杜仲化学成分、药理作用和临床应用研究进展

杜仲Eucommia ulmoides是我国特有的珍稀濒危二类保护植物,其皮、叶、雄花和种子均具有药用价值和食用价值。化学成分研究发现杜仲不同部位（皮、叶、雄花、种子）主要有木脂素类、环烯醚萜类、黄酮类、苯丙素类、萜类和甾体类等成分,具有抗骨质疏松、抗炎、神经保护、降血压、降血糖、调血脂、免疫调节、抗菌、抗病毒等药理作用,广泛应用在医药、保健食品、饲料添加剂及日化用品等多个领域。通过对2000年1月—2022年12月在中国知网（CNKI）和PubMed数据库中发表的杜仲文献进行检索,共检索到相关文献1772篇,其中有效文献188篇。综述了杜仲在化学成分、药理作用、临床研究和开发应用方面的研究进展,为后续杜仲的临床应用及相关产品开发提供参考。     

桉属间苯三酚-萜烯类化合物及其抗肿瘤作用机制研究进展

间苯三酚-萜烯为桉属Eucalyptus L.Herit植物中天然存在的主要活性成分,具有独特的聚酮-二萜骨架,抗癌活性显著,是抗癌先导化合物的潜在来源。综述桉属植物抗癌活性天然间苯三酚-萜烯类化合物的结构、作用机制,为间苯三酚-萜烯类抗癌新药的研发提供参考。     

In vitro antagonistic activity of monoterpenes and their mixtures against 'toe nail fungus' pathogens

The antibiotic effect of the active ingredients in Meijer medicated chest rub (eucalyptus oil, camphor and menthol) as well as the inactive ingredients (thymol, oil of turpentine, oil of nutmeg and oil of cedar leaf) were studied in vitro using the fungal pathogens responsible for onychomycosis, such as the dermatophytes Tricophyton rubrum, Trichophyton mentagrophytes, Microsporum canis, Epidermophyton fl occosum and Epidermophyton stockdale. The zones of inhibition data revealed that camphor (1). menthol (2). thymol (3). and oil of Eucalyptus citriodora were the most efficacious components against the test organisms. The MIC(100) for mixtures of these four components in various carrier solvents revealed that formulations consisting of 5 mg/mL concentrations of each have a potential to be efffective in controlling onychomycosis.     

Inhibitory effect of cyclic terpenes (limonene, menthol, menthone and thymol) on Fusarium verticillioides MRC 826 growth and fumonisin B1 biosynthesis

The minimum inhibitory concentration (MIC) of cyclic terpenes (limonene, menthol, menthone and thymol) against Fusarium verticillioides MRC 826 was assessed by using the semisolid agar antifungal susceptibility (SAAS) technique. Limonene, menthol, menthone and thymol were evaluated at final concentrations of 25, 50, 75, 150, 200, 250, 500 and 1000 μL/L of culture medium. Limonene and thymol showed the highest inhibitory effects on F. verticillioides development. Thus, the effects of monoterpenes on fumonisin B1 (FB1) biosynthesis were evaluated by using corn grain (Zea mays) as substrate. The monoterpenes were inserted on maize 1 day before inoculation with a conidial suspension of F. verticillioides to give final concentrations of 75 ppm. At this concentration, thymol was the most active inhibitor on FB1 biosynthesis.     

Controlled short-time terpene exposure induces an increase of the macrophages and the mast cells in bronchoalveolar lavage fluid

Eight healthy nonsmoking volunteers underwent terpene exposure (450 mg/m³ air) on 4 different occasions within a 2 week period. Total exposure time was 12 hours. Before and after the sequences of exposure, bronchoalveolar lavage was performed. Twenty hours after the exposure there was a significant (p < 0.05) increase of the alveolar cell concentration (median pre-exposure value 76 × 10⁶ cells/L, post-exposure value 126 × 10⁶ cells/L), predominantly due to an increment of the macrophages (from 72 × 10⁶ cells/L to 121 × 10⁶ cells/L). The mast cells also increased from 1/10 to 5/10 visual fields. No elevated concentrations of albumin, fibronectin, hyaluronan (hyaluronic acid), and tryptase were observed. We conclude that terpene exposure, in a concentration regarded as moderate, induces an acute alveolar cellular reaction in healthy subjects. © 1993 Wiley-Liss, Inc.     

Understanding Cannabis

Over the past decade, cannabis has gained popularity as a treatment for many conditions. Patients with various complaints ranging from chronic pain to insomnia to posttraumatic stress disorder are using cannabis with or without medical oversight. The effects of cannabis can vary widely depending on the strain that is consumed, the ratio of delta-9-tetrahydrocannabinol to cannabidiol, and the plant’s terpene profile. Considering the wide range of possible effects on the mind and the body, it is important for clinicians to have a basic understanding of medicinal cannabis, including the neurotransmitters and the endocannabinoid system. Thirty-three states have legalized the use of cannabis for prescribed medical purposes, and several others are considering doing so. Eleven states plus Washington DC, Guam, and Puerto Rico have legalized cannabis for recreational use. The objective of this article is to provide clinicians with the basic knowledge needed to understand the mechanism of action of medicinal cannabis in humans. We also identify some common terms associated with the cannabis culture and offer suggestions for patient teaching.     

Contact allergy to oxidized geraniol among Swedish dermatitis patients—A multicentre study by the Swedish Contact Dermatitis Research Group

Background

Geraniol is a widely used fragrance terpene, and is included in fragrance mix I. Geraniol is prone to autoxidation, forming the skin sensitizers geranial, neral, and geraniol‐7‐hydroperoxide. Oxidized geraniol has previously been patch tested in 1 clinic, giving 1% to 4.6% positive reactions in consecutive patients when tested at 2% to 11%.

Aim

To compare test reactions to pure and oxidized geraniol, to compare 2 different test concentrations of oxidized geraniol and to investigate the pattern of concomitant reactions to fragrance markers of the baseline series in a multicentre setting.

Methods

One thousand four hundred and seventy‐six consecutive patients referred for patch testing were patch tested with geraniol 6% pet. and oxidized geraniol 6% and 11% pet.

Results

Pure geraniol 6% pet., oxidized geraniol 6% pet. and oxidized geraniol 11% pet. gave 1%, 3% and 8% positive patch test reactions and 0.7%, 3% and 5% doubtful reactions, respectively. Approximately 50% of the patients with doubtful reactions to oxidized geraniol 6% pet. had positive reactions to oxidized geraniol 11% pet.

Conclusions

Oxidized geraniol 11% pet. provides better detection than oxidized geraniol 6% pet. As most patients reacted only to oxidized geraniol, it is important to explore further whether oxidized geraniol should be included in a baseline patch test series.

     

Fragrances and work-related asthma–California surveillance data, 1993–2012

Objective: Fragrance chemicals are used in a large array of products. Workers may be exposed to these chemicals in the workplace directly when used as air fresheners, or indirectly in personal care products used by coworkers or others. This study characterizes work-related asthma (WRA) cases associated with fragrance exposures in California workplaces from 1993 through 2012. Methods: We used the California Work-Related Asthma Prevention Program's surveillance database to identify individuals with physician-diagnosed WRA associated with the use of air fresheners and scented personal care products (perfumes, colognes, etc.). Cases were classified using previously published, standardized surveillance methods. Results: Perfume was the ninth most common exposure identified from 1993 through 2012. A total of 270 WRA cases associated with fragrance exposure were reported during this period, representing 3.8% of all confirmed cases. These 270 cases included 242 associated with perfume or cologne, 32 associated with air freshener, and 4 associated with both. Similar to non-fragrance cases, nearly a quarter of fragrance-associated cases were classified as new-onset asthma. Fragrance-associated cases were significantly more likely to be in office, health, and education jobs than non-fragrance-associated cases. When compared to non-fragrance cases, fragrance cases were significantly more likely to be female (94% vs 62%) and be classified as having work-aggravated asthma (38% vs 20%), yet had similar outcomes compared with cases associated with other exposures. Conclusions: Our surveillance data show that fragrance use in the workplace is associated with WRA. Prevention methods include employee education, enforced fragrance-free policies, well-designed ventilation systems, and good building maintenance.     

Amhezole,A Novel Fungal Secondary Metabolite from Aspergillus terreus for Treatment of Microbial Mouth Infection

Bio‐guided fractionation of Aspergillus terreus extract leads to isolation of a novel terpenoidal secondary metabolite. The isolated compound and the total alcoholic extract of Aspergillus terreus showed a remarkable activity against microbial mouth infections; namely, Candida albicans, Lactobacillus acidophilus, Streptococcus gordonii, and S. mutan. Moreover, the Minimum Inhibitory Concentration of the isolated compound was determined and showed low values. The combination of each of the alcoholic extract of A. terreus and the isolated compound Coe‐Comfort tissue conditioner inhibited the growth of Candida albicans at concentrations of 500 and 7.81 µg/mL, respectively, Lactobacillus acidophilus at concentrations of 250 and 7.81 µg/mL, respectively, Streptococcus gordonii at concentrations of 1000 and 62.50 µg/mL, respectively, and S. mutans at concentrations of 1000 and 125 µg/mL, respectively. The oral dosing of the extract and the isolated compound did not show any significant effect on the activity of alanine aminotransferase, aspirate aminotransferase, and the levels of blood urea and serum creatinine. Copyright © 2017 John Wiley & Sons, Ltd.     

Phytochemical screening and analgesic profile of the lyophilized aqueous extract obtained from Chrysobalanus icaco leaves in experimental protocols

Context: Chrysobalanus icaco L. (Chrysobalanaceae) has been used for the treatment of abdominal pain and cramps.

Objective: Assess the chemical and pharmacological profile of the lyophilized aqueous extract from C. icaco leaves (AEC).

Materials and methods: Chromatographic methods were used to assess compounds from AEC. Mice were treated with vehicle (control group) or AEC (100, 200 or 400?mg/kg, p.o.) (group with 7–8 mice) and the analgesic profile was assessed employing the acetic acid-induced writhing, formalin, hot plate tests and hyperalgesia induced by carrageenan (CG) or tumour necrosis factor-alpha. The animal motor performance was assessed using rota-rod and grip strength tests.

Results: The chromatographic profile of AEC demonstrated the presence of terpenoid compounds. The acute pretreatment with AEC, at all doses, produced a significant (p?<?0.01) inhibition of painful bahaviour (11.4?±?3.6; 10.3?±?2.8; 11.3?±?2.2) when compared to the control group (24.7?±?4.7) in acetic acid-induced writhing test. In the formalin test, AEC were effective in the second phase (p?<?0.01) (57.2?±?10.3; 56.3?±?9.2; 54.7?±?8.9) when compared to control group (121.9?±?18.5). No response was observed in the hot plate test. The higher dose of AEC produced a significant (p?<?0.01 or p?<?0.05) inhibitory effect on the mechanical hyperalgesia test. AEC did not affect the motor performance of the mice.

Discussion: The terpenoids from AEC are known for its analgesic and anti-inflammatory properties. So, these results corroborate the experiments using the AEC in inflammatory pain protocols.

Conclusion: Our results suggest that AEC act against inflammatory pain.