Hypocholesterolaemic mechanism of bitter melon aqueous extracts via inhibition of pancreatic cholesterol esterase and reduction of cholesterol micellar solubility

This study investigated the hypocholesterolaemic effects of bitter melon aqueous extracts (BMAE) in vitro, the inhibitory effects of BMAE on pancreatic cholesterol esterase (CEase) and incorporation of cholesterol into micelles were investigated. BMAE decreased the in vitro micellar solubility of cholesterol in a dose-dependent manner. The conformation of CEase was investigated by means of circular dichroism (CD) and fluorescence. The result revealed the decrease of α-helix contents, increase of β-sheet and exposure of aromatic amino acid residuals. The incorporation of cholesterol into micelles was inhibited by BMAE. A complex was observed by transmission electron microscopy (TEM), which indicated interaction between cholesterol and BMAE. The result revealed that BMAE can play a role in decreased intestinal cholesterol absorption via inhibition of CEase, and of micelle formation.     

Instrument-based Tests for Measuring Anterior Chamber Cells in Uveitis: A Systematic Review

ABSTRACT

Purpose

New instrument-based techniques for anterior chamber (AC) cell counting can offer automation and objectivity above clinician assessment. This review aims to identify such instruments and its correlation with clinician estimates.     

Immunomodulatory activity of Asparagus racemosus on systemic Th1/Th2 immunity: Implications for immunoadjuvant potential

Ethnopharmacological relevance

Roots of Asparagus racemosus Willd (Shatavari in vernacular) are widely used in Ayurveda as Rasayana for immunostimulation, galactogogue as also in treatment of conditions like ulcers and cancer. Various studies have indicated immunomodulatory properties of Shatavari root extracts and formulations.

Aim of the study

To study the effect of standardized Asparagus racemosus root aqueous extract (ARE) on systemic Th1/Th2 immunity of SRBC sensitized animals.

Materials and methods

We used HPTLC to quantify steroidal saponins (Shatavarin IV, Immunoside^®) and flow cytometry to study effects of ARE on Th1/Th2 immunity. SRBC specific antibody titres and DTH responses were also monitored as markers of Th2 and Th1 responses, respectively. We also studied lymphocyte proliferation. Cyclosporin, cyclophosphamide and levamisole were used as controls.

Results

Treatment with ARE (100 mg/(kg b.w. p.o.)) resulted in significant increase of CD3⁺ and CD4/CD8⁺ percentages suggesting its effect on T cell activation. ARE treated animals showed significant up-regulation of Th1 (IL-2, IFN-g) and Th2 (IL-4) cytokines suggesting its mixed Th1/Th2 adjuvant activity. Consistent to this, ARE also showed higher antibody titres and DTH responses. ARE, in combination with LPS, Con A or SRBC, produced a significant proliferation suggesting effect on activated lymphocytes.

Conclusion

The study suggests mixed Th1/Th2 activity of ARE supports its immunoadjuvant potential.     

Triterpenoid saponins, new metalloprotease snake venom inhibitors isolated from Pentaclethra macroloba.

We report here the antiproteolytic and antihemorrhagic properties of triterpenoid saponin inhibitors, named macrolobin-A and B, from Pentaclethra macroloba, against Bothrops snake venoms. The inhibitors were able to neutralize the hemorrhagic, fibrin(ogen)olytic, and proteolytic activities of class P-I and P-III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. Clotting and fibrinogenolytic activities induced by snake venoms and isolated thrombin-like enzymes were partially inhibited. Furthermore, the potential use of these inhibitors to complement antivenom therapy as an alternative treatment and/or used as molecular models for development of new therapeutical agents in the treatment of snake bite envenomations needs to be evaluated in future studies.     

兔眼后房型人工晶体置入后房水内丙二醛测定

应用ＴＢＡ荧光法检测了兔眼单纯晶体囊外摘除后和晶体囊外摘除并后房型人工晶体置入后房水内丙二醛含量，这二种手术后房水内丙二醛含量比正常眼显著增高（Ｐ＜０．００５，Ｐ＜０．００１）。结果提示前房内发生了脂质过氧化反应，这一发现有利于对眼内后房型人工晶体表面细胞反应及前膜形成进一步认识。     

Hypoglycaemic activity of Anthocleista vogelii (Planch) aqueous extract in rodents

The hypoglycaemic effect of Anthocleista vogelii was studied in mice, rats and rabbits. Aqueous extract of the plant obtained by infusion from finely pulverized root was used. The extract (100, 400 and 800 mg/kg) induced significant hypoglycaemic activity in a dose-related fashion at 2 h after oral administration in mice and rats with ED₂₅ of 250 mg/kg and 350 mg/kg respectively. The extract (800 mg/kg, orally) similarly induced statistically significant lowering of blood glucose levels at 8 h in normoglycaemic rabbits. The extract (400 mg/kg and 800 mg/kg, orally) also caused reduction of blood glucose levels in alloxan-induced diabetic animals. The results of this study indicate that the aqueous extract of the roots of Anthocleista vogelii possess favourable hypoglycaemic activity both in normo and hyperglycaemic animals compared to chlorpropamide as a standard.     

仙人掌提取物对小鼠血糖的影响

目的 :探讨仙人掌水性和酸性提取物对小鼠血糖的影响。方法 :糖尿病小鼠造模成功后分为 5组 :仙人掌酸提物 2个剂量组 (0 .5g·kg-1·d-1和 1.0g·kg-1·d-1) ,水提物 2个剂量组和优降糖组 (2 0 0mg·kg-1·d-1)。正常小鼠灌注等量生理盐水作为正常对照。 6组小鼠均连续给药 2 1d后测血糖。结果 :给药后仙人掌酸提物 2个剂量组血糖均较给药前降低 (P均 <0 .0 5 ) ,2个剂量组间差异无统计学意义 (P >0 .0 5 ) ,但 2组与优降糖组相比 ,P均 <0 .0 5 ;水提物 2个剂量组给药前后血糖无明显变化 (P >0 .0 5 )。结论 :仙人掌酸提物有降血糖作用     

抽空房水C3F8充填前房中期全眼球湿房角膜保存的实验研究

采用抽空房水Ｃ３Ｆ８（全氟丙烷）充填前房全眼球湿房保存角膜内皮细胞活性。通过内皮细胞显微照相、内皮细胞活性染色（锥蓝联合茜素红染色）、扫描电镜、保存后的兔角膜行实验性同种异体穿透角膜移植，证实保存７天内皮细胞结构完整，功能良好。     

Anthelmintic activity of some sudanese medicinal plants

The anthelmintic activity of aqueous extracts (0.25–50 mg/mL) from 14 plant species that represent seven families of the Sudanese flora was examined using the free living rhabditid nematode, Caenorhabditis elegans as a test organism. Extracts of Balanites aegyptiaca and Sesbania sesban were the most effective (LC₅₀, 0.8 and 8.0 mg/mL, respectively). Extracts of Albizzia anthelmintica, Cymbopogen narvatus, Abrus precatorius, Rhyncosia minima, Striga hermonthica and Anogeissus leiocarpa (LC₅₀, 9.5–84.6 mg/mL were less effective in this model test system. Extracts of six plant species, Albizzia malacophylla, Gardenia lutea, Physostigma mesoponticum, Salvadora persica, Xeromphis nilotica and Waltheria indica had no effect upon C. elegans survival.     

Analysis of Intestinal Perfusion Data for Highly Permeable Drugs Using a Numerical Aqueous Resistance—Nonlinear Regression Method

Purpose. To develop, validate and apply a method for analyzing the intestinal perfusion data of highly permeable compounds using the Numerical Aqueous Resistance (NAR) theory and nonlinear regression (NAR-NLR) and to compare the results with the well-established Modified Boundary Layer (MBL) Analysis. Methods. The NAR-NLR method was validated and the results were compared to the MBL analysis results using previously reported cephradine jejunal perfusion data. Using the Single Pass Intestinal Perfusion (SPIP) method, the concentration dependence of intestinal permeability was investigated for formycin B, proline, and thymidine, three compounds reported to be absorbed by carrier-mediated transport processes. The MBL and NAR-NLR analyses were then applied to the three sets of SPIP data. Results. The results demonstrate that the intrinsic MBL transport parameters were highly variable and, in one case, the analyses failed to give a statistically significant Michaelis constant. The MBL mean dimensionless wall permeabilities (P*_w) were greater than the NAR-NLR P*_w and were also highly variable. In all cases, the NAR-NLR variability was significantly lower than the MBL variability. The extreme variability in the MBL-calculated P*_w is due to the sensitivity of P*_w when the fraction of unabsorbed drug (C_m/C_o) is low or, alternatively, when P*_w approached the aqueous permeability, P*_aq. Conclusions. The NAR-NLR method facilitates the analysis of intestinal perfusion data for highly permeable compounds such as those absorbed by carrier-mediated processes at concentrations below their K_m. The method also allows for the use of a wider range of flow conditions than the MBL analysis resulting in more reliable and less variable estimates of intestinal transport parameters as well as intestinal wall permeabilities.