苦豆子抑菌洗液皮肤刺激性研究

目的:观察苦参抑菌洗液对家兔皮肤的反应情况,为临床安全用药提供依据。方法:按照卫生部《消毒技术规范》(2002版),采用急性皮肤刺激试验和多次皮肤刺激试验。结果:肉眼观察苦豆子抑菌洗液对急性皮肤及多次皮肤给药刺激改变,兔子皮肤均出现了不同程度的红斑、水肿。急性皮肤刺激试验的刺激指数为3.7,多次皮肤刺激试验的刺激指数为5.5。结论:苦豆子抑菌洗液对大白兔急性皮肤刺激强度和多次皮肤刺激强度均为中等刺激性。     

Spermicidal actions of extracts and compounds from Phytolacca dodecandra

The crude saponins from three plants, four purified saponins, and two synthetic derivatives were tested for spermicidal activity by means of an $\text{in vitro}$ incubation procedure. The crude saponins and two purified saponins derived from $\text{Phytolacca dodecandra}$ were found to have potent spermicidal activity. The most active compound tested against human sperm was lemmatoxin, a trisaccharide of oleanolic acid. Based on ED₅₀ values obtained in our test system, the crude saponin preparation from $\text{P. dodecandra}$ and lemmatoxin possessed nearly three times the spermicidal activities of a synthetic detergent currently used as a spermicidal agent. Biological activity could not be accounted for on the basis of surface activity.     

Effects of elm bark (Ulmus davidiana var. japonica) extracts on the modulation of immunocompetence in mice

The immunomodulative effects of elm bark extract were studied in vitro by the proliferation of splenocytes and the production capacity of three kinds of cytokines [interleukin (IL)-1beta, IL-6, and tumor necrosis factor (TNF)-alpha] by mouse peritoneal macrophages cultured with various fractions (methanol, hexane, chloroform, ethyl acetate, butanol, and water) of elm bark extract. Splenocyte proliferation and cell viability of peritoneal macrophages were increased with concentrations of polar fractions, such as butanol and water, in the range of 1-500 microg/mL. Significantly higher levels of the production of all three cytokines were detected with supplementation of methanol extract compared with other fractions. In order to elucidate its effect in vivo, elm bark water extract was orally administrated every other day for 2 weeks. Proliferation of splenocytes and the production capacity of cytokines (IL-1beta, IL-6, and TNF-alpha) by mouse peritoneal macrophages were used as indices for immune activity. Splenocyte proliferation induced by elm bark with lipopolysaccharide or concanavalin A stimulation was enhanced at 500 mg/kg of body weight concentrations compared to that of the control group. In the case of cytokines, the highest production of IL-6 and TNF was detected at 500 mg/kg of body weight concentrations. In conclusion, this study suggests through in vitro and in vivo experiments that Ulmus davidiana var. japonica (elm bark) extracts may enhance the immunocompetent properties such as splenocyte proliferation and cytokine production capacity by activated macrophages and have a protective effect in mice.     

The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its IC₅₀ values ranged from 47.1 to 210.5 µg/ml and IC₅₀ of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and 56.5 µg/ml, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.     

Gastroprotective effect and antioxidant properties of different Laurus nobilis L. leaf extracts

Laurus nobilis L. (Family Lauraceae) is an evergreen tree widely distributed in the Mediterranean area and Europe. It is used in folk medicine of different countries as a stomachic and carminative as well as in treatment of gastric diseases. Extracts obtained with different methods (methanol and chloroform) from laurel leaves were evaluated for their gastroprotective activities in the rat. The antioxidant capacity of the different extracts has been also measured in vitro. In order to confirm the activities investigated, histological observations were performed. The gastric damage was significantly reduced by all extracts administered. The more effective protection was produced by chloroformic and methanolic crude extracts. The results obtained after oral administration of L. nobilis leaf extracts are in good agreement with their antioxidant capacity, confirming the relationship between pharmacological efficacy and antiradical activity. Histological evidences confirm the results evaluated with the animal procedures.     

Preliminary evaluation on anti-inflammatory and analgesic effects of Sideritis syriaca L. herba extracts

We studied the anti-inflammatory and analgesic activity of extracts of Sideritis syriaca L. herba. Samples were collected from the wild plant, dried, powdered, and extracted with hexane and methanol. The extracts were evaporated to dryness and then suspended in suitable solvent. They were then tested for anti-inflammatory activity in the carrageenin rat paw edema test and for analgesic activity in the Randall and Selitto test and in the tail-flick test. At 24 hours after the treatment, the gastric mucosa of each rat was observed macroscopically. Based on these results the hexane extract was fractionated by column chromatography, and the fractions were obtained tested in the same way. Results showed interesting anti-inflammatory activity only for the hexane extract and all the fractions obtained from it. All the extracts and all the other fractions showed both peripheral and central analgesic activity. In rats treated with the tested compounds hyperemia and ulcers were absent. The data from this preliminary study reveal interesting pharmacological properties of S. syriaca L. herba extracts related to the marked analgesic activity and the absence of gastric ulcerogenic activity. The same is for anti-inflammatory activity, but in this case it seems to be related only to the apolar fraction.     

Radical scavenging, antibacterial, and antiproliferative activities of Melissa officinalis L. extracts

The aromatic herb Melissa officinalis L. can be used as an easily accessible source of natural antioxidants and as a possible food supplement and as a phytochemical. Radical scavenging, antibacterial, and antiproliferative activities of petroleum ether, chloroform, ethyl acetate, n-butanol, and water extracts of M. officinalis L. extracts were investigated. The results of antioxidative activity, obtained by electron spin resonance spectroscopy, confirmed that investigated extracts suppressed the formation of 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl, and lipid peroxyl radicals in all investigated systems in a dose-dependent manner. The maximum DPPH and hydroxyl radical scavenging activities (SA(DPPH) = SA(OH) = 100%) were achieved in the presence of n-butanol extract at concentrations of 0.4 mg/mL and 0.5 mg/mL, respectively. The highest lipid peroxyl scavenging activity (93.20%) was observed at a higher concentration (5 mg/mL) of n-butanol extract in the lipid peroxidation system. The most effective antibacterial activities were expressed by petroleum ether and ethyl acetate extracts on Sarcina lutea. Chloroform extract showed the strongest antiproliferative effect with 50% inhibitory concentration values of 0.09 mg/mL and 0.10 mg/mL for HeLa and MCF-7 cell lines, respectively. The present study demonstrated the high phenolic content and radical scavenging, antibacterial, and antiproliferative activities of extracts of M. officinalis L. originating from Serbia.     

Antiobesity activity of extracts from Lagerstroemia speciosa L. leaves on female KK-Ay mice

Banaba in the Tagalog name, Lagerstroemia speciosa L., has been used as a folk medicine for a long time among diabetics in the Philippines. Extracts from banaba leaves have been reported to reduce diabetic symptoms in genetically diabetic mice (Type II, KK-Ay). In the present study, female mice of the same strain showing remarkable body weight gain were used to examine the antiobesity effect of dietary banaba extract. Five-week-old female KK-Ay mice were fed a control diet or test diet containing 5% of a hot-water extract from banaba leaves instead of cellulose for 12 wk. Neither group showed any changes in diet intake during the experimental period. Body weight gain and parametrial adipose tissue weight were lowered significantly in the banaba diet group. Blood glucose levels were not suppressed in the banaba diet group, but hemoglobin A1C was found to be suppressed at the end of the experiment. No effects on the serum lipids were observed, but the mice fed banaba extract showed a significant decrease, to 65% of the control level in total hepatic lipid contents. This decrease was due to a reduction in the accumulation of triglyceride. These results suggest that banaba had a beneficial effect on obese female KK-Ay mice.     

Differences in gastroprotective and mutagenic actions between polar and apolar extracts of Ananas ananassoides

Several plants are used in folk medicine to treat gastrointestinal disorders. Ananas ananassoides (Baker) L.B. Smith (Family Bromeliaceae) is a medicinal plant commonly used in the central region of Brazil against gastric pain. We evaluated two extracts (methanol [MeOH] and dichloromethane [DCM]) obtained from the leaves of A. ananassoides for their ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% ethanol, absolute ethanol, non-steroidal anti-inflammatory drugs, and pylorus ligation) in mice and rats. The best results were obtained after pretreatment with the DCM extract, whereas the MeOH extract did not show any significant anti-ulcerogenic activity but presented mutagenic action. The mechanism of action of the DCM extract suggested the effective participation of endogenous sulfhydryl group in the gastroprotective action. The data, taken together with the absence of acute toxicity and mutagenicity, indicate the apolar extract, instead of the polar, extract of A. ananassoides as a safe and potential new anti-ulcerogenic drug.     

Anti-inflammatory and analgesic effects of Spartium junceum L. flower extracts: a preliminary study

Our objective was to study the anti-inflammatory and analgesic activity of extract of Spartium junceum L. flowers. Samples of flowers were collected from wild plants, dried, powdered, and extracted with hexane and methanol. The extracts were evaporated to dryness and then suspended in suitable solvent. They were then tested for anti-inflammatory activity in the carrageenin rat paw edema test and for analgesic activity in the Randall and Selitto mechanical pressure test and in the tail-flick test. Twenty-four hours after treatment, the gastric mucosa of each rat was observed macroscopically. Based on these results the hexane extract was fractioned by column chromatography, and the fractions obtained were tested in the same way. The results showed good anti-inflammatory activity only for a single fraction of the hexane extract, while all the extracts and all the other hexane fractions showed both peripheral and central analgesic activity. In rats treated with the tested compounds hyperemia and ulcers were absent. The data from this preliminary study reveal interesting pharmacological properties of S. junceum L. flowers extract related to the marked analgesic activity and the absence of gastric ulcerogenic activity.     

Comparison of the immunomodulatory effects of L. donovani and L. major excreted-secreted antigens, particulate and soluble extracts and viable parasites on human dendritic cells

In an experimental model of human monocyte-derived dendritic cells (DCs), the immunophenotype of mature DCs infected with Leishmania donovani and Leishmania major showed a weak decrease in the cell surface expression of CD40, CD86, HLA-DR and DC-SIGN compared with uninfected control DCs. This immunomodulatory effect was more pronounced after stimulation with excreted-secreted antigens (ESA) of both species but absent after stimulation with particulate and soluble extracts. Infection with viable promastigotes, as well as stimulation with ESA from L. donovani and L. major, decreased IL-10 and IL-12p70 secretion. To our knowledge, this is the first direct demonstration that ESA from Leishmania promastigotes can stimulate DCs in the same manner as viable promastigotes.     

染料木黄酮抗辐射研究进展

染料木黄酮的化学名为5,7,4’-三羟基异黄酮,是大豆异黄酮的主要成分及其生物活性基础。近年来大量研究发现,染料木黄酮具有较强的抗氧化活性,可以淬灭辐射诱导的自由基增多和增加抗氧化酶的活性,抑制膜的脂质过氧化;还可通过调节细胞周期、抑制细胞凋亡、调控细胞基因表达等减轻辐射损伤,促进损伤修复,表现出较强的抗辐射作用。     

Loquat (Eriobotrya japonica) extracts suppress the adhesion, migration and invasion of human breast cancer cell line

We examined the inhibitory effects of loquat methanol extract on the adhesion, migration, invasion and matrix metalloproteinase (MMP) activities of MDA-MB-231 human breast cancer cell line. Cells were cultured with DMSO or with 10, 25, or 50 µg/ml of loquat methanol extract. Both leaf and seed extracts significantly inhibited growth of MDA-MB-231 cells in a dose-dependent manner, although leaf extract was more effective. Adhesion and migration were significantly inhibited by loquat extracts in a dose-dependent manner. Loquat extract also inhibited the invasion of breast cancer cells in a dose-dependent manner and leaf extract was more effective than seed extract. MMP-2 and MMP-9 activities were also inhibited by loquat extract. Our results indicate that methanol extracts of loquat inhibit the adhesion, migration and invasion of human breast cancer cells partially through the inhibition of MMP activity and leaf extract has more anti-metastatic effects in cell based assay than seed extract. Clinical application of loquat extract as a potent chemopreventive agent may be helpful in limiting breast cancer invasion and metastasis.     

Aspirin attenuates the anxiolytic actions of ethanol.

The present study examined the effect of aspirin on the anxiolytic action of ethanol. Previous research has shown that ethanol reliably produces an anxiolytic effect on rodent's plus-maze performance while aspirin has been demonstrated to attenuate several of ethanol's behavioral actions. Female Sprague-Dawley rats were given s.c. aspirin doses of 0 or 150 mg/kg, followed 30 min later by s.c. ethanol doses of 0, 1.0 or 1.6 g/kg. After 5 min, animals were tested in the elevated plus-maze. Although aspirin did not have a significant effect on anxiety-related behavior, it did attenuate the anxiolytic action of ethanol at the dose of 1.0 g/kg, but not at the 1.6 g/kg dose. Thus, aspirin by itself does not appear to possess anxiolytic actions, but does modify the anxiolytic actions of 1.0 g/kg, but not 1.6 g/kg ethanol.     

Antimicrobial activities of Psophocarpus tetragonolobus (L.) DC extracts

Consecutive chloroform, ethanol, and ethyl acetate partitions of extracts from winged bean [Psophocarpus tetragonolobus (L.) DC] root, stem, leaf, and pod extracts were tested for their antimicrobial activity against 19 microbial species, including 11 bacterial pathogens, four yeasts, and four molds using the disk diffusion assay technique. The pod extract was found to be most effective against all of the tested organisms, followed by the stem, root, and leaf extracts, and the ethanol fraction showed the most significant (p < 0.05) antimicrobial activity against all of the tests among three soluble fractions of extract, followed by the ethyl acetate and chloroform fractions. The minimum inhibitory concentrations (MICs) of extracts determined by the broth dilution method ranged from 1.25 to 10.0 mg/mL. The MIC of ethanol fraction of pod extracts was the lowest by comparison with the other two extracts. The MIC for fungi was at or below 2.5 mg/mL and for bacteria was at or above 2.5 mg/mL.     

Chelating,antioxidant and hypoglycaemic potential of Muscari comosum (L.) Mill. bulb extracts

Abstract

The metal chelating activity, antioxidant properties and the effect on carbohydrate-hydrolysing enzyme inhibition of Muscari comosum extracts have been investigated. M. comosum bulbs contain a total amount of the phenols with a value of 56.6 mg chlorogenic acid equivalent per gram of extract and a flavonoid content of 23.4 mg quercetin equivalent per gram of extract. In order to evaluate the non-polar constituents, n-hexane extract was obtained. Gas chromatography–mass spectrometry analysis revealed the presence of fatty acids and ethyl esters as major constituents, with different aldehydes and alkanes as minor components. Ethanolic extract had the highest ferric-reducing ability power (66.7 μM Fe(II)/g) and DPPH scavenging activity with a concentration giving 50% inhibition (IC₅₀) value of 40.9 μg/ml. Moreover, this extract exhibited a good hypoglycaemic activity with IC₅₀ values of 81.3 and 112.8 μg/ml for α-amylase and α-glucosidase, respectively. In conclusion, M. comosum bulbs show promising antioxidant and hypoglycaemic activity via the inhibition of carbohydrate digestive enzymes. These activities may be of interest from a functional point of view and for the revalorization of this ancient non-cultivated vegetable of Mediterranean traditional gastronomy.     

Dichloromethane extracts of Sophora japonica L. stimulate osteoblast differentiation in mesenchymal stem cells

Sophora japonica L. fruit prevents bone loss by inhibiting osteoclast activity. We hypothesized that S japonica L. extracts could promote osteoblast differentiation. To test this hypothesis, we investigated the effect of S japonica L. on osteoblast differentiation and identified the bioactive compound(s) from S japonica L. The mature fruit of S japonica L. was partitioned with ethanol, hexane, dichloromethane (DCM), ethyl acetate, and butanol, and their effects were tested on osteoblast differentiation of C3H10T1/2 cells. DCM fractionated extracts were identified as the most osteogenic fractions. DCM fractionated extracts dose-dependently stimulated alkaline phosphatase activity and matrix mineralization. The DCM fractions also induced expression of osteoblast markers such as alkaline phosphatase, osterix, and osteocalcin in C3H10T1/2 and primary bone marrow cells. Genistein was found abundantly in the DCM fractions. Furthermore, the genistein and DCM fractions similarly modulated the expression of estrogen target genes and were both active in transfection assays that measured estrogen agonistic activity. Finally, pharmacological inhibition by treatment with an estrogen receptor antagonist or specific inhibition of gene expression by small interference RNAs targeted to estrogen receptor-β abolished the effects of the DCM extracts, further supporting the idea that the genistein in the DCM extracts mediated the pro-osteogenic effects. Taken together, we identified genistein as the key phytoestrogen responsible for the effects of S japonica L. on osteoblast differentiation.