Terpenoids and Bio-Functions of Essential Oils Hydrodistilled Differently from Freshly Immature and Mature Blumea balsamifera Leaves.

The volatiles and antioxidant capacity of essential oils (EOs) extracted from freshly immature and mature leaves of Blumea balsamifera at various hydrodistillation times were investigated. Seven major terpenoids were identified: two monoterpenes, camphor and L-borneol, and five sesquiterpenes, silphiperfol-5-ene, 7-epi-silphiperfol-5-ene, ß-caryophyllene, ɤ-eudesmol, and α-eudesmol. The quantity and terpenoid composition of the EOs were impressed by leaf maturity and hydrodistillation times. The yield of EOs from the immature leaves was 1.4 times that of mature leaves, with 73% of the yield acquired within the first 6 hours (hrs) of hydrodistillation. Approximately 97% of camphor and L-borneol, 80% of ß-caryophyllene, silphiperfolene, and 7-epi-silphiperfolene, 32% of ɤ-eudesmol, and 54% α-eudesmol were collected in the first 6 hrs of hydrodistillation. More ß-caryophyllene, ɤ-eudesmol, and α-eudesmol were found in the mature leaf EOs. The antioxidant capacity of the EOs was proportionally related to their terpenoid contents. The EOs extracted from immature leaves at 0-6 hrs of hydrodistillation demonstrated distinctive antibacterial activity against Staphylococcus aureus, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 mg/mL and 1 mg/mL, respectively.

Phenolics, Antioxidant and Antibacterial Activities of Immature and Mature Blumea balsamifera Leaf Extracts Eluted with Different Solvents.

Blumea balsamifera (L.) DC., belonging to the Asteraceae family, also known as "ngai camphor," is one of the traditional herbs used in Thailand for folk medicine and a component in local food and drinks. There was, however, no evidence indicating the presence of beneficial compounds at different leaf ages. Exploring various extraction solvents, we investigated the phenolics, flavonoids in particular quercetin content, antioxidant capacity, and antibacterial activity of immature and mature leaf extracts. The dried leaves were macerated in 50% ethanol, 95% ethanol, hexane, or decocted in water. Bioactive substances were analyzed by UV spectrophotometry and HPLC. Analysis of antioxidant capacity was done byDPPH, ABTS, FRAP, and NO scavenging assays. The antibacterial activity of immature leaf extract eluted with 50% ethanol was subsequentially evaluated in vitro. Extraction with 50% ethanol proved optimal, yielding 1.2-1.6-fold and 1.5-fold greater immature and mature leaf extracts than other solvents. More phenolics (1.2-fold), flavonoids (1.1-fold), quercetin content (4.8-fold), and antioxidant activity (1.3-fold) were found in the immature leaf extract. There was a significant positive correlation between antioxidant activity and bioactive compounds. The immature leaf extract eluted with 50% ethanol showed antibacterial activity against Staphylococcus aureus, with a minimum inhibitory concentration of 0.5 mg/mL. The immature leaves of B. balsamifera are a rich source of quercetin and phenolics, and 50% ethanol proved optimal for extracting bioactive components from these leaves.

Correlation between sensory and instrumental characterization of developed sunscreens containing grape seed extract and a commercial product.

OBJECTIVE: In the development of cosmetic products, sensory evaluation is an important step in determining consumer acceptance before it is released on a market but is often time-consuming and costly. However, correlating sensory characteristics with instrumental parameters using multivariate techniques is a potential way to facilitate the development of cosmetic products. METHODS: Sunscreen formulations varied in the content of grape seed extract (GSE) and ultraviolet (UV) filters, and benchmark products were characterized using sensory descriptive analysis and instrumental analysis. Principal Component Analysis (PCA) was applied to the panel's performance data to study how well the panelists performed compared to each other and to find an association between rheological and textural instrumental parameters of cream samples. Further, applying Partial Least Squares (PLS) regression analysis, the association between sensory attributes and instrumental parameters was analyzed. In addition, a preference for the sensory properties of the studied sunscreen products that are important for consumers living in Southeast Asia was assessed by PLS. RESULTS: In this study, both the sensory and instrumental properties of all tested formulations were described well by PCA. The practicality of PLS was confirmed by an established correlation between sensory attributes from the categories of appearance (glossiness), pick-up (integrity of shape, firmness, glossiness, stringiness), and after-feel (glossiness, spreadability, stickiness) with both rheological and textural parameters. Although the instrumental analysis could not completely replace sensory evaluation, a described method applying PLS can be used as an additional cost-effective and time-saving method during the development of cosmetic products. Moreover, PLS revealed that sunscreens with a light texture and glossy appearance providing smooth skin after-feel are likely to be preferred over the thicker formulations having a residual color appearance in Southeast Asia. CONCLUSION: Until a universal model is created, the cosmetics developers and companies can apply a described method of determining sensory properties from the instrumental parameters of their own products. Future studies will be worth exploiting the applicability of the PLS regression model on instrumental datasets predicting sensory characteristics of other sunscreen products.

OBJECTIF: Dans le développement de produits cosmétiques, l'évaluation sensorielle est une étape importante pour déterminer l'acceptation par le consommateur avant la mise sur le marché, mais elle est souvent longue et coûteuse. Cependant, la corrélation des caractéristiques sensorielles avec les paramètres instrumentaux à l'aide de techniques multivariées est un moyen potentiel afin de faciliter le développement des produits cosmétiques. MÉTHODES: Les formulations d'écrans solaires variants en termes de teneur en extrait de pépins de raisin (EPR) et en filtres ultraviolets (UV), et les produits de référence ont été caractérisés à l'aide d'une analyse sensorielle descriptive et d'une analyse instrumentale. L'analyse en composantes principales (ACP) a été appliquée aux données de performance du panel pour étudier la performance des panélistes les uns par rapport aux autres et pour trouver une association entre les paramètres instrumentaux rhéologiques et texturaux des échantillons de crème. En outre, l'association entre les attributs sensoriels et les paramètres instrumentaux a été analysée au moyen d'une analyse de régression PLS (Partial Least Squares). De plus, une préférence pour les propriétés sensorielles des produits de protection solaire étudiés importantes pour les consommateurs vivant en Asie du Sud-Est a été évaluée par PLS. RÉSULTATS: Dans cette étude, les propriétés sensorielles et instrumentales de toutes les formulations testées ont été bien décrites par l'ACP. L'aspect pratique de l'analyse PLS a été confirmé par une corrélation établie entre les attributs sensoriels des catégories de l'apparence (brillance), de la prise (intégrité de la forme, fermeté, brillance, filant) et de l'impression résiduelle (brillance, capacité d'étalement, adhésivité) avec les paramètres rhéologiques et texturaux. Bien que l'analyse instrumentale ne puisse pas remplacer complètement l'évaluation sensorielle, la méthode décrite appliquant la PLS peut être utilisée comme une méthode supplémentaire rentable et permettant de gagner du temps lors du développement de produits cosmétiques. En outre, l'analyse PLS a révélé que les écrans solaires à la texture légère et à l'aspect brillant, qui procurent une sensation de douceur sur la peau, sont susceptibles d'être préférés aux formulations plus épaisses ayant une couleur résiduelle en Asie du Sud-Est. CONCLUSION: En attendant la création d'un modèle universel, les développeurs et les entreprises de cosmétiques peuvent appliquer une méthode décrite pour déterminer les propriétés sensorielles à partir des paramètres instrumentaux de leurs propres produits. Les études futures devront exploiter l'applicabilité du modèle de régression PLS sur des ensembles de données instrumentales prédisant les caractéristiques sensorielles d'autres produits solaires.

Chemical and mechanical accelerated and long-term stability evaluation of sunscreen formulation containing grape seed extract.

BACKGROUND: Sunscreens and catechins from grape seed extract (GSE) are sensitive to various environmental factors and undergo certain changes over time that might affect the effectiveness of the final product. To this date, effects of thermal storage conditions have not been sufficiently addressed to guarantee the long-term stability of sunscreen formulations. AIMS: To study the chemical and mechanical accelerated and long-term stability of sunscreen formulation containing GSE at the Climatic Zone IVb conditions. METHODS: Stability studies were performed for 6 months for accelerated stability study at 30°C ± 2 and 50°C ± 2, 75 ± 5% relative humidity; and long-term stability study at 5°C ± 5. The quantification of constituents of three formulations: sunscreen with GSE, cream with UV filters only, and cream with GSE only was performed by high-performance liquid chromatography. In vitro spectrophotometry was used to determine changes in sun protection effectiveness through SPF and UVAPF values. Mechanical stability was evaluated by textural and rheological analyzes. RESULTS: All tested formulations were less stable at high-temperature conditions. The contents of catechin (С) and epicatechin (EC) in sunscreen with GSE were reduced to 37% and 50% at 50°C, respectively, whereas UV filters appeared to be stable. However, despite the significant reduction in catechins over time, polyphenols in GSE remained unchanged at different stored conditions. The SPF values and water resistance of sunscreen with GSE were maintained throughout the study. CONCLUSIONS: A current in vitro study has shown that sunscreen with GSE is a value-added anti-aging ingredient in sunscreen formulation because its polyphenolic composition as well as SPF values and water resistance were maintained under all temperature conditions over time.

Thermal Degradation Kinetics and pH-Rate Profile of Verbascoside and Stability Improvement by Solid Lipid Nanoparticles.

Thermal degradation of verbascoside (VB) in Acanthus ebracteatus Vahl (AE) always affects its health benefit. Here the temperature effect on VB in both AE extract and solid lipid nanoparticles (SLNs)-encapsulated AE extract was demonstrated using the Arrhenius plot. The reaction rate constants were calculated for shelf life and plotted to obtain pH-rate profiles. VB degradation was a first-order reaction. The reaction rate in a neutral to alkaline solution was faster than in an acidic solution. VB in AE extract-loaded SLNs was more stable than in uncapped AE extract. The shelf life of VB in SLNs was 153 days with activation energy (E a) of 76.16 kJ mol-1, whereas those of VB in AE extract and in AE extract solution were 75 days with E a = 78.03 kJ mol-1 and 12 days with E a = 49.24 kJ mol-1, respectively. Therefore, we anticipate that the AE extract-loaded SLNs will be beneficial for product development.

Effects of some medicinal plant extracts on dermal papilla cells.

INTRODUCTION: Miniaturization of the hair follicles is evident on the balding scalp. Approved medications, topical minoxidil, and oral finasteride for the treatment of alopecia sometimes come with undesirable adverse effects. The study was to examine the bioactivity of medicinal plants for finding the promising source of anti-hair loss application. METHODS: Ten ethanolic extracts were prepared from Acacia concina (Willd.) DC., Acanthus ebracteatus Vahl, Bridelia ovata Decne, Cleome viscosa L., Cocos nucifera L., Hibiscus subdariffla L., Oryza sativa L., Terminalia chebula Retz., Tinospora crispa (L.) Hook. f. & Thomson and cytotoxic tested on dermal papilla cells using MTT assay. The effect of the extracts on cell cycle was also determined using flow cytometry technique. Anti-inflammatory activity was examined by determining IL-1ß inhibition in RAW 257.4 cells. In vitro study of androgenic and 5α-reductase inhibitory activities were also determined using MTT assay and enzymatic reaction couple with liquid chromatography-mass spectrometry (LC-MS), respectively. RESULTS: Our results revealed that only A. ebracteatus promoted dermal papilla cell proliferation and the S and G2/M phases in cell cycle. A. ebracteatus also showed inhibitory activity against 5α-reductase and testosterone in reducing cell viability of the dermal papilla. Moreover, A. ebracteatus extract strongly inhibited LPS-stimulating IL-1ß production in RAW 264.7 cells in a dose-dependent manner. CONCLUSION: Our finding indicated that the ethanolic extract of A. ebracteatus is a promising candidate for anti-hair loss treatment.

Isolation and HPLC Quantitative Determination of 5α-Reductase Inhibitors from Tectona grandis L.f. Leaf Extract.

Steroid 5α-reductase plays a crucial role in catalyzing the conversion of testosterone to dihydrotestosterone, which is involved in many androgen-dependent disorders. Leaf-hexane extract from Tectona grandis L.f. has shown promise as a 5α-reductase inhibitor. The objectives of this current study were to isolate and identify 5α-reductase inhibitors from T. grandis leaves and to use them as the bioactive markers for standardization of the extract. Three terpenoid compounds, (+)-eperua-8,13-dien-15-oic acid (1), (+)-eperua-7,13-dien-15-oic acid (2), and lupeol (3), were isolated and evaluated for 5α-reductase inhibitory activity. Compounds 1 and 2 exhibited potent 5α-reductase inhibitory activity, while 3 showed weak inhibitory activity. An HPLC method for the quantitative determination of the two potent inhibitors (1 and 2), applicable for quality control of T. grandis leaf extracts, was also developed. The ethanolic extract showed a significantly higher content of 1 and 2 than found in the hexane extract, suggesting that ethanol is a preferable extraction solvent. This study is the first reported isolation of 5α-reductase inhibitors (1 and 2) from T. grandis leaves. The extraction and quality control methods that are safe and useful for further development of T. grandis leaf extract as an active ingredient for hair loss treatment products are also reported.

Anti-inflammation and gingival wound healing activities of Cannabis sativa L. subsp. sativa (hemp) extract and cannabidiol: An in vitro study.

OBJECTIVE: To evaluate the anti-inflammatory and gingival wound healing activities of Cannabis sativa L. subsp. sativa (hemp) extract and cannabidiol (CBD). DESIGN: The cellular bioactivities of hemp extract and CBD were determined the inhibition of TNF-α and IL-1ß in LPS-induced murine macrophage (RAW 264.7) cells by using ELISA while wound healing activity in human gingival fibroblast (HGF-1) cells was performed by a scratch test assay. The cytotoxicity was also concerned and evaluated by MTT assay. RESULTS: The hemp extract and CBD significantly decreased TNF-α release by up to 91.05 ± 2.91% and 50.78 ± 7.21% of LPS activity, respectively, in a dose-dependent manner, compared to 10 µg/mL hydrocortisone (61.67 ± 3.79%). The hemp extract and CBD also significantly decreased IL-1ß release, also in dose-dependent response, up to 78.03 ± 3.34% and 85.87 ± 1.11% of LPS activity, respectively, compared to 5 µg/mL hydrocortisone (80.81 ± 3.55%). The mean percentage of closure of the wound area was 27.92 ± 1.21% when exposed to 5 µg/mL hemp extract and 33.49 ± 1.67% when exposed to 0.5 µg/mL CBD, compared to 24.34 ± 2.29% for non-treated control. CONCLUSIONS: Our study demonstrates that both hemp extract and CBD can inhibit TNF-α and IL-1ß production in LPS-induced RAW 264.7 cells and promote wound healing in HGF-1 cells. This is the first to show that short-term exposure to hemp extract and CBD promoted gingival fibroblast wound healing, demonstrating that hemp extract and CBD have potential benefits in the treatment of oral inflammation and ulcers.

Clinical study of Asian skin changes after application of a sunscreen formulation containing grape seed extract.

BACKGROUND: Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by prolonged exposure to ultraviolet (UV) radiation. Although sunscreens are effective in preventing signs of photoaging, polyphenol-rich extracts, for example, grape seed extract (GSE) can provide additional protection through the broad spectrum of biological activities. AIMS: To access the effectiveness of a sunscreen formulation containing GSE as an important cosmetic ingredient for the improvement of age-related changes in Asian skin using noninvasive evaluation techniques. METHODS: Noninvasive methods were used to assess changes in the biophysical properties corresponding to aging signs including melanin and erythema indices, color parameters of the CIE L*a*b* system, elasticity, and hydration of the forearm skin before and after applying the sunscreen with GSE. In addition, to confirm the effectiveness of the tested product, we compared it with benchmark sunscreen, and a cream base containing either GSE or UV filters. RESULTS: Twice-daily application of sunscreen containing 3% GSE significantly reduced the level of melanin and erythema and improved overall skin tone. The hydration was drastically increased after 3 h of wearing formulation and was maintained relatively high for 5 h. Skin elasticity parameters, including Young's modulus, retraction time, and viscoelasticity, improved in participants of all age categories (35-59 years). Moreover, sunscreen with GSE, as acclaimed by participants, improved overall skin appearance. CONCLUSIONS: The balancing potential of GSE on the skin, combined with the photoprotective properties of UV filters demonstrated an added value as an anti-aging agent and proved efficacy for both photo- and chronologically-aged Asian skin.

Effects of Acanthus ebracteatus Vahl. extract and verbascoside on human dermal papilla and murine macrophage.

Androgenic alopecia is a common type of hair loss, usually caused by testosterone metabolism generating dihydrotestosterone and hair follicular micro-inflammation. These processes induce dermal papilla cells to undergo apoptosis. Currently approved effective medications for alopecia are Finasteride, an oral 5α-reductase inhibitor, Minoxidil, a topical hair growth promoter, and Diclofenac, an anti-inflammatory agent, all of which, however, have several adverse side effects. In our study, we showed the bioactivity of Acanthus ebracteatus Vahl. (AE) extract performed by 95% ethanol, and verbascoside (VB), a biomarker of AE extract. Both AE extract and VB were studied for their effects on dermal papilla cell viability and the cell cycle by using MTT assay and flow cytometry. The effect of an anti-inflammatory activity of AE extract and VB on IL-1ß, NO, and TNF-α, released from LPS induced RAW 264.7 cells, and IL-1α and IL-6 released from irradiated dermal papilla cells were detected using ELISA technique. The preventive effect on dermal papilla cell apoptosis induced by testosterone was determined by MTT assay. In controlled in vitro assays it was found that AE extract and VB at various concentrations induced dermal papilla cell proliferation which was indicated by an increase in the number of cells in the S and G2/M phases of the cell cycle. AE extract at 250 µg/mL concentration or VB at 62.50 µg/mL concentration prevented cell apoptosis induced by testosterone at a statistically significant level. In addition, both AE extract and VB greatly inhibited the release of pro-inflammatory cytokines from RAW 264.7 and dermal papilla cells. The release of IL-1ß, TNF-α, and NO from RAW 264.7 cells, as well as IL-1α and IL-6 from dermal papilla cells, was also diminished by AE extract 250 µg/mL and VB 125 µg/mL. Our results indicate that AE extract and VB are promising ingredients for anti-hair loss applications. However, further clinical study is necessary to evaluate the effectiveness of AE extract and VB as treatment for actual hair loss.

Effect of green tea extract loaded chitosan microparticles on facial skin: A split-face, double-blind, randomized placebo-controlled study.

INTRODUCTION: The bioactivities of green tea extract were indicated to promote skin health in vitro. Few clinical studies reported on skin nourishment of topical applying green tea extract due to the limited skin absorption. METHODS: This current study evaluated the clinical effectiveness and safety of green tea extract encapsulated chitosan microparticles (GTP) in emulsion base on a split-face, double-blind, randomized placebo-controlled study. Twenty-nine female volunteers were recruited into the study. They were randomly assigned to apply GTP and placebo creams on each half face for 8 weeks. The facial skin properties on both sides were monitored and evaluated every 2 weeks. RESULTS: The results revealed that skin elasticity (R2) of half face treated with GTP cream (0.748 ± 0.05) was superior to another that received placebo cream (0.722 ± 0.05) at 4th week. In addition, melanin index implying skin dullness of the half face that received GTP cream significantly improved within the 6th week after application (placebo =295.60 ± 58.81, GTP =282.70 ± 59.62). Most importantly, the photographs clearly indicated that the decreasing in facial wrinkles of volunteers applied with GTP cream was more than those applying placebo cream. Signs of skin irritation were not evident in both treatment and placebo cream groups. CONCLUSION: Based on study outcomes, the green tea extract encapsulated chitosan microparticles appear to be the promising active candidate for promoting skin elasticity and improving skin dullness and wrinkles.

Effects of Essential Oils and Some Constituents from Ingredients of Anti-Cellulite Herbal Compress on 3T3-L1 Adipocytes and Rat Aortae.

Cellulite is associated with a complex array of adipocytes under the skin and vascular system. A herbal compress that was previously developed was proven to have an anti-cellulite effect in healthy volunteers within 2 weeks of treatment. However, its mechanism and ingredients responsible for reducing cellulite were not known. The purpose of this study was to investigate the activity of eight essential oils in, and two water extracts from, the ingredients of the herbal compress together with nine monoterpenoid constituents on the 3T3-L1 adipocytes. The vasodilatory effect on rat aortae was also studied. The adipocytes were induced by dexamethasone, 3-isobutyl-1-methylxanthine and insulin. At all concentrations tested, all essential oils, water extracts and their monoterpenoid constituents significantly inhibited lipid accumulation activity (p < 0.05) and decreased the amount of triglycerides when compared to untreated cells (p < 0.01). In addition, our results showed that the mixed oil distilled from the herbal compress mixed ingredients could relax the isolated rat aorta (EC50 = 14.74 ± 2.65 µg/mL). In conclusion, all essential oils, extracts and chemical constituents tested showed effects on adipogenesis inhibition and lipolysis induction on the cultured adipocytes with the mixed oil demonstrating vasorelaxation activity, all of which might be the mechanisms of the anti-cellulite effects of the herbal compress.

Effect of grape seed extract on skin fibroblasts exposed to UVA light and its photostability in sunscreen formulation.

BACKGROUND: Grape seed extract (GSE) is rich in polyphenolic compounds, particularly (+)-catechin (C) and (-)-epicatechin (EC). Strong antioxidant activity of these compounds makes GSE to be value-added to the cosmetics with anti-aging properties. However, a lack of stability in different environmental conditions makes GSE challenging for the development of photostable cosmetic sunscreen products. AIMS: To evaluate photoprotective effects of GSE on human dermal fibroblasts irradiated with UVA light and assess photostability of catechins in cream formulations containing GSE alone or in combination with octyl methoxycinnamate (OMC). METHODS: MTT assay was used to assess protective effects of GSE on fibroblasts irradiated with UVA light. A photostability of C and EC in GSE and in cream formulation containing GSE was investigated using high-performance liquid chromatography and confirmed by reflection and transmission spectrophotometry using Transpore™ tapes and polymethacrylate (PMMA) plates as substrates. RESULTS: High UVA doses damaged fibroblast structure and inhibited their growth. However, GSE increased cell viability and effectively protected them from UVA damage. Photostability of C and EC was achieved by combination of GSE and OMC that also improved absorption capacity of UV filter and increased overall efficacy of formulation. PMMA plates showed better applicability for in vitro photostability testing of sunscreen formulations. However, despite the instability of Transpore® tape under heat from UV exposure, it can still be economically a substrate of alternative choice for screening. CONCLUSIONS: GSE can be used as an effective and sustainable natural resource for prevention of UV-induced skin damage providing long-term protection against premature skin aging.

Thermal Degradation Kinetics and pH-Rate Profiles of Iriflophenone 3,5-C-ß-d-diglucoside, Iriflophenone 3-C-ß-d-Glucoside and Mangiferin in Aquilaria crassna Leaf Extract.

The health benefits of the Aquilaria crassna Pierre ex Lecomte leaf extract (AE) make it very useful as an ingredient in food and pharmaceutical products. Iriflophenone 3,5-C-ß-d-diglucoside (1), iriflophenone 3-C-ß-d-glucoside (2) and mangiferin (3) are bioactive compounds of AE. We assessed the stability of AE by investigating the thermal degradation kinetics and shelf-life (t90%) of compounds 1, 2 and 3 using Arrhenius plot models and studied their pH-rate profiles. The results demonstrate that 1 and 2 were degraded, following a first-order kinetic reaction. The degradation of 3 followed first-order reaction kinetics when present in a solution and second-order reaction kinetics in the dried powder form of the extract. According to the first-order kinetic model, the predicted shelf-life (t90%) of the extract at 25 °C in dried form for compound 1 was 989 days with activation energy 129.86 kJ·mol-1, and for 2 it was 248 days with activation energy 110.57 kJ·mol-1, while in the extract solution, the predicted shelf-life of compounds 1-3 was 189, 13 and 75 days with activation energies 86.83, 51.49 and 65.28 kJ·mol-1, respectively. In addition, the pH-rate profiles of 1-3 indicated that they were stable in neutral to acidic environments.

Inhibition of 5α-Reductase, IL-6 Secretion, and Oxidation Process of Equisetum debile Roxb. ex Vaucher Extract as Functional Food and Nutraceuticals Ingredients.

This study aims to investigate the biological activities related to hair loss of Equisetum debile extracts, including 5α-reductase inhibition, interleukin-6 (IL-6) secretion reduction, and anti-oxidation. E. debile extracts were obtained by maceration in various solvents. Crude extract (CE) was obtained by maceration in 95% ethanol. Chlorophyll-free extract (CF) was the CE which of the chlorophyll has been removed by electrocoagulation. Hexane extract (HE), ethyl acetate extract (EA), and ethanolic extract (ET) were fraction extracts obtained from maceration in hexane, ethyl acetate, and 95% ethanol, respectively. The extracts were investigated for inhibitory activity against 5α-reductase and IL-6 secretion. Total phenolic contents (TPC) were investigated and antioxidant activities were determined by means of 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,2'-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP) assays. The inhibition of lipid peroxidation was determined by the ferric thiocyanate method. The cytotoxicity of the extracts on dermal papilla cells and irritation test by hen's egg test chorioallantoic membrane assay were also investigated. All extracts could inhibit 5α-reductase and decrease IL-6 secretion in lipopolysaccharide-stimulated macrophage. The antioxidant activity of E. debile extracts was directly related to their TPC. ET which contained the highest TPC (68.8 ± 6.7 mg GA/g) showed the highest equivalent concentration (EC1) of 289.1 ± 26.4 mM FeSO4/g, TEAC of 156.6 ± 34.6 mM Trolox/g, and 20.0 ± 6.0% DPPH inhibition. However, EA exhibited the highest inhibition against lipid peroxidation (57.2 ± 0.4%). In addition, EA showed no cytotoxicity on dermal papilla cell line and no irritation on chorioallantoic membrane of hen's eggs. In conclusion, EA was suggested as the most attractive ingredients for functional food and nutraceuticals because of the high inhibitory activity against 5α-reductase, IL-6 secretion, and lipid peroxidation inhibition.

Curcuma aeruginosa Roxb. essential oil slows hair-growth and lightens skin in axillae; a randomised, double blinded trial.

BACKGROUND: Androgenic hair-growth contributes to secondary gender characteristics but can be troublesome in women. Inhibiting axillary hair-growth via 5-α-reductases using the Thai medicinal plant, Curcuma aeruginosa Roxb. is an attractive treatment strategy. HYPOTHESIS/PURPOSE: C. aeruginosa essential oil (CA-oil) formulated as a lotion is an efficacious and safe inhibitor of axillary hair growth. STUDY DESIGN: This trial was a single center, randomized, double-blind, placebo controlled 10 weeks, intervention in 60 women (18-23 years) and 2 weeks washout with axillary hair length was the primary end-point. METHODS: Bioactive-enriched essential oil of C. aeruginosa was formulated with a base lotion. All participants were pre-challenged with lotions by 4-h patch irritation tests to exclude skin reactions. Participants were randomly allocated to use either 1 or 5%w/w CA-oil lotion on one axilla and base-lotion (placebo) to the other for 10 weeks followed by placebo in both axillae for 2 weeks. Every week, the axillae were photographed to measure hair lengths, shaved, and roll-on applicators containing appropriate lotion replaced. Also, skin melanin by spectrophotometry and hair density were measured. RESULTS: From weeks 5-11 of trial, 1 and 5%w/w CA-oil retarded growth by 13 ± 1.5% and 16 ± 0.9% respectively, while placebo was ineffective. CA-oil had no influence on hair density. Both concentrations of CA-oil rapidly and equally effectively brightened skin within 3 weeks which persisted 2 weeks after treatment ceased while placebo darkened the skin. Adherence appeared good as judged by consistency of lotion consumption and between axillae. Participants were satisfied with the treatment and reported reduced hairiness, freedom from any discomforts, but product odour attracted some negative comment. No adverse reactions ascribed to CA-oil were detected or reported. CONCLUSION: This study points to a safe and efficacious dual action on retarding hair-growth and skin lightening by CA-oil.

Germacrene Analogs are Anti-androgenic on Androgen-dependent Cells.

Anti-androgenic drugs are treatments for androgen-related disorders such as benign prostatic hyperplasia, acne, hirsutism, and androgenic alopecia. Germacrone (1), a sesquiterpene isolated from hexane extracts of Curcuma aeruginosa Roxb. rhizome, is an androgen inhibitor of steroid 5-alpha reductase in- vitro. Here, we used the similarity of germacrone's ,t,B-unsaturated carbonyl to testosterone's α,ß-unsaturated carbonyl to find germacrene analogs obtained from this plant and by semi-synthesis that might be more potent steroid 5-alpha reductase inhibitors. 8-Hydroxy germacrene B (4) was -13-fold more potent than its parent, I and the most potent (ICso, 0.15 ± 0.022 mM) among 9 compounds tested. The conformation of its cyclodecadiene ring and the α,ß-unsaturated ketone/hydroxy in the germacrene molecule might be crucial role for its anti-androgen activity. Moreover, I and 4 showed mild cytotoxic effect on prostate cancer cells. Neither compound was cytotoxic towards human dermal papilla cells at 100 µg/mL. We show that this SAR strategy created promising anti-androgenics for androgen dependent disorders and may create further analogues with further improvements in selectivity and clinical efficacy.