Hypolipidemic activity of Phellinus rimosus against triton WR-1339 and high cholesterol diet induced hyperlipidemic rats

Patients with the risk for atherosclerotic disease will be targeted to reduce the existing hyperlipidemia. The hypolipidemic activity of Phellinus rimosus was studied using triton WR-1339 and high cholesterol diet (HCD) induced models. The triton induced elevated lipid profile was attenuated by P. rimosus or standard drug atorvastatin. Similarly, administration of P. rimosus along with HCD significantly decline serum triglyceride, total cholesterol, low-density lipoprotein, with elevating the high-density lipoprotein. Thiobarbituric acid reacting substances in heart and liver significantly decreased; where as activity of enzymatic antioxidants and level of reduced glutathione were significantly increased. In both models, P. rimosus extract showed a significant ameliorative effect on the elevated atherogenic index as well as LDL/HDL-C ratio. The hypolipidemic activity of P. rimosus can be ascribed to its inhibitory effect on the liver HMG CoA reductase activity. The results suggest the possible therapeutic potential of this fungus as hypolipidemic agent.     

三养胶麦减肥、降脂及降血糖作用的实验研究

目的对三养胶麦成分进行减肥、降血脂、降血糖动物实验研究。方法通过喂养营养饲料建立大鼠肥胖模型,观察三养胶麦成分的减肥作用;通过喂养高脂饲料建立脂代谢紊乱大鼠模型,观察三养胶麦成分的降脂作用;通过尾静脉注射四氧嘧啶制备糖尿病小鼠模型,观察三养胶麦成分的降血糖作用。结果减肥实验中三养胶麦成分各剂量组大鼠体重明显低于模型组,且高、中剂量组体脂及体脂/体重指数明显低于模型组,差异有显著性意义（P〈0.05或P〈0.01）;降脂实验中三养胶麦成分高、中剂量组体重、血清三酰甘油（TG）含量明显低于模型组,差异有显著性（P〈0.05或P〈0.01）;降糖实验中三养胶麦成分高剂量组空腹血糖明显低于模型组,差异有显著性（P〈0.05）,但糖耐量实验中各组AUC没有显著性差异（P〉0.05）。结论三养胶麦成分具有辅助减肥、降血清三酰甘油及降空腹血糖的保健作用。     

NLRP3基因敲除增强芹菜素对triton-WR 1339所致高脂血症的降血脂及抗炎作用研究

目的探讨NLRP3对芹菜素降血脂和抗炎作用的干预及调控机制。方法采用Triton-WR1339对野生型(widetype,WT)C57BL/6小鼠和NLRP3-/-小鼠致高脂血症,给药组连续5 d灌胃给予芹菜素6.25 mg·kg^-1,收集血样及肝脏,测定血清中TC、TG、HDL、LDL;肝脏进行HE染色分析;ELISA测定血清中IL^-1β、IL-6、MCP-1含量。RT-qPCR测定肝脏中NLRP3、IL-4、ASC、CD36、CYP7A1、FGF21的mRNA表达水平。结果与NLRP3-/-模型组相比较,芹菜素降低NLRP3-/-模型小鼠血清TC、TG、LDL-C、IL^-1B、IL-6、MCP-1含量,提高HDL-C含量(P<0.05),减少肝脏脂肪病变比例;芹菜素对WT模型小鼠未见此作用。芹菜素均能上调WT和NLRP3-/-模型小鼠CD36、vLDLR的表达,抑制ASC、IL-4表达(P<0.05)。芹菜素仅调控NLRP3-/-模型小鼠的FGF21、CYP7A1的表达(P<0.05),对WT模型小鼠无作用。结论NLRP3基因敲除增强低剂量芹菜素改善Triton-WR 1339所致的高脂血症及炎症等症状。NLRP3基因敲除增强芹菜素调控血脂作用的机制可能为:NLRP3炎症小体缺失,从而增强芹菜素对FGF21/CYP7A1信号通路的调控相关。     

Screening and analysis of bioactive compounds in traditional Chinese medicines using cell extract and gas chromatography-mass spectrometry

As the cost of drug development is always many times more than that of drug discovery, predictive methods aiding in the screening of bioavailable drug candidates are of profound significance. In this paper, a novel method for screening bioactive compounds from traditional Chinese medicines (TCMs) was developed by using living cell extract and gas chromatography (GC)-mass spectrometer (MS). The method was validated by using elemene emulsion injection (EEI), a typical TCM with known active compound, to interact with murine ascites hepatocarcinoma cell strain with high metastatic potential (HCa-F). Finally, the method was applied to screen the bioactive compounds from multi-component zedoary turmeric oil and glucose injection (ZTOGI). After HCa-F cells was incubated in ZTOGI, ethyl acetate (EtOAc) was used to extract the compounds in the cells for GC-MS analysis. Fourteen compounds were detected in the desorption eluate of HCa-F cell extract of ZTOGI, and further identified by MS. Curzerene and beta-elemene were found to be two major bioactive compounds in ZTOGI. These results show that the method developed may be applied to quickly screen the potential bioactive components in TCMs interacting with the target cells.     

Possible antidiabetic and antihyperlipidaemic effect of fermented Parkia biglobosa (JACQ) extract in alloxan-induced diabetic rats

1. The hypoglycaemic effect of fermented seeds of Parkia biglobosa (PB; African locust bean), a natural nutritional condiment that features frequently in some African diets as a spice, was investigated in the present study in alloxan-induced diabetic rats. Its effect was compared with that of glibenclamide (Daonil; Sanofi-Aventis, Paris, France), a reference antidiabetic drug. The effects of PB on lipid profiles were also examined. 2. In order to assess the hypoglycaemic and hypolipidaemic effects of aqueous and methanolic extracts of PB on experimental animals, fasting plasma glucose (FPG), total cholesterol, triglyceride, high-density lipoprotein (HDL) and low-density lipoprotein (LDL) were determined. In addition, the weight of each animal was determined to assess any possible weight gain or loss in the experimental animals (diabetic rats treated with Daonil (group C), the aqueous extract of PB (group D) or the methanolic extract of PB (group E)) compared with control groups (non-diabetic (group A) and non-treated diabetic (group B)). 3. A single dose of 120 mg/kg, i.v., alloxan administered to rats resulted in significant increases in the FPG (P < 0.001) of test animals compared with controls. However, dietary supplementation with PB (6 g/kg extract for 4 weeks administered orally using an intragastric tube) ameliorated the alloxan-induced diabetes in a manner comparable with that of the reference antidiabetic drug glibenclamide. Aqueous and methanolic extracts of PB (6% w/w) elicited 69.2% and 64.4% reductions, respectively, in FPG compared with 70.4% in 0.01 mg/150 g glibenclamide-treated rats. 4. Although animals treated with the aqueous extract of PB gained weight in manner similar to normal controls, animals given the methanolic extract and glibenclamide lost weight in manner similar to non-treated diabetic rats. In addition, high levels of HDL and low LDL were observed in animals treated with the aqueous extract of PB, a pattern similar to that seen in normal controls. Low levels of HDL and high levels of LDL were observed in animals treated with the methanolic extract of PB, a pattern similar to that seen in non-treated diabetic controls. 5. The results of the present study demonstrate that both aqueous and methanolic extracts of fermented seeds of PB exert a hypoglycaemic effect; hence, PB has an antidiabetic property. However, only the aqueous extract of PB ameliorated the loss of bodyweight usually associated with diabetes. Although the aqueous extract has a favourable lipid profile, which is probably an indication of its possible anti-arteriogenic property (hypertension and ischaemic heart diseases being common complications in diabetes mellitus), the methanolic extract shows possible contraindication to ischaemic heart diseases.     

Optimization of ultrasonic-assisted extraction for bioactive compounds in Rubus ellipticus fruits: An important source for nutraceutical and functional foods

Bioactive compounds of Rubus ellipticus fruits are known for their potential in nutraceutical and functional food; however, systematic investigation on optimization of extraction conditions for improving yield is lacking. In the present study, extraction of bioactive compounds was performed using Plackett-Burman (PBD) and Central Composite Design (CCD). Parameters such as solvent to sample ratio, methanol concentration, and extraction temperature significantly (p < 0.05 and p < 0.001) influenced bioactive compounds extraction under linear, quadratic and interactive effects. The model predicted values of bioactive compounds and antioxidant activity were found close to the experimental value signifying the least coefficient of variation. Further, regression analysis showed a high coefficient of determination (R²) and a non-significant lack of fit. High-performance liquid chromatography equipped with a photodiode detector (HPLC- PDA) analysis detected the presence of seven bioactive compounds under optimal extraction conditions, among which catechin was maximum (27.67 mg/g DW). Results showed 35–99 percent improvement in yield to conventional studies and earlier reports on the species. The optimized process can further be upscaled for harnessing maximum benefits of the species in nutraceutical and energy supplement development program at an industrial scale.     

几种香茶菜属二萜化合物对自由基导致线粒体损伤的保护作用

目的了解香茶菜属二萜类化合物冬凌草甲素（Ｏｒｉｄ）、腺花香茶素（Ａｄｅ）、黄花香茶菜素（Ｓｃｕｌ）是否具有抗氧化作用。方法用分光光度法测定脂质过氧化物丙二醛（ＭＤＡ）含量及线粒体肿胀度。用荧光分光光度法测定线粒体膜流动性。结果Ｏｒｉｄ,Ａｄｅ,Ｓｃｕｌ４０,８０,１６０μｍｏｌ·Ｌ－１抑制铁－半胱氨酸（Ｆｅ２＋－Ｃｙｓ）引起的肝线粒体ＭＤＡ形成,并呈剂量依赖关系。Ｏｒｉｄ,Ａｄｅ,Ｓｃｕｌ１６０μｍｏｌ·Ｌ－１抑制肝线粒体膜流动性下降（Ｐ值分别为２．２９７±０．０２２,０．３８９±０．００９,０．３８２±０．０１３,Ｆｅ２＋－Ｃｙｓ的Ｐ值为０．４２３±０．０１４）;Ａｄｅ１６０μｍｏｌ·Ｌ－１还可抑制脂质过氧化引起的肝线粒体肿胀。结论Ｏｒｉｄ,Ａｄｅ,Ｓｃｕｌ可能通过抑制脂质过氧化而产生抗氧化作用     

Ethanol extract of the mushroom Coprinus comatus exhibits antidiabetic and antioxidant activities in streptozotocin-induced diabetic rats

ContextEdible mushrooms have a long history of use in traditional Chinese or Japanese medicine. Coprinus comatus (O.F. Müll.) Pers. (Agaricaceae) contains antioxidant and antidiabetic agents.ObjectiveTo identify the benefits of ethanol extracts of the C. comatus fruit body in streptozotocin-induced hyperglycaemic rats by evaluating their blood glucose, glycosylated haemoglobin (HbA1c), insulin, glucagon-like peptide-1 (GLP-1), dipeptidyl peptidase-4 (DPP-4), and glutathione (GSH) levels, with and without extract administration.Materials and methodsWistar rats were either left untreated or were administered 45 mg/kg body weight (BW) streptozotocin; 45 mg/kg BW metformin; or 250, 500, or 750 mg/kg BW extract for 14 days. The blood glucose, GLP-1, DPP-4, GSH, insulin, and HbA1c levels were determined. Data were analysed using analysis of variance and Duncan’s multiple range tests.ResultsPreliminary data showed that administration of C. comatus ethanol extract dose of 250, 500, and 750 mg orally has no toxicity effects after 24 h administration. The ethanolic extract of fruiting body of C. comatus considerably reduced the rat’s fasting blood glucose levels 26.69%, and DPP-4 6.97% at dose of 750 mg. The extract reduced HbA1c 4–4.30%, increased GLP-1 71.09%, GSH 11.19% at dose of 500 mg, and increased insulin levels 13.83%. Extracts contain bioactive compounds such as flavonoid, alkaloid, terpenoids, vitamins C and E, rutin, and saponin.ConclusionsThe C. comatus extract can be used as herbal medicine that reduces diabetic symptoms. Further investigation on C. comatus extracts should be conducted with gas chromatography-mass spectrometry to characterise the bioactive compounds.     

Inhibitory effect of aqueous extract of different parts of unripe pawpaw (Carica papaya) fruit on Fe2+-induced oxidative stress in rat pancreas in vitro

Abstract

Context: Carica papaya L. (Caricaceae) is widespread throughout tropical Africa; it is cultivated for its fruits and it is eaten in various ways.

Objective: This study sought to investigate the inhibitory effect of the aqueous extract of different parts of unripe pawpaw fruit on Fe²⁺-induced lipid peroxidation in rat’s pancreas in vitro.

Materials and methods: The aqueous extract of the unripe pawpaw fruit parts; peel (PG), seed (SG), flesh (FG), flesh with peel (FPG) and a combination of equal amount of all parts (CG) were prepared, the total phenolic content and the antioxidant activities of the extracts were then evaluated using various spectrophotometric methods.

Result: PG had the highest total phenol content (1.24?mg GAE/g), flavonoid content (0.63?mg QUE/g), reducing power (7.07?mg AAE/g) and Fe²⁺ chelating ability while the SG had the highest 1,1-diphenyl-2-picrylhydrazyl radical scavenging ability. Furthermore, all the extracts caused a significant decrease (p?<?0.05) in the malondialdehyde contents in the pancreas with SG (IC₅₀?=?4.25?mg/mL) having the highest inhibitory effect on Fe²⁺-induced lipid peroxidation.

Discussion and conclusion: This protective effect of the extracts on Fe²⁺-induced lipid peroxidation in rat pancreas could be attributed to their phenolic compounds and, the possible mechanism may be through their antioxidant activities. However, the effect of combination of different parts of unripe pawpaw fruit in equal amount (w/w) on the inhibition of Fe²-induced lipid peroxidation in rat pancreas exhibited additive properties.     

Protective effect of artichoke (Cynara scolymus) leaf extract against lead toxicity in rat

Abstract

Context: Artichoke, Cynara scolymus L. (Asteraceae), has many natural antioxidants and multiple pharmacological actions. Recent studies have shown that it has antitoxic activity.

Objective: Lead (Pb) is a dangerous environmental toxicant that induces a broad range of dysfunctions in human. This study evaluated the protective effect of the hydroethanolic extract of artichoke against altered biochemical parameters in rats fed with lead-containing diet.

Materials and methods: Thirty-two rats were randomly divided into four groups. The first (control) group received standard diet. The second, third and fourth groups received 500?mg lead/kg diet, 500?mg lead/kg diet plus 300?mg/kg b.w. artichoke extract daily, and 500?mg lead/kg diet plus 1?mg vitamin C/100?g b.w. daily for 6 weeks, respectively. Serum lead, lipoprotein profile, ALT (alanine transaminase), AST (aspartate transaminase), ALP (alkaline phosphatase), malondialdehyde (MDA) and liver histopathology assessments were conducted.

Results: Serum lead, triglyceride (TG), VLDL, ALT, AST, ALP and MDA levels decreased significantly (p?<?0.05) in the artichoke-treated group (35.85, 38.26, 38.38, 21.90, 12.81, 26.86 and 46.91%, respectively) compared to lead-intoxicated rats without treatment. No significant change was observed in serum lead, ALP and ALT between artichoke and vitamin C-treated groups (p?>?0.05). Furthermore, the liver histopathology in rats treated with artichoke showed a mild degree of lymphocyte infiltration that was relatively comparable to the control and vitamin C-treated groups.

Discussion and conclusion: These results clearly show that the artichoke extract in lead-poisoned rats has suitable chelating properties for the reduction of blood lead levels.     

Hypolipidemic and antioxidant effects of ethanol extract of Cassia fistula fruit in hyperlipidemic mice

Context: The plant Cassia fistula L. (Caesalpiniaceae) fruit was widely used by traditional practitioners to treat cardiovascular diseases (CVDs) in India. Hyperlipidemia is a lipid metabolism disorder and the major risk factor for the development of CVDs. Although most of the current hypolipidemic drugs are expensive and have potential side effects, the research focusing on natural alternative medicines is relevant.

Objective: To investigate the hypolipidemic and antioxidant effects of ethanol extract of C. fistula fruit (CFE) in high-fat diet (HFD) induced hyperlipidemia in mice.

Materials and methods: Oral administration of CFE at 100, 300 and 500?mg/kg body weight on HFD induced hyperlipidemia mice for 30 days. The standard drug atorvastatin (20?mg/kg) was used to compare the efficacy of CFE. Hypolipidemic effect was evidenced by the measurement of serum lipid profile and further confirmed by Oil Red O staining of adipose tissue. The hepatic and cardiac melondialdehyde (MDA) level and antioxidant enzyme activities including superoxide dismutase, catalase and glutathione peroxidase were determined.

Results: Treatment with CFE at different doses has significantly restored the levels of serum lipid, MDA and enzymes activities in the liver and heart of hyperlipidemia mice. Oil Red O staining of visceral adipose tissue has shown marked reduction of lipid accumulation in adipocytes; whereas, administration of CFE at 500?mg/kg showed remarkable (p?<?0.001) hypolipidemic and antioxidant effects in HFD fed mice.

Conclusion: C. fistula fruit demonstrated hypolipidemic and antioxidant properties in vivo and the results corroborate the use of this plant in traditional medicine for cardiac ailments.     

Green approach to extract bioactive compounds from orange peel employing hydrophilic and hydrophobic deep eutectic solvents

Consumer interest in natural products with advantageous biological impacts on their health has increased in recent years. Therefore, academic and industrial communities have concentrated their research on developing sustainable techniques for extracting bioactive compounds from natural resources. In the present study, extracts rich in bioactive compounds from orange peel were obtained using novel hydrophilic and hydrophobic deep eutectic solvents (DESs). Bioactive compounds such as carotenoids and polyphenols, their stability, antioxidant capacity, permeability, and biological activity were determined to consider their inclusion in food formulations. The results demonstrated that the highest total carotenoid values were obtained with hydrophobic DESs using DL-Menthol: camphor (163.5 ± 1.1 mg/100g_fw), DL-Menthol: Eucalyptol (168.7 ± 1.7mg/100g_fw), and lauric acid: octanoic acid (153.1 ± 7.1 mg/100g_fw). Total polyphenols were higher in hydrophilic DESs such as proline: malic acid (282.8 ± 7.3 mg/100g_fw). The antioxidant values showed that hydrophobic extracts have higher antioxidant activity than traditional solvents. Carotenoid stability was also improved using DL-Menthol: camphor, while lactic acid: glucose and proline: malic acid showed a better capacity to stabilize polyphenols. To simulate carotenoid and polyphenol permeation, the Parallel Artificial Membrane Permeability Assay (PAMPA) was used and demonstrated that DESs can enhance the permeability of these bioactive compounds. Biological tests were also performed, and the antiproliferative effect in HeLa cells showed only 26.70% cell viability in DL-Menthol: camphor extracts. Based on the presented results, DESs can be used to extract hydrophilic and hydrophobic compounds from orange peels, and the obtained extracts could be included in food formulations, avoiding the solvent elimination process.     

Subcritical water extraction and characterization of bioactive compounds from Haematococcus pluvialis microalga

In this work, extraction and characterization of compounds with antioxidant and antimicrobial activity from Haematococcus pluvialis microalga in red phase have been carried out. To do this, subcritical water extraction (SWE) has been combined with analytical techniques such as HPLC–DAD, HPLC–QqQ-MS and GC–MS and in vitro assays (i.e., for antioxidant and antimicrobial activity). The effect of the extraction temperature (50, 100, 150 and 200 °C) and solvent polarity has been studied in terms of yield and activity of the extracts. Results demonstrate that the extraction temperature has a positive influence in the extraction yield and antioxidant activity. Thus, the extraction yield achieved with this process was higher than 30% of dry weight at 200 °C as extraction temperature. Moreover, the extract obtained at 200 °C presented the highest antioxidant activity by far, while temperature does not seem to significatively affect the antimicrobial activity. Chemical composition was determined by HPLC–DAD, HPLC–QqQ-MS and GC–MS. Short chain fatty acids turned out to be responsible of the antimicrobial activity, whereas the antioxidant activity was correlated to vitamin E (present exclusively in the 200 °C extract), together with simple phenols, caramelization products and possible Maillard reaction products obtained during the extraction at high temperatures.     

辣木叶水提物对油酸钠-钠棕榈酸酯诱导的HepG2细胞脂质代谢及抗氧化能力的影响

目的 探讨辣木叶水提物（MOLAE）对脂肪堆积人HepG2细胞的调节作用。方法 制备MOLAE冻干粉；通过CCK-8法检测油酸钠-钠棕榈酸酯（O-P）对HepG2细胞活力的影响、油红O染色检测O-P对细胞脂质堆积的影响、试剂盒法检测O-P对细胞三酰甘油（TG）、总胆固醇（TC）水平的影响，筛选O-P诱导HepG2细胞脂质代谢异常模型的作用浓度及时间；CCK-8法检测辛伐他汀、MOLAE对HepG2细胞活力的影响，筛选安全作用浓度；设立对照组、模型组、辛伐他汀（阳性药，15 μmol·L^-1）组和MOLAE（3.125、6.250、12.500、25.000、50.000 μg·mL^-1）组，除对照组外，其他各组均给予0.4-0.2 mmol·L^-1的O-P诱导细胞脂质沉积，诱导3 h后开始给药，干预24 h后，CCK-8法检测细胞活性，油红O染色观察细胞中脂滴形成情况，试剂盒法测定细胞中TG、TC、谷胱甘肽（GSH）、超氧化物歧化酶（SOD）及丙二醛（MDA）水平。结果 确定造模方式为：0.4-0.2 mmol·L^-1的O-P作用HepG2细胞3 h后开始给药；10、15 μmol·L^-1的辛伐他汀和3.125～100.000 μg·mL^-1的MOLAE作用于HepG2细胞24、48 h后，不影响细胞活力。与模型组比较，不同浓度的MOLAE（3.125、6.250、12.500、25.000、50.000 μg·mL^-1）均能降低TG、TC、MDA水平（P<0.05、0.01），显著升高GSH、SOD水平（P<0.05、0.01）。油红O染色结果表明，辛伐他汀组和MOLAE组（12.5、25.0 μg·mL^-1）脂滴堆积现象均较模型组有明显改善。结论 MOLAE能够降低O-P诱导的HepG2细胞中TG、TC水平，提高GSH、SOD水平和降低MDA水平，减少细胞中脂质堆积的现象。     

Characterization of bioactive compounds and ameliorative effects of Ceratonia siliqua leaf extract against CCl4 induced hepatic oxidative damage and renal failure in rats

Ceratonia siliqua is a typical Mediterranean plant, mainly used in food and Tunisian traditional folk medicine. Among the tested extracts, the ethyl acetate fraction (EACs) exhibited the highest total phenolic and flavonoids content. The antioxidant activity in vitro systems showed a more significant potent free radical scavenging activity of this extract than other analysis fractions. The HPLC finger print of EACs active extract showed the presence of six phenolic compounds. The in vivo results showed that oral administration of CCl₄ enhanced levels of hepatic and renal markers (ALT, AST, ALP, LDH, γ-GT, urea and creatinine) in the serum of experimental animals. It also increased the oxidative stress markers resulting in increased levels of the lipid peroxidation with a concomitant decrease in the levels of enzymatic antioxidants (SOD, CAT, GPx) in both liver and kidney. The pre-treatment of experimental rats with 250 mg/kg (BW) of the EACs, by intraperitoneal injection for 8 days, prevented CCl₄ induced disorders in the levels of hepatic and kidney markers. The biochemical changes were in accordance with histopathological observations suggesting a marked hepatoprotective and nephroprotective effect of the EACs extract.     

Regulatory/modulatory effect of prune essence concentrate on intestinal function and blood lipids

Context: Prunus domestica Linn (Rosaceae) has been considered a functional food, owing to its various pharmacological activities, including antioxidant, anti-inflammatory, antidiabetic and anticancer.

Objective: This placebo-controlled, randomized study was framed to check the beneficial activity of prune essence concentrates (PEC) in corroboration with intestinal function and lipid profile in mildly hypercholesterolemic subjects.

Materials and methods: Sixty healthy mild hypercholesterolemic subjects were randomly chosen and segregated into three groups as placebo (consume 50?mL of simulated prune drink), PEC I (consume 50?mL of PEC/day) and PEC II (consume 100?mL of PEC/day) for 4 weeks with 2 weeks of follow-up without PEC consumption.

Results: Intake of PEC (I and II) for 4 weeks substantially ameliorated (p?Bifidobacterium spp. (1.18- and 1.19-fold) and Lactobacillus spp. (1.07- and 1.16-fold), but markedly lowered (p?Clostridium perfringens (5.97 and 8.35%) and Escherichia coli (6.25 and 9.38%). Meanwhile, the total cholesterol (TC; 5.90 and 6.99%) levels and LDL-c (6.68 and 6.53%) were significantly reduced (p?p?Discussion and conclusion: Overall, the results suggest that the use of PEC may positively regulate the intestinal microflora and thereby effectively lower the TC levels and thus act as a hypocholesterolemic agent.     

Ameliorative and antioxidant effects of myrtle berry seed (Myrtus communis) extract during reflux-induced esophagitis in rats

Context Myrtle, Myrtus communis L. (Myrtaceae), is a medicinal plant well known for its richness in phenolic compounds and its beneficial effects for the treatment of gastrointestinal disorders.

Objective In the present work, the protective effect of the myrtle berry seed aqueous extract (MBSAE) against esophageal reflux (ER)-induced damage in esophagus mucosa as well as the mechanisms implicated was determined.

Materials and methods In this respect, adult male Wistar rats were used and divided into seven groups: Control, ER, ER?+?various doses of MBSAE, ER?+?famotidine or ER?+?gallic acid. The ER was induced and animals were per orally (p.o.) treated with MBSAE or reference molecules during 6 h. The phytochemical screening was determined using colourimetric analysis.

Results MBSAE is rich in total polyphenols and anthocyanins and exhibited an important in vitro antioxidant activity. In vivo, we firstly found that ER led to marked macroscopic and histopathological changes in esophagus. The results showed, also, that the ER was accompanied by a state of oxidative stress as assessed by an increase of lipid peroxidation, a decrease of the sulphhydryl groups and glutathione levels, as well as antioxidant enzyme activities depletion. MBSAE abrogated all morphological, histopathological and biochemical alterations. We showed also that ER increased esophageal calcium, hydrogen peroxide (H₂O₂) and free iron levels while MBSAE treatment protected against intracellular mediators deregulation.

Conclusion Our data suggest that MBSAE exerted a potential protective effect against ER-induced damage in rat esophagus, at least in part, due to its antioxidant properties.     

In vitro immunomodulatory activity and in vivo anti-inflammatory and analgesic potential with gastroprotective effect of the Mediterranean red alga Laurencia obtusa

Context: Red algae have been recognized as a rich natural source of compounds possessing interesting biological and pharmacological activities.

Objective: This work investigates anti-inflammatory, analgesic and gastroprotective activities of MeOH/CH₂Cl₂ crude extract and its fractions F1 (50% MeOH) and F2 (80% MeOH) from the whole alga plant Laurencia obtusa Hudson (Rhodomelaceae).

Materials and methods: Anti-inflammatory activity was evaluated in vitro using cytometric bead array (CBA) technology to follow up the secretion of tumour necrosis factor alpha (TNF-α) in lipopolysaccharide activated THP-1 monocytic cells at doses of 10–250?μg/mL and in vivo using carrageenan-induced paw oedema in Wistar rats at doses of 25, 50, 100 and 200?mg/kg. Crude extract and fractions were tested at the doses of 25, 50, 100 and 200?mg/kg for peripheral and central analgesic activity by acetic acid-induced writhing test and hot-plate method, respectively, in Swiss albino mice. Gastroprotective activity was evaluated using HCl/ethanol-induced gastric ulcer test in rats at doses of 25, 50, 100 and 200?mg/kg.

Results: Crude extract, F1 and F2 showed an interesting inhibition of TNF-α secretion with IC₅₀ values of 25, 52 and 24?μg/mL, respectively, and a significant anti-inflammatory activity in vivo (p?< 0.01), 3?h after carrageenan injection, the oedema inhibition was 55.37%, 52.18% and 62.86%, respectively, at the dose of 100?mg/kg. Furthermore, they showed a significant peripheral analgesic activity with 53.79%, 55.92% and 57.37% (p?< 0.01) of writhing inhibition, respectively. However, no significant activity was found in the hot-plate test. An interesting gastroprotective effect was observed with crude extract and its fractions F1 and F2 with a gastric ulcer inhibition of 65.48%, 77.42% and 81.29%, respectively, at the dose of 50?mg/kg.

Discussion and conclusion: These results suggest that L. obtusa might be used as a potential source of natural anti-inflammatory and analgesic agents with gastroprotective effect.     

Improved in vitro dissolution parameters and in vivo hypolipidemic efficiency of atorvastatin calcium through the formation of hydrophilic inclusion complex with cyclodextrins

An aim of the present study was to improve the dissolution of the inherently low water solubility hypolipidemic agent, Atorvastatin calcium (ATC), through the preparation and characterization of ATC with cyclodextrins (CDs) inclusion complexes employing different techniques. A second goal was to study the in vivo hypolipidemic efficacy of ATC‐complexes with enhanced dissolution characteristics. Inclusion complexation of ATC with β‐cyclodextrin (β‐CD) and hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) was evaluated in aqueous and solid states. ATC formed inclusion complexes with β‐CD and HP‐β‐CD depending to a great extent upon ATC ionization state. Evaporation and freeze‐drying were the most efficient techniques to achieve complexation. In contrast, kneading was an inefficient tool to create true inclusion complexes, which could reflect the hindrance of drug–CDs interactions in the semisolid medium. The ATC:CD ratio of 1:2 showed better dissolution characteristics compared to a 1:1 ratio. Moreover, the in vivo hypolipidemic activities of ATC‐CDs (β‐CD and HP‐β‐CD) complexes were greater (P<0.05) than the other investigated formulations. Thus the nature of the carrier did not play a critical role in the dissolution characteristics of the inclusion system. In contrast, the carrier molar ratio, and the employed complexation technique were found to be key factors in enhancing the ATC dissolution rate, yielding performances as well as the in vivo hypolipidemic efficacies. Drug Dev Res 72: 379–390, 2011. © 2011 Wiley‐Liss, Inc.     

虎杖水提液利胆保肝作用研究

目的初步研究虎杖水提液的利胆保肝作用。方法以大鼠胆管插管法,十二指肠给药,记录给药前1h,给药后1,2,3和4h胆汁流量及胆汁中胆红素(TBIL)和胆固醇(CHO)含量,观察虎杖水提液利胆作用;采用腹腔注射CCl4橄榄油溶液复制小鼠急性肝损伤模型,检测血清丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)含量,观察其对肝的保护作用。结果虎杖水提液可增加大鼠胆汁分泌量(P<0.05或P<0.01);可明显降低CCl4模型小鼠血清ALT和AST含量(P<0.05或P<0.01)。结论虎杖水提液具有利胆和保肝作用。