Four new steroidal glycosides from Lilium lancifolium Thunb. and their antitumor activity.

Four new steroidal glycosides (1-4), including two steroidal saponins named lililancifoloside B and C (1-2), one pregnane glycoside named lililancifoloside D (3), and one C22-steroidal lactone glycoside named lililancifoloside E (4), together with five known ones (5-9), were isolated from the bulbs of Lilium lancifolium Thunb. By using spectroscopic analysis, including 1D, 2D NMR, and HR-ESI-MS, the structures of 1-4 were elucidated. All isolates were tested for their cytotoxic potential against the MCF-7, MDA-MB-231, HepG2, and A549 cell lines. Compound 6 distinguished out among them, IC50 values of 3.31, 5.23, 1.78, and 1.49 µM against the four cell lines, respectively. Other compounds such as compound 3, 5, and 9 have also shown specific cytotoxic activity. Next, studies showed that compound 6 might cause HepG2 cells to undergo a cell cycle arrest during the G2/M phase and apoptosis.

Low molecular-weight polyguluronate phosphate: An immunostimulant by activating splenocyte/macrophage invitro and improving immune response invivo.

The substituents and backbones are two main factors affecting immune activities of polysaccharides. In the present study, we firstly evaluated the immunostimulating effects of phosphorylated, sulfated, H-phosphonated and nitrated derivatives of low-molecular-weight polymannuronate (LPM) and polyguluronate (LPG) on splenocytes and peritoneal macrophages in vitro. The results showed that the phosphate group was the best substituent to enhance the immune activities, and LPG phosphate (LPGP) had much better activity than LPM phosphate (LPMP). Further studies showed that LPGP not only promoted the proliferation of mouse splenocytes in the presence of either LPS or Con A, but also acted as an excellent peritoneal macrophage activator to enhance the cell phagocytosis, energy metabolism, cytokines release and activities of intracellular enzymes. The studies in RAW264.7 cells revealed that LPGP activated the TBK1-IκBα-NF-κB and the TBK1-IRF3 pathway. Moreover, LPGP rescued the immune response in the Cyclophosphamide-treated mice in vivo. In conclusion, LPGP is a potential alginate-based biological response modifier (BRM).

Upconversion Luminescence-Initiated and GSH-Responsive Self-Driven DNA Motor for Automatic Operation in Living Cells and In Vivo.

In light of the worthy design flexibility and the good signal amplification capacity, the recently developed DNA motor (especially the DNA walker)-based fluorescent biosensors can offer an admirable choice for realizing bioimaging. However, this attractive biosensing strategy not only has the disadvantage of uncontrollable initiation but also usually demands the supplement of exogenous driving forces. To handle the above obstacles, some rewarding solutions are proposed here. First, on the surface of an 808 nm near-infrared light-excited low-heat upconversion nanoparticle, a special ultraviolet upconversion luminescence-initiated three-dimensional (3D) walking behavior is performed by embedding a photocleavage linker into the sensing elements, and such light-controlled target recognition can perfectly overcome the pre-triggering of the biosensor during the biological delivery to significantly boost the sensing precision. After that, a peculiar self-driven walking pattern is constructed by employing MnO2 nanosheets as an additional nanovector to physically absorb the sensing frame, for which the reduction of the widespread glutathione in the biological medium can bring about sufficient self-supplied Mn2+ to guarantee the walking efficiency. By selecting an underlying next-generation broad-spectrum cancer biomarker (survivin messenger RNA) as the model target, we obtain that the newly formed autonomous 3D DNA motor shows a commendable sensitivity (where the limit of detection is down to 0.51 pM) and even an outstanding specificity for distinguishing single-base mismatching. Beyond this sound assay performance, our sensing approach is capable of working as a powerful imaging platform for accurately operating in various living specimens such as cells and bodies, showing a favorable diagnostic ability for cancer care.

[An integrative metabolomics and network pharmacology method for exploring bioactive components and preliminary pharmacodynamics in medicinal parts of Harrisonia perforata].

In this paper,metabolomics and network pharmacology were used to investigate the bioactive components of Harrisonia perforata and their possible mechanisms of action. Metabolites in the flowers,fruits,branches,leaves and stalks of H. perforata were analyzed by ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Meanwhile,multiple statistical analysis methods including principal component analysis( PCA) and orthogonal partial least squares discriminant analysis( OPLS-DA)were applied to screen and identify differential compounds. With metabolomics method,9 differential compounds were preliminarily identified from leaves and other non-traditional medicinal parts. Subsequently,these compounds were explored by using network pharmacology. With gastrointestinal absorption and drug-likeness as limiting conditions,they were imported into the Swiss ADME,from which 7 compounds with potential medicinal activity were obtained. Then,their targets were predicted by PharmMapper,with Human Protein Targets Only and Normalized Fit Score>0. 9 set as limiting conditions,and 60 standardized potential targets were identified with Uniprot. KEGG( Kyoto encyclopedia of genes and genomes) pathway data was obtained using metascape and the " potential active ingredients-target-pathway" network was constructed with Cytoscape 3. 7. 2. The enrichment analysis of KEGG demonstrated that the 60 targets were enriched in 78 signaling pathways( min overlap: 3,P value cutoff: 0. 01,min enrichment: 1. 5),many of which are related to anti-bacteria,anti-inflammation and anti-virus,such as IL-17 signaling pathway,RIG-I-like receptor signaling pathway and NOD-like receptor signaling pathway. Finally,depending on the clinical activity of H. perforata,the relevant signaling pathways were analyzed through experimental data and literature. Dehydroconiferyl alcohol was reported to have the anti-inflammatory effect and perforamone D to possess the antimycobacterial activity. The KEGG pathway enrichment analysis showed that dehydroconiferyl alcohol could act on the Alzheimer's disease( AD) signaling pathway by targeting CDK5 R1 and BACE1. ACh E inhibitor is the most promising drug to treat AD,while dehydroconiferyl alcohol has been proved to inhibit ACh E according to literature. The experimental results revealed that the extract of leaves of H. perforata can effectively inhibit the growth of Staphylococcus aureus. These are consistent with the enrichment analysis results of KEGG. This study explored the bioactive components and pharmacodynamics of the leaves of the H. perforata,laying a theoretical foundation for its in-depth development and rational application.

Research and application of nanometer black phosphorus in phototherapy and drug carrier / 药学学报

The emerging nano-black phosphorus materials have created a new platform for biomedical research. Nano-black phosphorus has the following advantages: black phosphorus can produce singlet oxygen under near-infrared light irradiation, so it can be used as a photosensitizer for photodynamic therapy;black phosphorus has extensive light absorption in the long wavelength region, and this near-infrared photothermal property can be used in photothermal therapy. The high specific surface area and unique fold structure of the black phosphorus nanosheet make it have very high drug loading.This paper mainly reviews the applications of black phosphorus in biological imaging, photothermal therapy, photodynamic therapy, and as a drug carrier in recent years. Based on the photoelectric properties of black phosphorus nanomaterials combined with intelligent drug delivery platform, the synergistic effects of light/heat/chemistry, light/chemistry/gene, and light/chemistry/immunity can be produced, which has a broad application prospect.

An integrative metabolomics and network pharmacology method for exploring bioactive components and preliminary pharmacodynamics in medicinal parts of Harrisonia perforata / 中国中药杂志

In this paper,metabolomics and network pharmacology were used to investigate the bioactive components of Harrisonia perforata and their possible mechanisms of action. Metabolites in the flowers,fruits,branches,leaves and stalks of H. perforata were analyzed by ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Meanwhile,multiple statistical analysis methods including principal component analysis( PCA) and orthogonal partial least squares discriminant analysis( OPLS-DA)were applied to screen and identify differential compounds. With metabolomics method,9 differential compounds were preliminarily identified from leaves and other non-traditional medicinal parts. Subsequently,these compounds were explored by using network pharmacology. With gastrointestinal absorption and drug-likeness as limiting conditions,they were imported into the Swiss ADME,from which 7 compounds with potential medicinal activity were obtained. Then,their targets were predicted by PharmMapper,with Human Protein Targets Only and Normalized Fit Score>0. 9 set as limiting conditions,and 60 standardized potential targets were identified with Uniprot. KEGG( Kyoto encyclopedia of genes and genomes) pathway data was obtained using metascape and the " potential active ingredients-target-pathway" network was constructed with Cytoscape 3. 7. 2. The enrichment analysis of KEGG demonstrated that the 60 targets were enriched in 78 signaling pathways( min overlap: 3,P value cutoff: 0. 01,min enrichment: 1. 5),many of which are related to anti-bacteria,anti-inflammation and anti-virus,such as IL-17 signaling pathway,RIG-I-like receptor signaling pathway and NOD-like receptor signaling pathway. Finally,depending on the clinical activity of H. perforata,the relevant signaling pathways were analyzed through experimental data and literature. Dehydroconiferyl alcohol was reported to have the anti-inflammatory effect and perforamone D to possess the antimycobacterial activity. The KEGG pathway enrichment analysis showed that dehydroconiferyl alcohol could act on the Alzheimer's disease( AD) signaling pathway by targeting CDK5 R1 and BACE1. ACh E inhibitor is the most promising drug to treat AD,while dehydroconiferyl alcohol has been proved to inhibit ACh E according to literature. The experimental results revealed that the extract of leaves of H. perforata can effectively inhibit the growth of Staphylococcus aureus. These are consistent with the enrichment analysis results of KEGG. This study explored the bioactive components and pharmacodynamics of the leaves of the H. perforata,laying a theoretical foundation for its in-depth development and rational application.

Identification of Synthetic Cannabinoid 5F-EDMB-PICA in Suspicious Herbal Products / 法医学杂志

Objective To study the qualitative analysis strategy for unknown synthetic cannabinoid in the suspicious herbal product when no reference substance is available. Methods The synthetic cannabinoid in herbal blend was extracted with methanol. The extract was concentrated by rotary evaporator and separated and purified by preparative liquid chromatography, to obtain high purity synthetic cannabinoid sample. Gas chromatography-mass spectrometry （GC-MS）, ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry （UPLC-QTOF-MS） and nuclear magnetic resonance （NMR） were used to determine the structure of the prepared compound. Results High purity unknown sample （10 mg） was obtained by preparative liquid chromatography. The sample was analyzed by GC-MS, UPLC-TOF-MS and NMR, and through spectrum analysis, the unknown synthetic cannabinoid was determined as 5F-EDMB-PICA. Conclusion The method to extract unknown synthetic cannabinoid from low content herbal products by preparative liquid chromatography was established, and the structure of the unknown sample was identified by comprehensive use of GC-MS, UPLC-QTOF-MS and NMR. The information will assist forensic laboratories in identifying this substance or other compounds with similar structures in their casework.

The Inhibitory Effect of Propylene Glycol Alginate Sodium Sulfate on Fibroblast Growth Factor 2-Mediated Angiogenesis and Invasion in Murine Melanoma B16-F10 Cells In Vitro.

Melanoma is one of the most malignant and aggressive types of cancer worldwide. Fibroblast growth factor 2 (FGF2) is one of the critical regulators of melanoma angiogenesis and metastasis; thus, it might be an effective anti-cancer strategy to explore FGF2-targeting drug candidates from existing drugs. In this study, we evaluate the effect of the marine drug propylene glycol alginate sodium sulfate (PSS) on FGF2-mediated angiogenesis and invasion. The data shows that FGF2 selectively bound to PSS with high affinity. PSS inhibited FGF2-mediated angiogenesis in a rat aortic ring model and suppressed FGF2-mediated invasion, but not the migration of murine melanoma B16-F10 cells. The further mechanism study indicates that PSS decreased the expression of activated matrix metalloproteinase 2 (MMP-2) and matrix metalloproteinase 9 (MMP-9), and also suppressed their activity. In addition, PSS was found to decrease the level of Vimentin in B16-F10 cells, which is known to participate in the epithelial-mesenchymal transition. Notably, PSS did not elicit any changes in cancer cell viability. Based on the results above, we conclude that PSS might be a potential drug to regulate the tumor microenvironment in order to facilitate the recovery of melanoma patients.

Baicalin protects human retinal pigment epithelial cell lines against high glucose-induced cell injury by up-regulation of microRNA-145.

BACKGROUND: Diabetic retinopathy (DR) is a common complication of diabetes mellitus, which is a major reason of blindness. Baicalin (BAI) is a flavonoid extracted from Scutellaria baicalensis, whose pharmacological characterizes have been widely reported in various diseases. However, it remains unclear the effect of BAI on DR. The study aimed to confirm the protective effect of BAI on DR. METHODS: ARPE-19 cells and HRMECs were exposed to the high glucose (HG) environment to construct a cell injury model. After treatment with HG and BAI, cell viability, apoptosis, inflammatory cytokines and ROS generations were determined in ARPE-19 cells and HRMECs. Subsequently, microRNA-145 (miR-145) inhibitor and its negative control were transfected into ARPE-19 cells, and the regulatory effects on HG-and BAI-co-treated cells were detected. NF-κB and p38MAPK signaling pathways were finally examined to state the underling mechanisms. RESULTS: HG treatment significantly induced ARPE-19 cells and HRMECs injury in vitro. BAI significantly promoted cell proliferation, reduced apoptosis, as well as inhibited the release of IL-1ß, IL-6, IL-8 and ROS level in HG-injured ARPE-19 cells and HRMECs. Additionally, the expression level of miR-145 was up-regulated in HG-and BAI-co-treated cells. More importantly, miR-145 inhibition reversed the protective effect of BAI on HG-injured ARPE-19 cells. Besides, we observed that BAI inhibited the activations of NF-κB and p38MAPK pathways by up-regulating miR-145. CONCLUSIONS: Results demonstrated that BAI exhibited the protective effect against HG-induced cell injury by up-regulation of miR-145.

Applying Statistical and Complex Network Methods to Explore the Key Signaling Molecules of Acupuncture Regulating Neuroendocrine-Immune Network.

The mechanisms of acupuncture are still unclear. In order to reveal the regulatory effect of manual acupuncture (MA) on the neuroendocrine-immune (NEI) network and identify the key signaling molecules during MA modulating NEI network, we used a rat complete Freund's adjuvant (CFA) model to observe the analgesic and anti-inflammatory effect of MA, and, what is more, we used statistical and complex network methods to analyze the data about the expression of 55 common signaling molecules of NEI network in ST36 (Zusanli) acupoint, and serum and hind foot pad tissue. The results indicate that MA had significant analgesic, anti-inflammatory effects on CFA rats; the key signaling molecules may play a key role during MA regulating NEI network, but further research is needed.

Studies on the binding properties of Zn2+ ion to quercetin and the antioxidant ac-tivi ties / 药学实践杂志

Objective To study the anti-oxidation properties of Zn2+-quercetin complexes .Methods The binding stoi-chiometric ratios and the binding constant of Zn2+ to quercetin were measured with UV-Vis spectroscopy .The binding sites on quercetin were determined via1 H NMR spectroscopy .The antioxidant activities of Zn2+-quercetin complexes were compared to quercetin by scavenging DPPH radical method .The binding ratio of Zn2+ to quercetin depends on neutralization of phenol groups of quercetin .Results The binding ratio of Zn2+ to quercetin is 1:2 when less than two OH groups were deprotonated . The binding ratio is 1:1 when more than three OH groups were deprotonated .The apparent binding constant is 2 .42 × 106 M -1 for the 1:1 Zn2+-quercetin complex .The 3′-OH and 4′-OH of quercetin are involved in the Zn2+ binding .The scavenging DPPH radical activity of Zn2+-quercetin complex is 2 .3 times of quercetin .Conclusion These results provide a new insight to expand applications of this traditional Chinese medicine .

Effects of Dendrobium huoshanense on expressions and activities of hepatic microsomal cytochrome P450s in mice / 中国中药杂志

This study was carried out to investigate the effect of oral administration of Dendrobium huoshanense on the expressions and activities of hepatic microsomal cytochrome P450s in mice, and to provide a reference for the evaluation of drug-drug interactions between D. huoshanense and clinical drugs. The C57BL/6 mice were randomly divided into blank control group, D. huoshanense low dose group (crude drug 1.25 g·kg⁻¹), D. huoshanense high dose group (crude drug 7.5 g·kg⁻¹), and phenobarbital positive control group (0.08 g·kg⁻¹). Each group was intragastrically administered with drugs for 2 weeks. The mice were sacrificed and their liver microsomes were prepared. The expressions of major subtypes of P450 enzyme were determined by Western blot and the probe drugs were used to detect the enzyme activities of P450 subtypes with protein expression changes. Western blot analysis showed that the protein expressions of CYP1A1, CYP1A2 and CYP2B in liver tissues were up-regulated in D. huoshanense-treated group. In vitro enzyme activity tests showed that there were no significant difference in metabolism of 7-ethoxyresorufin (a probe drug for CYP1A1) and bupropion (a probe drug for CYP2B) between D. huoshanense group and control group. The metabolism of phenacetin (a probe drug for CYP1A2) showed a statistical difference in rate Vmax, and it was significantly increased by approximately 20% in D. huoshanense group as compared with the blank control group, and the clearance CLint in treated group was also increased by about 32%. Therefore, oral administration of D. huoshanense had no effects on the activities of most hepatic P450 enzymes in mice, with no drug-drug interaction related to the P450 enzyme system in most clinical drugs theoretically. However, oral administration of D. huoshanense may accelerate the metabolism of CYP1A2-catalyzed drugs, which needs to be considered in clinical practice.

New nanomicelle curcumin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment.

CONTEXT: A stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics. OBJECTIVES: The objective of this article was to describe a novel curcumin containing a nanomicelle formulation using a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer. METHODS: Nanomicelle curcumin was formulated and optimized and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vitro cellular uptake/in vivo corneal permeation, and in vitro antioxidant activity/in vivo anti-inflammatory efficacy. RESULTS: The solubility, chemical stability, and antioxidant activity were greatly improved after the encapsulation of the PVCL-PVA-PEG nanomicelles. The nanomicelle curcumin ophthalmic solution was simple to prepare and the nanomicelles are stable to the storage conditions, and it had good cellular tolerance. Nanomicelle curcumin also had excellent ocular tolerance in rabbits. The use of nanomicelles significantly improved in vitro cellular uptake and in vivo corneal permeation as well as improved anti-inflammatory efficacy when compared with a free curcumin solution. CONCLUSIONS: These findings indicate that nanomicelles could be promising topical delivery systems for the ocular administration of curcumin.

Influence of Traditional Chinese Medicine Five-element Music combined with language induction on the psychological status and quality of life among maintenance hemodialysis patients / 中国实用护理杂志

Objective To observe the influence of traditional Chinese Medicine (TCM) Five-element music combined with language induction on the psychological status and quality of life among maintenance hemodialysis patients. Methods A total of 66 maintenance hemodialysis patients were divided into the Five-element music group (n=34) and the routine care group (n=32) according to date of hemodialysis. The routine group accepted routine care. The music group accepted the intervention of traditional Chinese Medicine Five-element music combined with language induction on the basis of routine care. Four weeks later, the changes of Hospital Anxiety Depression Scale (HAD), the MOS item Short From Health Survey (SF- 36) were observed to assess the effect before and after the intervention. Results HAD comparison in the group: After 4-week intervention, in Five-element music group, the depression and anxiety score of HAD and HAD total score were 3, 5, 9 (meadian score), which had improved significantly than before, which were 4, 7, 12 (meadian score), the difference was significant (Z=-2.645,-2.927,-3.220, P0.05). SF-36 comparison in groups: After 4-week intervention, in Five-element music group, the physical, physiological function,overall health, energy status, social function, emotional function, mental health factors of SF-36 scored 63, 88, 74, 41, 75, 75, 100, 80 (meadian score), which had improved significantly compared with before, which were 45, 0, 68, 40, 58, 75, 17, 72 (meadian score), the difference was significant (Z=-3.895--2.027, P0.05). After 4 weeks, the routine group′s each factor score had no significant difference compared with before (P > 0.05). Conclusions TCM Five-element music has a certain effect on improving the psychological status and the quality of life of the patients in maintenance hemodialysis.

Effect of Ginkgo Biloba Extract on the Pharmacokinetics and Metabolism of Clopidogrel in Rats.

Ginkgo biloba extract (GBE), a traditional herbal product used worldwide as both medicine and supplement, is often supplied with clopidogrel for the treatment of cerebrovascular diseases. The aim of the current study was to explore the effect of GBE on the metabolism and pharmacokinetics of clopidogrel. The in vitro study using rat liver microsomes revealed that GBE significantly induced the conversion of clopidogrel into its active metabolite. The effect of GBE on the pharmacokinetics of clopidogrel was also investigated in vivo. Compared to rats without GBE pretreatment, administration of 4 mg/kg, 20 mg/kg, and 100 mg/kg of GBE significantly decreased the Cmax and the AUC0-∞ of clopidogrel in a dose-dependent manner. As expected, pretreatment of high dose GBE significantly increased the Cmax and AUC0-∞ of the clopidogrel active metabolite. However, no marked change was observed following medium and low dose of GBE, suggesting that the biotransformation of clopidogrel was altered differently by high dose of GBE. Our study suggested that the awareness of the potential herb-drug interactions between GBE and clopidogrel should be increased in clinical practice. Copyright © 2016 John Wiley & Sons, Ltd.

The evaluation on embryotoxicity of Dipsaci Radix with mice and embryonic stem cells.

ETHNOPHARMACOLOGICAL RELEVANCE: Dipsaci Radix (DR), the dried root of Dipsacus asper Wall. ex Henry, has been used to treat pregnant disorders for thousands of years, and currently has been ranked as the first selective herb for prevention of miscarriage clinically; however, there is no sufficient evidence so far to assess its safety. The purpose of this study was to examine the impacts of DR aqueous extracts on embryonic development with mice and embryonic stem cells (ESCs). MATERIAL AND METHOD: In a segment II study, pregnant ICR mice were randomly assigned into 5 groups, i.e. mice were orally treated with DR aqueous extracts at dosages of 0 (distilled water, as negative controls (G1 group)), 2, 8, 32 g/kg/d (G2, G3, G4 group), and vitamin A (as positive controls (G5 group)) respectively. Maternal and embryo-fetal parameters were evaluated after cesarean section. The fetal skeletal development was further assessed with the alizarin red S and H&E staining and fluorescent imaging. Meanwhile, IC50 values for both ESCs and 3T3 cells were detected with MTT assays. RESULT: Compared to G1 group, the maternal body-weight in G3 and G4 groups was significantly lower (P<0.05-0.001), and the fetal malformation rate increased in G2, G3 and G4 groups as a dose-dependent manner, although a statistical significance was only reached in G4 group (P<0.001). The morphologic and histochemistry abnormalities of fetal skeletal development such as delayed osteogenesis and mineralization in the cartilaginous tissue were found after DR treatments (32 g/kg/d). There was no significant difference between IC50 ESC (6.826 ± 0.311 mg/ml) and IC50 3T3 (5.132 ± 0.142 mg/ml, P>0.05). CONCLUSION: DR aqueous extracts at the dosage of 8 or 32 g/kg/d (4.3 or 17.2 folds of recommended daily-dosage for adult human respectively) might cause adverse impacts in maternal healthy and embryo-fetal development. It suggests that high-dose and long-term administration of DR preparations should be unsafe to pregnant women.

Clinical Observation of Acupuncture-moxibustion plus Moving Cupping on the Back for Sub-health in the Undergraduates / 上海针灸杂志

Objective To observe the clinical efficacy of acupuncture-moxibustion plus moving cupping on the back in treating sub-health in the undergraduates. Method According to the theory of preventive treatment in the Chinese medicine, 30 undergraduates with sub-health were treated by acupuncture at Baihui (GV20), Guanyuan (CV4), and bilateral Zusanli (ST36), plus moving cupping to the Governor Vessel, totally for 20 d. The Self-rating Sub-health Scale (SRSHS) was adopted for evaluation before and after intervention, for observing the clinical efficacy. Result Of the 30 subjects, 14 were recovered, 14 showed effective, 2 failed, and the total effective rate was 93.3%. The SRSHS score dropped significantly after intervention (P＜0.001). The psychological factor responded most significantly to the intervention, followed by the physical factor, while the social function factor didn’t show a significant change. Conclusion Acupuncture-moxibustion plus moving cupping is significantly effective in improving and treating the sub-health state in the undergraduates.

Novel mucoadhesive polysaccharide isolated from Bletilla striata improves the intraocular penetration and efficacy of levofloxacin in the topical treatment of experimental bacterial keratitis.

OBJECTIVES: The objective of the present study was to evaluate a novel mucoadhesive polymer extracted from Bletilla striata for ocular delivery of 0.5% levofloxacin in rabbits, and to determine its improved efficacy against experimental keratitis. METHODS: B. striata polysaccharide (BsP) was subjected to cell cytotoxicity and ferning tests. The pharmacokinetics and bioavailability of topically applied 0.5% levofloxacin-BsP eye drops was investigated and compared with 0.5% levofloxacin eye drops (Cravit). Experimental Staphylococcus aureus keratitis was induced and treated with levofloxacin or levofloxacin-BsP eye drops. KEY FINDINGS: BsP markedly increased the proliferative capacity of a human corneal epithelial [corrected] cell line. The ferning test showed that BsP exhibited optimal performance as a tear fluid. The polysaccharides significantly increased intra-aqueous penetration and corneal accumulation in rabbits. Treatment with levofloxacin-BsP reduced the number of organisms more significantly than eye drops containing levofloxacin alone. CONCLUSIONS: BsP appears to be a promising candidate as a vehicle for topical ophthalmic drug delivery, especially for antibiotics.

Clinical evaluation of electronic dental analgesia during ultrasonic scaling / 中华口腔医学杂志

<p><b>OBJECTIVE</b>To evaluate the effect of electronic dental analgesia (EDA) device--Team Up Duo during ultrasonic scaling.</p><p><b>METHODS</b>The clinical trial was conducted as a randomized double-blind split-mouth design. Eighty-one patients requiring ultrasonic scaling were selected as subjects. Patients received treatment using the EDA device either in an active or an inactive state in paired quadrants. The patients scored their pain/discomfort levels with visual analog scale (VAS) after each procedure and filled a questionnaire.</p><p><b>RESULTS</b>In questionnaire, 79.0% patients felt EDA could relieve pain/discomfort during ultrasonic scaling. But the double-blind test showed that Team Up Duo was effective in 46.9% patients overall. The effective rate was 55.1% and 34.4% in groups with or without attachment loss, respectively. In CP group, the success rate of EDA was not statistically significantly different between the groups according to sex, age or site.</p><p><b>CONCLUSIONS</b>When using Team Up Duo during ultrasonic scaling, most patients subjectively believed that it was effective for controlling pain. In fact, this EDA device was effective in partial patients.</p>

The in vivo formation of cementum-like tissue by bovine cementoblasts / 中华口腔医学杂志

<p><b>OBJECTIVE</b>To test the bovine cementoblasts (CBs) cementum-forming ability in vivo.</p><p><b>METHODS</b>Root fragments of newborn bovine freshly extracted mandibular incisor were cultured routinely and 4th-5th passages of CBs were harvested. CBs were then cultured in the medium supplemented with 50 mg/L alpha-ascorbic acid and 10 mmol/l beta-glycerolphosphate to form a thick layer as tissue engineering scaffold for cementum formation. Collagen membrane was used as control scaffold. 2 x 10(6) cells were attached to the CBs-made carrier as well as collagen membrane scaffolds and transplanted subcutaneously into immunodeficient mice. Transplants were harvested at 7th week. Histological sections were stained with HE, alizarin red S and van Kossa methods as well as monoclonal Ab against bovine cementum attachment protein (CAP).</p><p><b>RESULTS</b>CBs-made scaffold supported more cementum-like tissue (CLT) formation than collagen-made scaffold. The CLT formed on CBs scaffold was partly calcified with embedded cells. Uncalcified cementoid-like material could be seen on the surface and was encircled by cubical CB-like cells. The CLT was also positive to CAP and van Kossa staining.</p><p><b>CONCLUSIONS</b>These results suggest that the bovine CBs can form cementum-like tissue. The cell-made carrier is a better scaffold than collagen membrane.</p>