Pinoresinol diglucoside activates Nrf2 pathway to improve osteoporosis in mice / 中华内分泌外科杂志

Objective:Rosin alcohol two glycosidase (pinores inoldiglucoside, PDG) effect on the improvement of the osteoporosis in mice and the possible mechanism of action.Methods:A mouse model of osteoporosis was established by removing bilateral ovaries. According to the random number table method, 50 mice were divided into model (MOD) group (equal volume of normal saline), positive control (PC) group (0.2 mg/kg estradiol), PDG-low dose (L) group (5 mg/kg) PDG), PDG-high dose (H) group (10 mg/kg PDG by gavage) and PDG-H+ML385 group (10 mg/kg PDG by gavage after intramuscular injection of 30 mg·kg-1 ML385), 10 mice in each group; Another 10 mice without any ovarian treatment were selected as sham group (intragastric administration of the same amount of normal saline). After 3 weeks of drug intervention, the serum alkaline phosphatase (ALP), tartrate resistant acid phosphatase (TRAP), interleukin-6 (IL-6) and tumor necrosis factor were detected by enzyme-linked immunosorbent assay (ELISA) -α (TNF-α). The levels of superoxide dismutase (SOD) and malondialdehyde (MDA) were measured by dual energy X-ray. The mRNA and protein expression levels of nuclear factor related factor 2 (Nrf2), oxidase heme oxygenase 1 (HO-1), quinone oxidoreductase 1 (NQO1) were detected by real-time fluorescence quantitative PCR (qRT-PCR) and Western blot, respectively.Results:The serum ALP levels in Sham, MOD, PC, PDG-L, PDG-H and PDG-H + ML385 groups were (25.88±3.42), (47.42±5.32), (36.20±3.37), (38.95±3.24), (29.66±2.64), (39.57±2.06) U/dL, respectively; The serum trap levels were (2.18±0.40), (4.69±0.83), (3.58±0.38), (3.67± 0.48), (2.93±0.26), (3.81±0.49) U/L, respectively; BMD (153.04±12.96), (86.25±6.71), (126.53±8.99), (119.77±8.84), (139.18±15.94), (92.09±4.17) mg/cm 2; The expression levels of Nrf2 mRNA were 1.00±0.00, 0.35±0.04, 0.67±0.05, 0.54±0.03, 0.82±0.08 and 0.48±0.04, respectively; The expression levels of HO-1 mRNA were 1.00±0.00, 0.25±0.03, 0.56±0.03, 0.47± 0.03, 0.71±0.04 and 0.37±0.04, respectively; The expression levels of nqo1mrna were 1.00±0.00, 0.38± 0.02, 0.63±0.03, 0.58±0.04, 0.79±0.05 and 0.44±0.03, respectively; Nrf2 protein expression levels were 0.98±0.08, 0.26±0.04, 0.52 ±0.06, 0.46±0.03, 0.86±0.07, 0.45±0.05. HO-1 protein expression levels were 0.39±0.02, 0.09±0.01, 0.15 ±0.03, 0.17±0.03, 0.26±0.03, 0.12±0.02. NQO1 protein expression levels were 0.53±0.03, 0.21±0.02, 0.38±0.04, 0.29±0.02, 0.55±0.03, 0.24±0.04, respectively; The levels of serum IL-6 were (104.25±11.35), (515.38±74.48), (351.78± 65.12), (364.73±36.64), (246.18±17.52), (408.93±32.56) pg/ml, respectively; The levels of serum TNF-α were (33.79±3.55), (170.11±19.24), (76.09±8.99), (84.95±6.12), (66.98±3.73), (119.04±9.75) pg/mL, respectively; The serum SOD levels were (258.47±19.25), (72.15±8.12), (187.60±14.63), (152.61±12.36), (204.22±19.65), (138.01±13.62) U/mL, respectively; The serum MDA levels were (2.02±0.27), (4.75±0.73), (3.19±0.46), (3.7±0.49), (2.91±0.42), (4.10 ±0.25) μmol/L respectively. There were significant differences between MOD group and Sham group, or PC, PDG-L, PDG-H, PDG-H+ML385 group and MOD group,or PDG-H+ML385 group and PDG-H ( P<0.05) . Conclusion:PDG can reduce bone inflammation and oxidative stress by activating Nrf2 pathway and improve the state of osteoporosis.

A study on alpha-terpineol in Alzheimer's disease with the use of rodent in vivo model, restraint stress effect and in vitro Amyloid beta fibrils

Abstract Alzheimer's disease (AD) is a neurological disorder in which the neuronal degeneration is associated with inflammatory processes and oxidative stress. Since alpha-terpineol was shown to possess antioxidant and anti-inflammatory effects, the administration of this compound was studied on a rat model of AD. To create this model, Aβ1-42 was injected into the hippocampus of male Wistar rats. Generated AD models were divided into simple AD models and AD models in which short-term immobilization stress was added. Preventive and therapeutic (post-AD induction) effects of alpha-terpineol consumption (100 mg/Kg) were subsequently investigated in AD models, which were compared with control groups. Biochemical factors (superoxide dismutase and malondialdehyde), histological manifestations (amyloid plaques and neuron counts) and possible memory impairment (shuttle-box experiment) were investigated in all groups. For the in vitro experiment, alpha-terpineol effect was checked on Aβ1-42 fibril formation. In preventive and therapeutic modes, alpha-terpineol consumption could improve neurogenesis and long-term memory while reducing amyloid plaque counts and ameliorating biochemical factors (higher levels of superoxide dismutase and malondialdehyde and reduced levels of MDA). In vitro, shorter fibrillar structures were formed in the presence of alpha-terpineol, which indicates an anti-amyloid effect for this compound. In conclusion, alpha-terpineol significantly counteracted AD consequences.

GC-IMS Analysis of Volatile Components in Rhododendri Mollis Flos at Different Flowering Stages / 中国实验方剂学杂志

Objective:The volatile components of Rhododendri Mollis Flos were determined and the differences of volatile components at different flowering stages were compared and analyzed. Method:Gas chromatography-ion mobility spectrometry （GC-IMS） was used to detect the volatile components in Rhododendri Mollis Flos at different flowering stages （bud stage， initial flowering stage， half-flowering stage， blooming stage and late blooming stage）. GC-IMS spectra combined with cluster analysis， principal component analysis （PCA） and orthogonal partial least squares-discriminant analysis （OPLS-DA） were used to compare the differences and similarities of volatile components in different flowering stages. Result:A total of 70 volatile components in Rhododendri Mollis Flos at different flowering stages were detected， among which 67 were common components， and 47 were identified qualitatively， mainly alcohols， esters and aldehydes. Carveol was a special component at the late blooming stage. The content of alpha-terpineol is the highest at the initial flowering stage， but not at the blooming stage and late blooming stage. The relative contents of the active ingredients ［6-methyl-5-hepten-2-one， nonanal， alpha-terpineol， 1，8-cineole， linalool oxide， 1-octen-3-ol， （<italic>E</italic>）-3-hexenol］ showed a decreasing trend during flowering stages. GC-IMS spectra showed that the samples at different flowering stages had their own characteristic peak regions， and also had common regions. The results of cluster analysis， PCA and OPLS-DA all showed that the samples at different flowering stages were distinguishable. OPLS-DA was used to screen 19 different components to distinguish different flowering stages， including <italic>γ</italic>-butyrolactone， 1，8-cineole， ethyl hexanoate， etc. Conclusion:Rhododendri Mollis Flos samples at different flowering stages can be distinguished obviously， and the active substances in the volatile components are gradually dissipated with the degree of flower opening， which can provide reference for the improvement of material basis and the study of different flowering stages of Rhododendri Mollis Flos.

Eficacia terapéutica frente a la caspa grasa y la caspa seca de compuestos basados en terpineol, ácido salicílico y climbazol / Therapeutic effectiveness against oily or dry dandruff of compounds based on terpineol, salicylic acid and climbazole

Introducción: la caspa se define como una descamación excesiva del cuero cabelludo, en general acompañada de prurito. Su etiología es multifactorial y depende de la presencia de levaduras del género Malassezia, de la producción de sebo y de la susceptibilidad individual. Más allá de los tratamientos tradicionales para controlar la caspa, existen nuevas formulaciones que pueden incluir queratolíticos como el ácido salicílico, el climbazol, que además de agente antimicótico presenta potenciales propiedades antiproteolíticas o el terpineol, antimicótico de amplio espectro con acción antiinflamatoria. Objetivo: el objetivo principal de este estudio, consistió en evaluar el efecto sobre la caspa grasa de un champú con terpineol, extracto de sauce, ácido salicílico, climbazol y lipoaminoácido seborregulador y de una loción con terpineol, ácido salicílico, climbazol y glucósidos del extracto de roble y té verde. Se evaluó igualmente la eficacia sobre la caspa seca de un champú con terpineol, extracto de sauce, ácido salicílico y climbazol. Se realizaron una visita inicial (T0), otra al finalizar tratamiento (T28) y una final (T42), para evaluar la eventual reaparición de la caspa una vez suspendido el tratamiento. Material y Método: estudio unicéntrico abierto, no aleatorizado, a simple ciego, de 42 días de duración, llevado a cabo en 78 pacientes con caspa grasa o seca. Se clasificó la gravedad de la caspa en 4 grados. Según el tipo de caspa y su grado, se administraron un champú para caspa grasa (A), un champú para caspa seca (B), una loción para caspa grasa (C) o un champú neutro (D). Se establecieron 4 grupos de tratamiento en función del producto asignado (A, B, AC y CD). Resultados: un 59% de los participantes fueron mujeres y un 41% varones. La edad media fue de 47 años (rango 20-72). Del total de pacientes: 20 presentaron caspa grasa en grado medio-bajo (grupo A), 20 caspa seca en cualquier grado (grupo B), 17 caspa grasa en grado elevado (grupo AC) y 21 caspa grasa en grado medio-alto (grupo CD). Al cabo de cuatro semanas de tratamiento, el grado de caspa se redujo vs. basal en ≥70% de los casos en todos los grupos. Estas cifras ascendieron, en los pacientes con caspa grasa, a un 70% (grado bajo-medio), un 76,2% (grado medio-alto) y un 88,2% (grado elevado); el efecto fue más notable en aquellos con caspa seca, donde la cifra fue del 90%. La eliminación de la caspa fue completa en el 78,5%, 62,5%, 47% y 44,4% de ellos, respectivamente. Una vez transcurridas las dos semanas de lavado posterior al tratamiento, el nivel de caspa siguió descendiendo en un 55% de los pacientes tratados con el champú A, un 57,1% de los que emplearon la loción C, el 58,8% de los que usaron el champú A + la loción C, y el 35% de los que recibieron el champú B. Se declararon satisfechos o muy satisfechos con el producto un 70% de los pacientes del grupo A, un 80% del grupo B, un 66,7% del grupo CD y un 70,6% del grupo AD. Conclusiones: los resultados obtenidos en este estudio, orientan acerca de la eficacia frente a la caspa grasa y la caspa seca de dos champúes y una loción basados en terpineol, ácido salicílico y climbazol. Se requieren investigaciones adicionales que amplíen los resultados en este campo.

Introduction: dandruff is defined as excessive flaking of the scalp accompanied by itching. The etiology is multifactorial and depends on the presence of Malassezia yeasts, sebum production and individual susceptibility. Beyond traditional treatments to control dandruff, there are new formulations that may include keratolytics such as salicylic acid; climbazole, an antifungal agent which potential antiproteolytic properties, or terpineol, broad-spectrum antifungal with antiinflammatory action. Objective: the main objective of this study was to evaluate the effect on seborrheic dandruff of a shampoo with terpineol, willow extract, salicylic acid, climbazole and sebum-regulating lipoaminoacid, and a lotion with terpineol, salicylic acid, climbazole and glycosides from oak and green tea extract. Effectiveness on dry dandruff of a shampoo containing terpineol, willow extract, salicylic acid and climbazole was also evaluated. Three study visits were performed (T0, T28 and T42). Methods: single-center, open, non-randomized, single-blind, 42-day study conducted in 78 patients with seborrheic or dry dandruff. Dandruff severity was classified into 4 grades. A shampoo for oily dandruff (A), a shampoo for dry dandruff (B), a lotion for oily dandruff (C) and a neutral shampoo (D) were administered. Four treatment groups were established according to the assigned treatment (A, B, AC and CD). Results: 59% of participants were women and 41% men. The average age was 47 years (range 20-72). Of the total patients, 20 had medium-low oily dandruff (group A), 20 dry dandruff at any level (group B), 17 severe oily dandruff (AC) and 21 medium-high oily dandruff (group CD). After four weeks of treatment the severity of dandruff was reduced vs. baseline in ≥70% of cases in all groups; for oily dandruff results were 70% (low-medium grade), 76.2% (medium-high) and 88.2% (high level); the effect was most marked in patients with dry dandruff (90%). Dandruff removal was complete in 78.5%, 62.5%, 47% and 44.4% of them, respectively. Two weeks after having suspended the treatment, dandruff level continued to decline in 55% of patients treated with shampoo A, 57.1% of those who used the lotion C, 58.8% of patients who used shampoo A + lotion C, and 35% of those receiving shampoo B. Seventy per cent of patients in group A, 80% in group B, 66.7% of the CD group and 70.6% of the AD group were satisfied or very satisfied with the study treatments. Conclusions: the results obtained in this study suggest the effectiveness against oily and dry dandruff of two shampoos and a lotion based on terpineol, salicylic acid and climbazole. Further research to extend the results in this field is required.

Biotransformation of (-)-alpha-Pinene by Whole Cells of White Rot Fungi, Ceriporia sp. ZLY-2010 and Stereum hirsutum

Two white rot fungi, Ceriporia sp. ZLY-2010 (CER) and Stereum hirsutum (STH) were used as biocatalysts for the biotransformation of (-)-alpha-pinene. After 96 hr, CER converted the bicyclic monoterpene hydrocarbon (-)-alpha-pinene into alpha-terpineol (yield, 0.05 g/L), a monocyclic monoterpene alcohol, in addition to, other minor products. Using STH, verbenone was identified as the major biotransformed product, and minor products were myrtenol, camphor, and isopinocarveol. We did not observe any inhibitory effects of substrate or transformed products on mycelial growth of the fungi. The activities of fungal manganese-dependent peroxidase and laccase were monitored for 15 days to determine the enzymatic pathways related to the biotransformation of (-)-alpha-pinene. We concluded that a complex of enzymes, including intra- and extracellular enzymes, were involved in terpenoid biotransformation by white rot fungi.

Antibacterial activity of α-terpineol may induce morphostructural alterations in Escherichia coli

The antibacterial effect of α-terpineol from Cinnamomum longepaniculatum (Gamble) N. Chao leaf essential oils were studied with special reference to the mechanism of inhibiting the standard strain of Escherichia coli (CMCC (B) 44102) growth at ultrastructural level. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) and time-kill curves of α-terpineol were determined; Escherichia coli was treated with α-terpineol and observed under a transmission electron microscope. The MIC and MBC values of α-terpineol were all 0.78 µL/mL, and time-kill curves showed the concentration-dependent. Under the transmission electron microscopy (TEM), Escherichia coli exposed to MIC levels of α-terpineol exhibited decreased cell size and irregular cell shape, cell wall and cell membrane were ruptured, nucleus cytoplasm was reduced and nuclear area gathered aside. Results suggest that α-terpineol has excellent antibacterial activity and could induce morphological changes of Escherichia coli.

Determination of Four Components in Fresh Houttuynia cordata from Different Harvest Time with Gas Chromatography-Mass Spectrometry / 世界科学技术-中医药现代化

This study was aimed to establish a method for assay of 4-terpineol, α-terpineol, bornyl acetate and methyl-n-nonylketone in Houttuynia cordata with gas chromatography-mass spectrometry (GS/MS) for the first time in order to provide experimental evidences for its quality control. Undecylen was analyzed quantitatively. GC/MS method was used in the content determination of 4 kinds of components in Houttuynia cordata. GC conditions were that the temperature was firstly increased to 70oC for 5 min, and then 5oC·min-1 to 140oC for 5 min. Then, the temperature was increased by 10oC·min-1 to 250oC for 10 min. The temperature of the injection port was 230oC. The carrier gas was high purity helium. The flow rate was 1.0 mL·min-1. The split ratio was 10:1. The sample quantity was 1 μl. MS conditions were that the detector was MS, EI was 70ev, the temperature of four poles was 150oC, the temperature of ion source was 230oC. The results showed that there was good linearity of four components, which were 4-terpineol, α-terpineol, bornyl acetate and methyl-n-nonylketone obtained within the ranges of 6.492~129.84μg·min-1, 1.097~21.944 μg·min-1, 12.128~242.56 μg·min-1, and 84.76~169.52 μg·min-1, respectively. The average recoveries of the four components were 81.2%, 80.6%, 88.3%, and 84.6%, respectively. The RSDs were 1.5%, 2.3%, 1.1%, and 0.7%, respectively. It was concluded that the method was simple, sensitive, and easy to operate. The simultaneous measurement of multiple indexes on the component for quality evaluation of Houttuynia cordata can effectively reflect the quality of Houttuynia cordata. It can also be used in the quality assessment of fresh Houttuynia c ordate .

Antimicrobial Effects of Linalool and alpha-Terpineol against Methicillin-Resistant Staphylococcus aureus Isolated from Korean

Methicillin-resistant Staphylococcus aureus (MRSA) is one of the important causative microbes for nosocomial infection and has been isolated from the dental environment. The purpose of this study was to investigate the antimicrobial activity of linalool and alpha-terpineol against MRSA isolates from a Korean population. In the experiments, we determined the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of these two compounds against 18 strains of MRSA. The data revealed that the MIC90/MBC90 values of linalool and alpha-terpineol against MRSA were >12.8 mg/ml and 6.4 mg/ml, respectively. These results indicate that alpha-terpineol has more potent antimicrobial activity against MRSA than linalool and may have utility as an anti-MRSA cleansing agent for dental instruments and dental unit chairs.

THE PHARMACOLOGICAL PROPERTIES OF A NEW ANTIASTHMATIC DRUG, a-TERPINEOL / 中国药理学通报

a-Terpineol as an another antiasthmatic principle of essential oil of Artemisia argyi was studied. It had relaxant effect on isolated guinea pig tracheal smooth muscle preparations, the effective threshold concentrations being between 2. l-4.2x10-5 g/ml, and the EC50 being 0.71-1.15x10-4g/ml. It could protect guinea pigs from the acetylcholine and histamine-induced asthma when given orally or aer-osolly. The level of cAMP in the tracheal smooth muscle of guinea pigs was elevated in the presence of l0-4g/ml a- terpineol. The drug could block the development of desensitization to isoproterenol on isolated guinea pig tracheal smooth muscle preparations, and its relaxant effect did not be- influenced on the desensitized preparations also. In addition, a-terpineol had the Inhibitory effect of anaphylactic mediators release antagonistic effect of the mediators, antitussive and expectorant effect, and the inhibitory effect on isolated ed guinea pig atria. The toxiicological studies showed that it had good safety margin. ( + ) - a-Terpineol amd (-) a -terpineol had similarquality and potency of actions.