In Vitro Effectiveness of a Terpenic Denture Cleanser on Old Biofilm Surfaces

Purpose

To assess the effects of terpenic denture cleanser on denture biofilm removal using scanning electron microscopy (SEM).

Materials and Methods

The internal surface biofilm of four maxillary dentures was elucidated with Caristop‐revelador Dual Tone, and 40 blue‐stained specimens (0.6 cm × 0.4 cm × 2 mm) were obtained. These specimens were randomly assigned to one of the following four groups of 10 specimens each: control, Eci Clean, Fitty Dent, and terpenic denture cleanser. The period of immersion in each solution was 12 hours. Biofilm removal was evaluated using SEM, and morphologically varying areas of the SEM images were quantified with Imaris software. The data were analyzed using Kolmogorov‐Smirnov, t‐tests, ANOVA, and Tamhane's tests (p = 0.05).

Results

Data revealed that terpenic denture cleanser removed significantly more biofilm than any other treatment examined in this study. The t‐tests revealed significant differences in the clean area that resulted from the use of the terpenic cleanser compared with the clean area that resulted from the use of Eci Clean (p = 0.013). Fitty Dent was the least effective and left dirty acrylic resin. The average areas with few removed layers were 59.3%, 43.3%, and 9.5% in Fitty Dent, Eci Clean, and terpenic cleanser groups, respectively. Tamhane's tests indicated that the Eci Clean and Fitty Dent groups were significantly different from the 0.5% terpenic cleanser group (p = 0.008).

Conclusion

The terpenic denture cleanser was effective in removing denture biofilm.     

山茱萸总萜对KKay糖尿病小鼠的治疗作用研究

目的 观察山茱萸总萜对KKay糖尿病小鼠的治疗作用。方法 选择KKay糖尿病小鼠模型,分别以低、中、高剂量（0.05、0.10、0.20 g/kg）的山茱萸总萜ig给药5周。每天给药前观察动物一般状况;给药前及给药期间每周测定1次小鼠体质量、空腹血糖;给药第5周,进行ip葡萄糖耐量试验（IPGTT）,采血测定胰岛素（Ins）、糖化血红蛋白（HbA1c）、糖化血清蛋白（GSP）、总胆固醇（TC）、三酰甘油（TG）、高密度脂蛋白（HDL）、低密度脂蛋白（LDL）水平,计算胰岛素抵抗指数（IR）。结果 与模型组比较,山茱萸总萜可以剂量相关性地减轻KKay小鼠体质量,高剂量组第1、2和5周差异显著（P<0.05）;各剂量组自给药第1周起即可显著降低空腹血糖水平（P<0.05、0.01）;高剂量组显著降低IPGTT中小鼠血糖-时间曲线下面积（P<0.05）;山茱萸总萜可以剂量相关性地降低Ins、HbA1c、GSP、TC、TG、LDL水平、降低IR。结论 山茱萸总萜对于KKay小鼠糖尿病相关症状和指标具有剂量相关性的改善作用,可改善脂质代谢紊乱,提示其在治疗伴有胰岛素抵抗和脂质代谢紊乱的轻、中度2型糖尿病方面具有良好的应用前景。     

Novel Compounds with new Anti‐Ulcergenic Activity from Convolvulus pilosellifolius Using Bio‐Guided Fractionation.

Oral administration of the total alcohol extract of Convolvulus pilosellifolius Desr. (250 and 500 md/kg) showed potent anti‐ulcerogenic activity in absolute ethanol‐induced ulcer model in rats; it showed percent protection of control ulcer by 69.2 and 84.6%, respectively, while standard ranitidine (100 mg/kg) exhibited 46.2%. Bio‐guided work leads to isolation of two novel compounds (1 and 2), which were identified through ¹H, ¹³C NMR, HMPC, HMQC and DEPT as: methyl 2‐(hydroxymethyl) octanoate, named as amanitate, and 16‐amino‐9,13‐dimethyl‐17‐(prop‐1‐en‐2‐yl)‐hexadecahydro‐1H‐cyclopenta[a] phenanthren‐3‐ol, named as asmatol. Both compounds (50 mg/kg) possessed anti‐ulcerogenic activity with 95.4% and 55.84% protection, respectively. Two known compounds (3 and 4) were also isolated and identified through comparison with authentic samples and confirmed through different NMR techniques as kampeferol and quercetin. These compounds also showed anti‐ulcerogenic activity with 78.38% and 5.38% protection, respectively. The cytoprotective mechanism explains the potent anti‐ulcerogenic activity of the total alcohol extract and the isolated compounds. The extract was highly safe as the LD₅₀ was more than 5000 mg/kg. These results were well supported by the sub‐chronic toxicity study, as the extract (500 mg/kg) administrated orally to rats for 35 consecutive days showed no alteration in the liver and kidney functions. Copyright © 2016 John Wiley & Sons, Ltd.     

The application of anethole,menthone, and eugenol in transdermal penetration of valsartan: Enhancement and mechanistic investigation

Context: The main barrier for transdermal delivery is the obstacle property of the stratum corneum. Many types of chemical penetration enhancers have been used to breach the skin barrier; among the penetration enhancers, terpenes are found as the most highly advanced, safe, and proven category.

Objective: In the present investigation, the terpenes anethole, menthone, and eugenol were used to enhance the permeation of valsartan through rat skin in vitro and their enhancement mechanism was investigated.

Materials and methods: Skin permeation studies of valsartan across rat skin in the absence and the presence of terpenes at 1% w/v, 3% w/v, and 5% w/v in vehicle were carried out using the transdermal diffusion cell sampling system across rat skin and samples were withdrawn from the receptor compartment at 1, 2, 3, 4, 6, 8, 10, 12, and 24?h and analysed for drug content by the HPLC method. The mechanism of skin permeation enhancement of valsartan by terpenes treatment was evaluated by Fourier transform infrared spectroscopy (FTIR) analysis and differential scanning calorimetry (DSC).

Results: All the investigated terpenes provided a significant (p?<?0.01) enhancement in the valsartan flux at a concentration of 1%, and less so at 3% and 5%. The effectiveness of terpenes at 1% concentration was in the following order: anethole?>?menthone?>?eugenol with 4.4-, 4.0-, and 3.0-fold enhancement ratio over control, respectively. DSC study showed that the treatment of stratum corneum with anethole shifted endotherm down to lower melting point while FTIR studies revealed that anethole produced maximum decrease in peak height and area than other two terpenes.

Conclusion: The investigated terpenes can be successfully used as potential enhancers for the enhancement of skin permeation of lipophilic drug.     

Topical antiinflammatory and analgesic activities of Copaifera duckei dwyer

The oleoresin of several Copaifera species is used widely in the Amazonian Region mainly as a topical antiinflammatory and healing agent. The topical analgesic and antiinflammatory activities of Copaifera duckei oleoresin, whose terpenoidal chemical composition has been characterized, are now examined. Antiinflammatory activity was evaluated in rats using the carrageenin-induced paw edema and the granuloma tests, and in mice by the croton oil-induced dermatitis test. Analgesic activity was determined in mice using the writhing test method. In the carrageenin-induced edema and granuloma tests the oleoresin in a dose of 1,802 mg/kg inhibited the edema by 18% and granuloma by 42% (p < 0.05), this last result similar to that observed with dexamethasone. Topical doses of 517 mg/kg, 1,035 mg/kg and 1,802 mg/kg produced 52%, 58% and 62% (p < 0.05) reduction of the edema induced by croton oil, respectively, and 48%, 56% and 65% inhibition of the writhing process (p < 0.05). These results suggest that the Copaifera duckei oleoresin has topical antiinflammatory and analgesic activities.     

A double-blind,placebo controlled study of Ginkgo biloba extract (‘Tanakan’) in elderly outpatients with mild to moderate memory impairment

Summary

Thirty-one patients over the age of 50 years and showing a mild to moderate degree of memory impairment entered a 6-month double-blind, placebo controlled, parallel group design study to assess the effects of a standardized Ginkgo biloba extract (containing 24% flavonoid glycosides and 6% terpenes) on cognitive function. Patients were allocated at random to receive oral doses of 40?mg Ginkgo biloba extract or identical placebo 3-times daily. Assessments were made at baseline and after 12 and 24 weeks of treatment using a range of psychometric tests. Efficacy data were available for 27 patients (15 in the placebo group and 12 in the active treatment group). Statistical analysis of the data as compared to baseline suggests that Ginkgo biloba extract had a beneficial effect on cognitive function in this group of patients. Performance on the Digit Copying sub-test of the Kendrick battery was significantly improved at both 12 and 24 weeks, while the median speed of response on a computerized version of a classification task also showed a significant superiority over placebo at 24 weeks.     

INHIBITION OF CREATINE KINASE ACTIVITY IN RAT BRAIN BY METHYL BROMIDE GAS

Rats were exposed to 290 or 495 ppm methyl bromide gas for 6 h/day, 3 times/wk for 4 to 8 wk. Creatine kinase (CK), aspartate aminotransferase (ASAT), and lactate dehydrogenase (LDH) activities and bromide ion concentrations were measured in eight regions of the brain. Methyl bromide gas inhibited CK activities in all regions of the brain, though the inhibition tended to be smallest in the cerebellum (hemisphere and vermis) and largest in the brainstem (hypothalamus, midbrain, and medulla oblongata). The dose of methyl bromide to inhibit CK activities was lower than that to damage the central nervous system histologically. No inhibition of ASAT or LDH activities was seen except for a slight inhibition of these in striatum. Inhibition of CK activities did not increase clearly on increasing dose (290 to 495 ppm) or on prolonging exposure period (4 to 8 wk). Although 50% recovery of CK activities and the half-life of bromide ion agreed well in the medulla oblongata, changes in CK activities and bromide ion concentrations did not correlate otherwise. Thus, inhibition of CK activities in brain appears to be a sensitive indicator of methyl bromide intoxication, and may be related to genesis of its neurotoxicity. The inhibition seems to be caused by methyl bromide itself rather than by bromide ion. When effects on enzyme activities in brain homogenate were examined in vitro by bubbling with methyl bromide gas, CK inhibition was seen within 15 s of exposure. Dithiothreitol suppressed the CK inhibition, whereas N -acetylcysteine did not. These observations suggest that methyl bromide may attack sites in the CK molecule different from those attacked by ethylene oxide or acrylamide.