Assessment of the Antimetastatic Activity of Extracts of Filipedula ulmaria Depending on Extractant

Pharmaceutical Chemistry Journal - Three extracts were produced from the above-ground part of the meadowsweet Filipendula ulmaria (L.) Maxim. using water, 40% ethanol, and 70% ethanol. Comparative...     

Evaluation of anti-inflammatory and antinociceptive activities of Murraya exotica

Context:?Leaves of Murraya exotica L. (Rutaceae) are used for the treatment of various disorders such as cough, fever, and infectious wounds, as well as alleviating pains in folk medicine in southern China.

Objective:?The objectives of this study were to investigate the in vivo antinociceptive and anti-inflammatory activities of ethanol (70%) extracts and isolated compounds obtained from the dried leaves of M. exotica.

Materials and methods:?The antinociceptive activities were evaluated with the methods of acetic acid-induced writhing response and hot-plate latent pain response test. Carrageenan induced hind paw edema, xylene induced ear edema, and a rat knee osteoarthritis model were employed to measure the anti-inflammatory activities. The compounds were isolated using column chromatography and thin-layer chromatography, and the structures identified by ¹H NMR, ¹³C NMR, MS, and IR.

Results:?The ethanol (70%) extracts significantly decreased in the acetic acid-induced writhing response; increased in hot-plate latency; suppressed xylene induced ear swelling and the carrageenan-induced paw edema effectively. In the rat knee osteoarthritis model, the treatment of the ethanol (70%) extracts resulted in a significant increase in the activity of superoxide dismutase, an inhibition on inducible nitric oxide synthase activity, and a decrease in the contents of interleukin-1β and tumor necrosis factor-α of the rat serum. Following this, we explored the components of the ethanol (70%) extracts and isolated six known coumarins, including murracarpin, which exhibited the most potential in antinociceptive and anti-inflammatory activities.

Discussion and conclusion:?M. exotica displayed remarkable antinociceptive and anti-inflammatory activities.     

银杏叶提取物的树脂柱色谱脱酸工艺研究

目的 优化树脂柱色谱法脱除银杏叶提取物中总银杏酸的最佳工艺。方法 通过单因素和响应面法实验,以体积流量、洗脱剂乙醇体积分数、洗脱液接收体积为考察因素,以银杏叶提取物中总银杏酸去除率、总黄酮转移率和提取物收率的综合评分为指标,优化树脂柱色谱法脱除总银杏酸最佳工艺。结果 最佳工艺参数为体积流量1.2 BV/h,洗脱剂乙醇体积分数70%,洗脱液接收体积3 BV。结论 本工艺稳定、可行、重复性好,可作为银杏叶提取物树脂柱色谱脱酸工艺。     

Studies of the biological activity of an oil extract of the snakeflower Lamium album

An oil extract was prepared from the above-ground part of the snakeflower Lamium album; this contained a total chlorophyll derivative content of 0.46 ± 0.02 mg/ml. The extractant was a biphasic system consisting of ethanol and sunflower oil. Studies of the biological activities of the snakeflower oil extract were performed in models of hemolytic and iron-deficiency anemia. The antianemic activity of Lamium album L. was assessed in each of these models. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 42, No. 6, pp. 43–45, June, 2008.     

Chemical composition and biological activity of a fraction of meadowsweet extract

Studies of the chemical composition of a butanol fraction of an extract from the above-ground part of the meadowsweet in 70% ethanol yielded five substances which were flavonoids (quercetin, isoquercetin, quercetin 4′-glucoside, rutin) and phenolcarboxylic acids (gallic acid). The fraction was found to have nootropic actions, with antiamnestic, antihypoxic, antioxidant, and adaptogenic activities. Studies of the antioxidant properties of the individual compounds showed that isoquercetin, quercetin 4′-glucoside, and rutin were more active than dihydroquercetin and ascorbic acid.     

石蒜碱的纸层分离和分光光度测定

用95%酒精回流提取石蒜总生物碱,经用正丁醇:乙醇:氢氧化铵:水(90:10:1:97v/v)混合液的上层溶液为推进剂,进行上行纸层分离后,石蒜碱可以很好地与石蒜中其他生物碱分开。纸上的石蒜碱在萤光灯下呈蓝绿色斑点,斑点经酒精洗脱后,可在紫外分光光度计波长288毫微米处测其含量。本法的回收率为93.7±1.1%,样品分析时的平均百分偏差约为±5%。     

Gastroprotective activity of atractylenolide III from Atractylodes ovata on ethanol‐induced gastric ulcer in vitro and in vivo

Objectives The rhizome of Atractylodes ovata De Candolle is popularly used in traditional Chinese medicine to treat gastrointestinal diseases. However, the major gastroprotective compounds of A. ovata have not been identified. This study reports on the principal gastro‐ protective component of A. ovata. Methods Five sesquiterpenoids (atractylon, atractylenolides I, II, III and biatractylolide) were isolated from the extracts of A. ovata rhizome via silica gel column chromatography. The gastroprotective effects of these five sesquiterpenoids were measured in in‐vitro ethanol‐induced primary culture rat gastric mucosal (PRGM) cell damage and in‐vivo ethanol‐induced acute rat gastric ulcer models. Key findings Atractylon, atractylenolide I and biatractylolide were strongly toxic in PRGM cells, whilst atractylenolides II and III were not. Atractylenolide II did not show cytoprotective effects, but oral administration of atractylenolide III dose‐dependently prevented ethanol‐induced PRGM cell death and cell membrane damage. The EC50 values were 0.27 and 0.34 mm , respectively. In the in‐vivo assay, atractylenolide III 10 mg/kg significantly reduced 70% ethanol‐induced Wistar rat gastric ulcer. Atractylenolide III could inhibit matrix metalloproteinase (MMP)‐2 and MMP‐9 expression through upregulation of tissue inhibitors of metalloproteinase from the gastric ulcerated tissues. Conclusions Atractylenolide III was the major gastroprotective component of A. ovata in ethanol‐induced acute gastric ulcer. It is suggested that the gastroprotective mechanism of atractylenolide III was via inhibition of the MMP‐2 and MMP‐9 pathway.     

民族药小槐花质量标志物候选成分的研究

目的：开展对豆科山蚂蝗属药用植物小槐花（Desmodium caudatum（Thunb.）DC.）叶的化学成分研究,为小槐花质量标准体系的建立提供物质基础。方法：将小槐花叶经70%乙醇提取后,综合运用大孔吸附树脂柱色谱、硅胶柱色谱、制备型高效液相色谱等方法分离和纯化小槐花叶的化学成分,根据所得单体理化性质及波谱数据鉴定各化合物结构。结果：从小槐花叶中分离鉴定了13个化合物：清缸酒酚（1）、柠檬酚（2）、8-异戊烯基山柰酚（3）、二氢山柰酚（4）、neophellamuretin（5）、异柠檬酚（6）、槲皮素（7）、山柰酚（8）、牡荆素（9）、当药黄素（10）、大豆皂醇 B（11）、黄槿酮A （12）、黄槿酮 D （13）,其中化合物7、8、12和13为小槐花中各药用部位均含有的成分。结论：化合物7、8、12和13可作为小槐花的候选质控成分。     

Effect of p-chlorophenylalanine on the loss and maintenance of tolerance to ethanol

Rats were rendered tolerant to the motor-impairing effects of ethanol by daily oral administration. Subsequently, ethanol was withdrawn and the effect of p-chlorophenylalanine (p-CPA) on tolerance loss was examined. In two separate studies it was demonstrated that p-CPA, in a dosage regimen that produces extensive depletion of brain serotonin (5-HT), accelerated tolerance loss. These experiments suggest that at least part of p-CPA's inhibitory effect on net tolerance development to ethanol can be accounted for by its accelerating effect on tolerance loss; however, an inhibitory effect on tolerance acquisition cannot be excluded. On the other hand, once tolerance was established, p-CPA did not affect the maintenance of tolerance to ethanol.     

Occurrence of aflatoxin B1 contamination in dairy cows feed in Iran

Aflatoxins (AFs) are secondary toxic metabolites produced by fungal species. Occurrence of aflatoxin B1 (AFB1) was determined in 210 dairy cow feed samples consisting of concentrate (n=?70), corn silage (n =?70) and alfalfa hay ( n=?70) obtained from dairy farms in central part of Iran during July–September 2014. AFB1 analysis was carried out by using the competitive enzyme-linked immunosorbent assay technique for screening and high performance liquid chromatography for confirmatory purpose. AFB1 was detected in 88 analyzed samples (41.9%), ranging from 1.87 to 19.41?μg/kg; and 70 samples (33.3%) had levels of the toxin above the Iranian national standard and European Commission limits (5?μg/kg). The frequencies of AFB1 contamination in the samples were as follows: alfalfa hay, 55.7%; concentrate, 44.3% and corn silage, 25.7%. The high occurrence of AFB1 contamination may be attributed to poor harvesting technique, environmental conditions, insect infestation or unsuitable storage conditions. Hence, the contamination with AFs could be a potential hazard for human and animal health.     

女贞子提取工艺的研究

目的 优化女贞子的最佳提取条件。方法 采用正交试验法设计实验,考察乙醇浓度、加醇量、提取时间和提取次数,通过齐墩果酸、特女贞苷含量测定及浸膏得率来确定最佳乙醇提取工艺;考察粉碎度对女贞子提取工艺的影响,比较女贞子提取液趁热过滤浓缩与静置24 h后过滤浓缩的结果差异,并比较女贞子醇提工艺和水提工艺的各项指标。结果 女贞子最佳提取工艺为加10倍量的70%乙醇,提取3次,每次1 h,提取液趁热过滤浓缩。结论 该优化提取工艺合理可行,更适合生产。     

Gastroprotective activity of Eriobotrya japonica seed extract on experimentally induced gastric lesions in rats

The effect of Eriobotrya japonica seed extract (ESE) prepared with 70% ethanol on gastric mucosal injury was investigated. Six experimental models with different action mechanisms were used for the evaluation. Three concentrations of ESE were prepared for each model. ESE administration was initiated 14 days before induction of gastric mucosal injury, and its effect was investigated. ESE inhibited formation of gastric mucosal injury.     

Gastroprotective effect of standardized leaf extract from Careya arborea on experimental gastric ulcers in rats

Context: The leaf of Careya arborea Roxb. (Lecthidaceae) has been advocated in Ayurveda for the treatment of various disorders, including ulcers, healing of wounds and several skin diseases.

Objective: The 70% ethanol (EtOH) extract of C. arborea leaves (CALE) was investigated for its gastroprotective effect in different gastric ulcer models.

Materials and methods: CALE (100, 200, and 400?mg/kg body weight) was administered orally, twice daily for 5?d, for preventing aspirin (ASP)-, EtOH-, pylorus ligation (PL)-, and cold restraint stress (CRS)-induced ulcer in rats. The status of the antioxidant enzymes in CRS-induced ulcers, H⁺K⁺ATPase activity, gastric wall mucous in EtOH-induced ulcer, and gastric secretion parameters were estimated in the PL-induced ulcer model.

Results: CALE exhibited significant (p?<?0.01) dose-dependent inhibition of ulcer index in ASP 12.90–51.61%, EtOH 11.97–40.35%, PL 28.63–63.92%, and CRS 38.30–66.37%, respectively. A significant (p?<?0.001) decrease occurred in the level of H⁺K⁺ATPase, volume of gastric juice, and acid output. Simultaneously, the level of gastric wall mucus was increased significantly (p?<?0.05). The antioxidant enzyme levels of LPO and SOD were decreased with concomitant increase in catalase activity in CRS-induced ulcers. High-performance thin-layer chromatography (HPTLC) showed the presence of quercetin, ellagic acid, and gallic acid (0.31%, 0.24%, and 0.71% w/w, respectively) in CALE.

Conclusions: Our results show that C. arborea possesses significant gastro-protective activity, probably due to its free radical scavenging activity, and validate the folklore claim.     

Influence of Ethanol on Physical State of Freeze-Dried Mannitol

Purpose  The purpose of this study is to characterize freeze-dried mannitol prepared from an ethanol-containing solution as a function of the ethanol ratio, mannitol concentration, and annealing in the freeze-drying cycle. Methods  The characteristics of the freeze-dried mannitol were evaluated by X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The reconstitution time was measured for the freeze-dried solids as well as the residual moisture and ethanol by Karl–Fischer titration and gas chromatography, respectively. Results  The XRD pattern of 5% (w/v) mannitol freeze-dried from aqueous solution with no annealing cycle showed all the five characteristic peaks at 13.6° and 17.2° 2θ for the α polymorph, at 14.6° and 23.4° 2θ for the β polymorph and at 9.7°2θ for the δ polymorph. The addition of ethanol to the initial solutions resulted in only a peak at 9.7° 2θ, indicating the presence of only the δ polymorph, regardless of the ethanol ratio in the initial solutions used [10, 20, 30, and 40% (v/v)]. However, annealing during freeze-drying influenced the XRD pattern; in particular, for the solid prepared from the 10% ethanol solution. Annealing of the 10% ethanol solution promoted the formation of the α polymorph and produced a different peak that might be attributable to another polymorph. In DSC thermograms, an endotherm and a subsequent exotherm were found in the temperature range of 150°C to 160°C, which corresponded to the transition of the δ form to α or β forms. The magnitude of this transition was smaller as the ethanol ratio increased for the solids from ethanol-containing solutions with an annealing cycle. In other words, annealing of the ethanol-containing solutions promoted δ polymorph formation in the lyophiles. In addition, the mannitol concentration affected the polymorphism in freeze-dried solids prepared from aqueous and 10% ethanol solutions. Addition of ethanol in the initial solution, in particular, at a lower ethanol level (10% v/v), and a higher concentration of mannitol could also promote the generation of lumps in freeze-dried solids during reconstitution, and result in longer reconstitution time. The residual moisture levels were less than 0.5%, and residual ethanol levels were less than 0.1%, irrespective of the formulation used. Conclusions  The physical state and reconstitution time of the freeze-dried mannitol appears to be a complex function of the ethanol and mannitol concentrations in the initial solution before freeze-drying and of annealing during the freeze-drying process.     

葡萄籽原花青素降血脂药效部位筛选

目的：研究不同组分葡萄籽原花青素降血脂药效。方法：采用不同浓度乙醇渗漉提取、大孔树脂分离纯化,制得10%、30%、50%、70%乙醇部位葡萄籽原花青素提取物,建立大鼠高血脂模型,分别测定各组血清甘油三酯（TG）、总胆固醇（TC）、谷丙转氨酶（ALT）、谷草转氨酶（AST）的含量,以及Lee’S指数和脏器指数,对各提取物进行药效学研究,确定葡萄籽原花青素降血脂有效部位。结果：葡萄籽原花青素提取物10%、30%、50%乙醇部位具有明显降低高血脂大鼠模型的TG的含量（P<0.01）;同时50%乙醇部位还可以明显降低高血脂大鼠模型的ALT和AST含量（P<0.01）;10%、30%、50%、70%乙醇部位能抑制Lee’S指数的升高（P<0.01或P<0.05）;10%乙醇组显著升高肾脏指数;10%、30%、50%、70%乙醇组能显著升高脾脏指数（P<0.01）;10%、50%、70%乙醇组能显著降低总脂指数（P<0.01）。结论：50%乙醇部位葡萄籽原花青素提取物为葡萄籽降血脂有效部位。     

无梗五加果实提取物对大鼠CYP450活性的影响

目的研究无梗五加果实提取物对大鼠CYP450亚型CYP1A2、CYP2C19、CYP2E1、CYP3A4活性的影响。方法以咖啡因、奥美拉唑、氯唑沙宗和咪达唑仑作为CYP1A2、CYP2C19、CYP2E1和CYP3A4特异性探针药物,配制cocktail混合探针溶液,建立同时测定4种探针药物血药浓度的高效液相色谱法。将SD大鼠随机分为无梗五加果实70%乙醇提取物组、水提取物组和对照组,每天分别ig无梗五加果实70%乙醇提取物溶液、水提取物溶液和溶剂10 mL/kg,连续给药1周,于第8天ip混合探针药物10 mL/kg,分别在给药0、0.083、0.25、0.417、0.583、0.833、1、2、3、5、8、11、12 h于大鼠眼眶静脉丛采血,采用HPLC法对血浆样品进行分析,对给药组和对照组探针药物的药动学参数生物半衰期(t_(1/2))进行比较。结果与对照组比较,无梗五加果实水提取物组和70%乙醇提取物组咖啡因、咪达唑仑的t_(1/2)显著降低,奥美拉唑、氯唑沙宗的t_(1/2)显著增加,差异均具有统计学意义(P0.05、0.01)。结论无梗五加果实70%乙醇提取物和水提取物对大鼠的CYP2C19、CYP2E1有抑制作用,对大鼠的CYP1A2、CYP3A4有诱导作用。     

Sex differences in nicotine substitution to a pentylenetetrazol discriminative stimulus during ethanol withdrawal in rats

Rationale: Nicotine and ethanol are frequently co-abused in men and women, but few studies compare common stimulus effects produced by these substances between males and females. Objectives: This study compared the anxiety-like behavior induced by nicotine prior to and during ethanol withdrawal in intact male, sham-operated female, and ovariectomized (OVX) rats. Methods: Using an animal model of anxiety, the pentylenetetrazol (PTZ) drug-discrimination assay, rats were trained to discriminate PTZ (16 mg/kg, i.p.) from saline and were subjected to the following tests: (1) PTZ-lever selection at 12 h after termination of ethanol diet (4.5% for 10 days); (2) dose–response tests for nicotine (0.08– 1.3 mg/kg) prior to ethanol and 1.5, 6, and 7 days after ethanol withdrawal. Results: (1) During acute ethanol withdrawal (12 h), more male rats (43.4%) responded on the PTZ lever than OVX (29%) or sham female (15.3%) rats. (2) For nicotine dose–response tests, more male rats (70%) selected the PTZ lever than OVX (37.5%) or sham female (50%) rats prior to ethanol. At 1.5 days, nicotine fully generalized to the PTZ stimulus in male (100%) and OVX (90%), but only partially in sham female (50%) rats. At 6 days and 7 days after ethanol withdrawal, the PTZ-lever selection decreased, but more male rats (78%) tended to respond on a PTZ lever than OVX (63.6%) or sham female rats (62.5%). Conclusions: Acute nicotine produces anxiety-like behavior similar to that of PTZ in male and female rats, and this effect of nicotine is intensified during ethanol withdrawal in male and OVX rats, but not in sham female rats. Received: 20 July 1999 / Final version: 29 December 1999     

The fatty acid-rich fraction of Eruca sativa (rocket salad) leaf extract exerts antidiabetic effects in cultured skeletal muscle,adipocytes and liver cells

Context: Eruca sativa Mill. (Brassicaceae), commonly known as rocket salad, is a popular leafy-green vegetable with many health benefits.

Objective: To evaluate the antidiabetic activities of this plant in major insulin-responsive tissues.

Materials and methods: Five E. sativa leaf extracts of varying polarity were prepared (aqueous extract, 70% and 95% ethanol extracts, the n-hexane-soluble fraction of the 95% ethanol extract (ES3) and the defatted 95% ethanol extract). Eruca sativa extracts were investigated through a variety of cell-based in vitro bioassays for antidiabetic activities in C2C12 skeletal muscle cells, H4IIE hepatocytes and 3T3-L1 adipocytes. Guided by the results of these bioassays, ES3 was fractionated into the saponifiable (SM) and the unspaonifiable (USM) fractions. Glucose uptake was measured using [³H]-deoxy-glucose, while the effects on hepatic glucose-6-phosphatase (G6Pase) and adipogenesis were assessed using Wako AutoKit Glucose and AdipoRed assays, respectively.

Results: ES3 and its SM fraction significantly stimulated glucose uptake with EC₅₀ values of 8.0 and 5.8?μg/mL, respectively. Both extracts significantly inhibited G6Pase activity (IC₅₀ values of 4.8 and 9.3?μg/mL, respectively). Moreover, ES3 and SM showed significant adipogenic activities with EC₅₀ of 4.3 and 6.1?μg/mL, respectively. Fatty acid content of SM was identified by GC-MS. trans-Vaccenic and palmitoleic acids were the major unsaturated fatty acids, while palmitic and azelaic acids were the main saturated fatty acids.

Discussion and conclusion: These findings indicate that ES3 and its fatty acid-rich fraction exhibit antidiabetic activities in insulin-responsive cell lines and may hence prove useful for the treatment of type 2 diabetes.     

Rhobupcyanoside B,A new cyanoside from Rhodiola bupleuroides

One new cyanoside, rhobupcyanoside B (1), together with 7 known ones, was isolated from the 70% ethanol extract of the roots and rhizomes of Rhodiola bupleuroides. Their structures were determined by spectroscopic methods, including 2D NMR techniques. Compound 1 was evaluated for its inhibitory activity against α-glucosidase with IC₅₀ value of 278.28 ± 0.55 μM by comparing with the positive control (acarbose) at 210.40 ± 0.32 μM.     

Isolation and properties of the pituitary gonadotropin from silver carp (Hypophthalmichthys molitrix)

The gonadotropin of silver carp (scGTH) was purified from the pituitary glands in a yield of 8.4 mg g through extraction with 6% ammonium acetate (pH 5.1)–40% ethanol followed by 80% ethanol precipitation. DEAE-cellulose chromatography and gel filtration. The molecular weight of scGTH is about 32 000 as estimated by gel filtration. Leucine and serine were the two N-termini of scGTH. The amino acid composition of scGTH is rich in aspartic acid asparagine, glutamic acid/glutamine, valine, proline and half cystine. Its carbohydrate content is 22.2%. Biologically, scGTH significantly stimulated the steroidogenesis in carp testis and ovary in vitro and induced the ovulation in loaches. It also stimulated the ³²P-phosphate uptake into 1-day-old chicken testis. Immunologically. scGTH could cross-react with the anti-serum against cGTH and vice versa. In both cases parallel displacement curves were displayed.