furthermore, astragalus polysaccharide-superparamagnetic iron oxide nanocomplex (APS-SPIONs) was successfully constructed by EDC/NHS esterification method. The structure of APS-SPIONs was confirmed by dynamic light scatter and infrared spectrometer, and the contents of iron and polysaccharide were characterized by spectrophotometry. The effect of APS-SPIONs on inducing mouse macrophages RAW264.7 polarization was investigated by flow cytometry. The RAW264.7 macrophages-HepG2 human hepatoma cancer cells Transwell co-culture system was established to investigate APS-SPIONs improve anti-tumor function of macrophages in vitro, and the proliferation activity of APS-SPIONs on RAW264.7 detected by cell counting kit-8 (CCK-8) method. The results showed that the average particle size and zeta potential of APS-SPIONs were (82.93 ± 1.47) nm and (-24.00 ± 0.47) mV. Polysaccharide and Fe content were 8.69% and 7.04%, respectively. APS-SPIONs effectively induced the polarization of RAW264.7 into M1 type in vitro, improving the anti-tumor ability of macrophages in a co-culture system, without effecting the proliferation of macrophages. Our study provides a drug development strategy and preliminary research results to educate macrophages and reshape the tumor immune microenvironment to achieve tumor-killing effects.

Research progress of injectable in situ hydrogel embolic agents / 药学学报

Embolotherapy is a common method for clinical intervention in the treatment of diseases including aneurysms, arteriovenous malformations and solid tumors, and embolic agents are a decisive factor affecting the effect of embolization. Although various embolic agents like coils, microspheres, and Onyx have been used clinically, there are still some treatment limitations: such as weak blood vessel penetration, easy to aggregate, poor mechanical properties, adhesion to catheters, and the need for toxic solvents (e.g. dimethyl sulfoxide). In recent years, a number of studies have found that in situ hydrogels have good application prospects in the field of vascular embolization. When low viscosity precursor solution is injected into the targeted blood vessel via microcatheters, it will undergo a sol-gel transition through physical and/or chemical cross-linking to form hydrogel to block blood flow. In addition, these in situ hydrogels can load drugs by pore embedding, electrostatic interaction, chemical bonding, etc., and have excellent sustained-release properties. This review summarizes the research progress of injectable in situ hydrogel vascular embolic agents in the past ten years, with a view to provide references for the development of new embolic agents in the future.

Progress in the prevention and treatment of age-related macular degeneration with active ingredients of traditional Chinese medicine / 药学学报

Age-related macular degeneration (AMD) is one of the main causes of vision loss among middle-aged and elderly people worldwide. The prevention and treatment of AMD is a current topic of interest in ophthalmology but remains challenging. Oxidative stress-induced retinal pigment epithelial cell autophagic dysfunction, cellular senescence, and an abnormal immune inflammatory response are key pathogenic factors for AMD. Many bioactive ingredients of traditional Chinese medicine not only exert anti-oxidative, anti-inflammatory, anti-aging, and anti-apoptotic effects, but also prevent/block the occurrence of AMD through different pathways. This review summarizes our current understanding of the pathogenesis of AMD, the types of natural bioactive ingredients capable of treating AMD, as well as the known mechanisms by which these agents act, and may provide new strategies for the prevention and treatment of AMD.

Research progress on Fe-based metal-organic frameworks in antitumor drug delivery / 药学学报

Fe-based metal-organic frameworks (MOFs) are a class of polymer crystals formed by the combination of Fe ions or Fe clusters with organic ligands through coordination bonds. At present, Fe-based MOFs can be mainly prepared by solvothermal synthesis, ultrasonic synthesis, microwave synthesis, and dry-gel conversion, etc. Fe-based MOFs have the characteristics of strong drug loading capacity of inorganic nano-carrier and high safety of organic nano-carrier, and have good tumor targeting and the capacity of inducting tumor's ferroptosis, which have high potential in the delivery of antitumor drugs. Recently, Fe-based MOFs have also been developed with various functions such as imaging, magnetic hyperthermia, photothermal therapy, photodynamic therapy, and intelligent response, which can facilitate diagnosis and monitor drug distribution while delivering antitumor drugs, and can produce synergistic antitumor effects combined with thermotherapy and phototherapy, and can also control the precise release of drugs. Reviewing the advances in the synthesis methods, characteristics as well as functions and types of Fe-based MOFs can provide a basis for the further applications of Fe-based MOFs in antitumor drug delivery.

Research progress of natural polysaccharides and their nano-sized drug delivery systems in regulating tumor microenvironment / 药学学报

Natural polysaccharides with good biocompatibility and unique tumor immunomodulatory activity are becoming an important adjuvant anticancer therapy in clinic. In the field of pharmaceutics, natural polysaccharides can be used as not only bioactive components but also drug delivery carriers, as well as tumor-targeted ligands. Besides, various novel drug delivery systems based on natural polysaccharides exhibit unique advantages in regulating tumor immune microenvironment. In this review, we summarize the progress on natural polysaccharides in tumor microenvironment (TME) regulation and the designs of nano-sized drug delivery system, and point out challenges of polysaccharide-based drug delivery systems in the future application, and also give the potential solutions for these issues.

Effects of preparation technologies and entrapment materials on encapsulation efficiencies of three constituents' liposomes / 中成药

AIM To prepare the liposomes loaded with celastrol,tanshinone Ⅱ A and tanshinone Ⅱ A sodium sulfonate and to evaluate the effects of preparation technologies and entrapment materials on the encapsulation efficiencies.METHODS The liposomes for three constituents were prepared by film dispersion method and reverse phase evaporation method,respectively.50％ Lecithin high potency,80％ egg yolk lecithin,92％ lecithin high potency and complex phospholipid (5 ∶ 1 for ratio of dipalmitoyl phosphatidylcholine to 50％ lecithin high potency) were served as entrapment materials.The encapsulation efficiencies were thus calculated based on the measured ean sizes and polydispersity of the liposomes.RESULTS Celastrol and tanshinone Ⅱ A sodium sulfonate liposomes accomplished by reverse phase evaporation method got the highest encapsulation efficiency when entrapped with 80％ egg yolk lecithin and 92％ lecithin high potency,respectively,which were higher than those prepared by film dispersion method.And celastrol liposomes exhibited an even superior performance than tanshinone Ⅱ A sodium sulfonate liposomes.Tanshinone Ⅱ A lipisome prepared by film dispersion method and then entrapped with 50％ lecithin high potency obtained its the highest value of encapsulation efficiency,which was much lower than those of another two liposomes.CONCLUSION Reverse phase evaporation method is appropriate for hydrophobic celastrol with multiple hydrogen bonds and hydrophilic sodium tanshinone Ⅱ A without hydrogen bonds to prepare their liposomes,while film dispersion method is applicable to hydrophobic tanshinone Ⅱ A without hydrogen bonds.

Determination of five marker components and total flavonoids in Paishi Granules / 中成药

AIM To determine the contents of five marker components and total flavonoids in Paishi Granules (a medication to remove stones in the body,containing Glechomae Herba,Akebiae Caulis,Cynanchi Paniculati Radix et Rhizoma,etc.).METHODS The content determination of various components in 50％ methanol extract of Paishi Granules was accomplished by RP-HPLC.The analysis was performed on a 30 ℃ thermostatic Aglient SBC1s column (250 mm ×4.6 mm,5 μm),with the mobile phase comprising of acetonitrile-0.05％ phosphoric acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 240 nm.The content of total flavonoids was detected by ultraviolet spectrophotometry.RESULTS Chlorogenic acid,loganin,rutin,rosmarinic acid and ammoninm glycyrrhizinate showed good linear relationships within the ranges of 18.88-604.00,18.50-592.00,20.25-648.00,18.75-600.00 and 18.81-602.00 μg/mL,whose average recoveries were 97.9％,100.7％,103.3％,96.4％ and 102.4％ with theRSDsof1.4％,0.4％,2.7％,1.2％ and 2.3％,respectively.The contents of total flavonoids in twenty batches of samples all met pharmacopeia requirements,while those of marker components were found to be different,among which loganin displayed the most significant change,followed by rutin and ammoninm glycyrrhizinate.CONCLUSION This simple,accurate and reliable method can be used for the quality control of Paishi Granules.

Preparation And Characterization of Tripterine-Coix Seed Component Microemulsions And Its Inhibition on Lung Cancer In Vivo / 世界科学技术-中医药现代化

This study was aimed to prepare tripterine-coix seed component microemulsions (TCC-MEs) with coix seed oil and coix seed polysaccharide as bimodal excipients and evaluate its activity on anti-lung cancer in vivo.Coix seed oil was extracted by supercritical extraction methods and coix seed polysaccharide was obtained through hot water extraction and alcohol precipitation from coix seed.Then,coix seed oil was used as the oil phase,and coix seed polysaccharide aqueous solution was used as the aqueous phase.RH40 was used as the surfactant.PEG400 was used as cosurfactant to prepare microemulsion.TCC-MEs were made by water titration method and characterized by size,polymer dispersity index (PDI),zeta potential,encapsulation efficiency and drug loading capacity.And then,anti-tumor activity of TCC-MEs was evaluated on the xenograft Lewis tumor mouse models.The liver and kidney toxicity was evaluated by HE staining and biochemical indicators.The results showed that the optimized prescription for TCC-MEs was coix seed oil 400 mg,RH40 300 mg,PEG 400 100 mg,coix seed polysaccharide 50 mg,tripterine 10 mg;and the tripterine encapsulation efficiency was (90.72 ± 0.28)％;the drug loading capacity was (1.08 ± 0.17)％;the mean diameter of microemulsion was (43.86 ± 0.22) nm;PDI was 0.10 ± 0.01;the zeta potential was (-13.14 ± 1.35) mV.The activity of anti-lung cancer in TCC-MEs was significantly better than that of the control group,with no significant liver and kidney toxicity after treatment with TCC-MEs.It was concluded that the prepared TCC-MEs had advantages of small amount of conventional auxiliary materials,small particle size and high stability.This study showed that the combination of triptolide and coix seed to microemulsion system has synergistic and attenuated effect.

Pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo / 中成药

AIM To investigate the pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo.METHODS Twelve rats were divided into model group and sham group,after which the osteoporotic rat model was established by removing bilateral ovaries.After intragastric administration with total flavonoids (500 mg/kg),HPLC-DAD was applied to detecting the plasma concentrations of total flavonoids' prototype glycosides (epimedin A,epimedin B,epimedin C,icariin) and their metabolites (sagittatoside A,sagittatoside B,2-O-rhamnosylicariside Ⅱ,baohuoside Ⅰ,icaritin) at thirteen time points (0.083,0.25,0.5,0.75,1,2,3,4,6,8,12,24 and 48 h),then the plasma concentration-time curves were drawn,followed by the calculation of pharmacokinetic parameters.RESULTS Doubled peaks were observed in the plasma concentration-time curves of total flavonoids' prototype glycosides and their metabolites in both groups.Compared with the sham group,the integrated AUC and Cmax in the model group were significantly decreased (P ＜ 0.01),as well as the prolonged t1/2 (P ＜ 0.01).CONCLUSION The in vivo absorption and metabolism of total flavonoids from Epimedii Folium are much slower in the state of osteoporosis,thus affects the efficacy.

Study on biosynthesis of silver nanoparticles using fagopyri dibotryis rhizoma extract and optimization of synthesis conditions / 中国中药杂志

Silver nanoparticles were synthesized from the extract of Fagopyri Dibotryis Rhizoma and the optimization of synthesis was studied. The absorbance of UV-visible spectroscopy was determined under the different influencing factors such as extracting time of Fagopyri Dibotryis Rhizoma powder, reation temperature of synthesis, volume of Fagopyri Dibotryis Rhizoma extract and concentration of AgNO3 to seek the optimization conditions. By means of FT-IR, TEM, DLS and XRD, the silver nanoparticles were characterized. The results showed that when the boiling time of Fagopyri Dibotryis Rhizoma powder was 5 min, resultant temperature was 25 degrees C, the volume ratio of 0.1 g x mL(-1) Fagopyri Dibotryis Rhizoma extract and 1 mmol x L(-1) AgNO3 was 1 to 10, and the reaction time was 3.5 h, the obtained silver nanoparticles had mean size about 27 nm and Zeta potential about -34.3 mV with good uniformity and dispersivity. Therefore, the green synthesis method of silver nanoparticles using extract of traditional Chinese medicine is stable and feasible.

Family size, fertility preferences, and sex ratio in China in the era of the one child family policy: results from national family planning and reproductive health survey.

OBJECTIVES: To examine the impact of the one child family policy in China on fertility, preferred family size, and sex ratio. DESIGN: Secondary analysis of data from the Chinese cross sectional national family planning and reproductive health survey, 2001. Interviews of representative sample of women aged 15-49. RESULTS: Data were obtained from 39,585 women, with a total of 73,202 pregnancies and 56,830 live births. The average fertility rate in women over 35 (n = 17,078) was 1.94 (2.1 in rural areas and 1.4 in urban areas) and for women under 35 (n = 11,543) 1.73 (1.25 and 1.79). Smaller families were associated with younger age, higher level of education, and living in an urban area. The male to female ratio was 1.15 and rose from 1.11 in 1980-9 to 1.23 for 1996-2001. Most women wanted small families: 35% preferred one child and 57% preferred two. CONCLUSION: Since the one child family policy began, the total birth rate and preferred family size have decreased, and a gross imbalance in the sex ratio has emerged.

Anxiety and depression in adolescents in urban and rural China.

The goal was to assess rates of anxiety and depression in adolescents in two areas of Zhejiang Province, China. A cross-sectional survey was carried-out using a self-report questionnaire developed for this study. Participants were middle school students (age range 13-16 years) in an urban and a rural setting. There were 1576 completed questionnaires. Symptoms of anxiety sufficient to interfere with enjoyment of life, relaxation, and sleep were common (48%, 40%, and 27%, respectively). School-related problems were the predominant sources of worry. One third reported a history of depression, 16% had at times felt life was not worth living, and 9% reported that they had attempted suicide. Girls were more likely to report symptoms of depression. Patterns of help-seeking showed reliance on friends and parents; only 1% had sought professional help. There were no significant differences in anxiety and depression between one-child and multisibling families.

Health and health care-seeking behavior of adolescents in urban and rural China.

A cross-sectional survey was conducted among 13-18-year-old adolescents in Zhejiang Province, China. Morbidities showed few urban/rural differences. Concerns were mainly related to academic pressure. Respondents were eager users of health services; 73% were taking regular medication, but 52% had never attended a dentist.

Disparities in economic development in Eastern China: impact on nutritional status of adolescents.

OBJECTIVE: To compare the effects of disparities in economic development in urban and rural Eastern China on the nutritional status of adolescents. DESIGN: A cross-sectional survey consisting of self-completion questionnaires, anthropometry and haemoglobin measurement. SETTING: Twelve middle schools in an urban and a rural area of Zhejiang Province: Hangzhou, the capital, and Chunan, a poor mountainous area. SUBJECTS: Some 4835 young adolescents (predominant age range 13-16 years). RESULTS: The mean body mass index (BMI) was significantly higher in urban Hangzhou (P = 0.01) Overweight affected 3.6% overall; adjusted odds ratios (ORs) showed male sex (OR 2.1, 95% confidence interval (CI) 1.1-3.4) and urban residence (OR 9.1, 95% CI 3.7-22) to be the most important risk factors. The prevalence of underweight was 18%, with no significant urban-rural difference. Predictors of underweight were male sex (OR 1.5, 95% CI 1.1-2.0) and low household income (OR, 1.3, 95% CI 1.1-1.5). Mean haemoglobin was significantly lower in the rural area. Anaemia was more common in girls, 51% compared with 21% of the boys, but rural residence was not an independent risk factor. Rural students exercised more and had a less varied diet than their urban counterparts. Around one-third of the respondents consumed dietary supplements on a regular basis. CONCLUSIONS: These results suggest that in urban areas of Eastern China a dual picture is emerging with the problems of excess (overweight and obesity) coexisting with underweight and anaemia. In rural areas the problems of relative nutritional deprivation predominate, but the long-term consequences of such marginal underweight and anaemia are not clear.

Growth status and menarche in urban and rural China.

OBJECTIVE: To examine the relationship between current age at menarche and growth status in an urban and rural area of Eastern China. STUDY DESIGN: Cross-sectional survey: self-completion questionnaire and anthropometry in 12 schools in urban Hangzhou and rural Chunan in Zhejiang Province. RESULTS: The median menarcheal age calculated by probit analysis was significantly different in the two areas: 12.8 years (SD 0.9) in the urban area and 13.2 (SD 1.0) in the rural area (p < 0.001). Girls who reach menarche are significantly heavier and taller with higher BMIs than those of the same age who are pre-menarche. After adjustment for BMI and other possible confounders, urban girls were still menstruating significantly earlier than girls in rural areas (OR 3.3, 2.1-5.2). CONCLUSIONS: The age of menarche is probably still declining in China. Although BMI is an important factor in the onset of menstruation, some other unmeasured environmental variable may be implicated in this population.