Biological activities of extracts and compounds from Thai Kae-Lae (Maclura cochinchinensis (Lour.) Corner).

BACKGROUND AND AIMS: The purpose of this study was to investigate the biological properties of Kae-Lae (Maclura cochinchinensis (Lour.) Corner), a traditional medicinal plant used in Ayurvedic recipes in Thailand. To achieve this objective, heartwood samples were collected from 12 sources across Thailand. Fractional extracts (n-hexane, ethyl acetate, and ethanol) and the dominant compounds (morin, resveratrol, and quercetin) were examined for their abilities on cytotoxicity, antioxidant, anti-inflammation, and antileukaemic activity (Wilms' tumour 1 protein was used as a well-known biomarker for leukaemic cell proliferation). METHODS: The study used MTT to assess cytotoxicity in leukaemic cells (K562, EoL-1, and KG-1a). Antioxidant activities were evaluated using ABTS, DPPH, and FRAP assays. The anti-inflammatory activity was investigated by detecting IL-2, TNF-α, and NO using appropriate detection kits. Wilms' tumour 1 protein expression was measured by Western blotting to determine the anti-leukaemic activity. The inhibition of cell migration was also analyzed to confirm anticancer progression. RESULTS: Among the tested extract fraction, ethyl acetate No. 001 displayed strong cytotoxicity specifically in EoL-1 cells, while n-hexane No. 008 demonstrated this effect in three cell lines. Resveratrol, on the other hand, displayed cytotoxicity in all the tested cells. Additionally, the three major compounds, morin, resveratrol, and quercetin, exhibited significant antioxidant and anti-inflammatory properties. In particular, resveratrol demonstrated a noteworthy decreased Wilms' tumour 1 protein expression and a reduction in cell proliferation across all cells. Moreover, ethyl acetate No. 001, morin, and resveratrol effectively inhibited MCF-7 cell migration. None of these compounds showed any impact on red blood cell haemolysis. CONCLUSION: Based on these findings, it can be concluded that Kae-Lae has promising chemotherapeutic potential against leukaemic cells, with fractional extracts (ethyl acetate and n-hexane) and resveratrol exhibiting the most potent cytotoxic, antioxidant, anti-inflammatory, and anti-cell migration activities.

Ultrasound-assisted green extraction methods: An approach for cosmeceutical compounds isolation from Macadamia integrifolia pericarp.

This study aimed was to examine the potential of several green extraction methods to extract cosmetic/cosmeceutical components from Macadamia integrifolia pericarps, which were a by-product of the macadamia nut industry. M. integrifolia pericarps were extracted by conventional solvent extraction process using 95% v/v ethanol and various green extraction methods, including infusion, ultrasound, micellar, microwave, and pulsed electric field extraction using water as a clean and green solvent. The extracts were evaluated for total phenolic content using Folin-Ciocalteu method.The antioxidant activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing/antioxidant power, and ferric-thiocyanate method. The anti-skin ageing activities were investigated by means of collagenase, elastase, and hyaluronidase inhibition using enzyme-substrate reaction assay. The irritation profile of the extracts was evaluated by the hen's egg test-chorioallantoic membrane (HET-CAM) test. The results noted that ultrasound-assisted extraction yielded the significantly highest extract amount with the significantly highest total phenolic content (p < 0.05), especially when the extraction time was 10 min. The aqueous extract from ultrasound-assisted extraction possessed the most potent antioxidant and anti-skin ageing activities (p < 0.05). Its antioxidant activities were comparable to ascorbic acid and Trolox, whereas the anti-skin ageing activities were equivalent to epigallocatechin-3-gallate and oleanolic acid. Besides, the extract was safe since it induced no irritation in the HET-CAM test. Therefore, ultrasound-assisted extraction was suggested as an environmentally friendly extraction method for M. integrifolia pericarp extraction and further application in the cosmetic/cosmeceutical industries.

Phytochemical, Antioxidant, Antihyaluronidase, Antityrosinase, and Antimicrobial Properties of Nicotiana tabacum L. Leaf Extracts.

Nicotiana tabacum L. (tobacco) is an important and valuable crop for the cigarette industry. However, cigarette cessation has been encouraged worldwide. Therefore, this study aimed to investigate the potential of N. tabacum leaf extract use in other industries besides cigarette production, especially cosmeceutical industries, which are of interest for increasing the value and widening the applications of N. tabacum. The leaves of N. tabacum var. Virginia and Turkish were extracted by maceration using 95% v/v ethanol or petroleum ether. The extracts were evaluated for their phytochemical compositions, antioxidant capacity, and anti-aging, antimelanogenic, and antimicrobial activities. The phytochemical screening of the extracts revealed terpenoids, steroids, alkaloids, tannins, and carbohydrates in all of the N. tabacum leaf extracts. The total phenolic content was detected to be the highest in the ethanolic extract of Virginia tobacco leaf, which had the most significantly potent antioxidant and antihyaluronidase activity (P < 0.05). On the contrary, the extracts from the Turkish variety demonstrated the most powerful antimicrobial activity against Staphylococcus aureus. Thus, ethanolic extracts of N. tabacum var. Virginia are suggested as good natural anti-aging ingredients with potent antioxidant and antihyaluronidase effects, whereas the leaf of N. tabacum var. Turkish is suggested as a good source of natural antimicrobial components, particularly for S. aureus inhibition. In summary, in addition to the cigarette industry, N. tabacum leaf could be a source of pharmaceutical and cosmeceutical compounds, particularly natural anti-aging and antimicrobial ingredients.

Antileukaemic Cell Proliferation and Cytotoxic Activity of Edible Golden Cordyceps (Cordyceps militaris) Extracts.

Golden cordyceps (Cordyceps militaris) is a mushroom of the genus Cordyceps. It has been used as a food supplement for both healthy and ill people. In this study, the antileukaemic cell proliferation activities of golden cordyceps extracts were examined and compared with standard cordycepin (CDCP) in EoL-1, U937, and KG-1a cells. Wilms' tumour 1 (WT1) protein was used as a biomarker of leukaemic cell proliferation. The cytotoxicity of the extracts on leukaemic cells was determined using the MTT assay. Their inhibitory effects on WT1 protein expression and cell cycle progression of EoL-1 cells were investigated using Western blotting and flow cytometry, respectively. Induction of KG-1a cell differentiation (using CD11b as a marker) was determined using flow cytometry. The golden cordyceps extracts exhibited cytotoxic effects on leukaemic cells with the highest IC50 value of 16.5 ± 3.9 µg/mL, while there was no effect on normal blood cells. The expression levels of WT1 protein in EoL-1 cells were decreased after treatment with the extracts. Moreover, cell cycle progression and cell proliferation were inhibited. The levels of CD11b increased slightly following the treatment. All these findings confirm the antileukaemic proliferation activity of golden cordyceps.

Enhanced Antioxidant, Hyaluronidase, and Collagenase Inhibitory Activities of Glutinous Rice Husk Extract by Aqueous Enzymatic Extraction.

In this research, we aimed to compare the biological activities related to cosmeceutical applications of glutinous rice husk extracted by aqueous enzymatic extraction (AEE) and conventional solvent extraction. Cellulase enzymes were used to assist the extraction process. The vanillic and ferulic acid contents of each extract were investigated by high-performance liquid chromatography, and their antioxidant and anti-aging activities were investigated by spectrophotometric methods. The irritation effects of each extract were investigated by the hen's egg test on chorioallantoic membrane. The rice husk extract from AEE using 0.5% w/w of cellulase (CE0.5) contained the significantly highest content of vanillic and ferulic acid (p < 0.05), which were responsible for its biological activities. CE0.5 was the most potent antioxidant via radical scavenging activities, and possessed the most potent anti-skin wrinkle effect via collagenase inhibition. Aside from the superior biological activities, the rice husk extracts from AEE were safer than those from solvent extraction, even when 95% v/v ethanol was used. Therefore, AEE is suggested as a green extraction method that can be used instead of the traditional solvent extraction technique given its higher yield and high quality of bioactive compounds. Additionally, CE0.5 is proposed as a potential source of natural antioxidants and anti-aging properties for further development of anti-wrinkle products.

Potential cosmeceutical lamellar liquid crystals containing black longan (Dimocarpus longan Lour.) seed extract for MMP-1 and hyaluronidase inhibition.

The aims of this study were to evaluate the biological activities of black Dimocarpus longan Lour. seed extracts and develop a lamellar liquid crystal (LLC). Different solvents, including petroleum ether, ethyl acetate, and 95% v/v ethanol, were used in the maceration of black D. longan seeds. The inhibitory activities on matrix metalloproteinase-1 (MMP-1) and hyaluronidase were evaluated. The irritating potency of D. longan seed extracts was determined using the hen's egg chorioallantoic membrane test. The extract with the strongest anti-ageing activities and no irritant impact was examined for its chemical contents using high-performance liquid chromatography and incorporated into the LLC. Various factors affecting the LLC formulations, including surfactant types and amounts, thickening agent types and amounts, and various oil types, were investigated. The results demonstrated that the ethyl acetate extract (EtOAc) was the most potent inhibitor of MMP-1 (IC50 = 21.7 ± 5.4 µg/mL) and hyaluronidase (oleanolic acid equivalent = 0.44 ± 0.03 g per g extract). Interestingly, its MMP-1 inhibition was equivalent to that of oleanolic acid, corilagin, and gallic acid. Furthermore, its hyaluronidase inhibition was equivalent to that of gallic acid and ellagic acid. Gallic acid, which was the most abundant compound (15.6% ± 0.06% w/w) was suggested as the compound responsible for the biological activities of EtOAc extract. Considering its potential anti-skin ageing properties with no irritation of EtOAc extract, it was incorporated into the most suitable LLC, which was composed of 5% w/w Lexfeel® D5 oil, 0.5% w/w Carbopol® U21, 2% w/w Liquid Crystal Cream Maker, and 92.5% w/w DI water. The LLC containing EtOAc extract presented birefringence under a polarizing light microscope, indicating its crystallinity. The formulation had good stability after heating-cooling cycles in terms of external appearance, crystallinity, viscosity, and pH (5.5). As a result, it is recommended as a potential cosmeceutical formulation for anti-skin wrinkling. It is proposed that more research be conducted on the safety and efficacy of the treatment on human volunteers.

Comparison of chemical profiles, antioxidation, inhibition of skin extracellular matrix degradation, and anti-tyrosinase activity between mycelium and fruiting body of Cordyceps militaris and Isaria tenuipes.

CONTEXT: Cordyceps militaris and Isaria tenuipes (Cordycipitaceae) are high-value fungi that are used for health-promoting food supplements. Since laboratory cultivation has begun for these fungi, increased output has been achieved. OBJECTIVE: This study compared the chemical profiles, antioxidant, anti-tyrosinase, and skin extracellular matrix degradation inhibition between mycelium and fruiting body of C. militaris and I. tenuipes. MATERIALS AND METHODS: The antioxidative potential of 10% v/v aqueous infused extract from each fungus was separately investigated using 2,2-azinobis(3-ethylbenzo-thiazoline-6-sulphonic acid) (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant ability, and ferric thiocyanate methods. The inhibition against MMP-1, elastase, and hyaluronidase were determined to reveal their anti-wrinkle potential. Anti-tyrosinase activities were determined. RESULTS: C. militaris and I. tenuipes extracts were found to contain a wide range of bioactive compounds, including phenolics, flavonoids, and adenosine. A correlation was discovered between the chemical compositions and their biological activities. The extract from I. tenuipes fruiting body (IF) was highlighted as an extraordinary elastase inhibitor (IC50 = 0.006 ± 0.004 mg/mL), hyaluronidase inhibitor (IC50: 30.3 ± 3.2 mg/mL), and antioxidant via radical scavenging (ABTS IC50: 0.22 ± 0.02 mg/mL; DPPH IC50: 0.05 ± 0.02 mg/mL), thereby reducing ability (EC1: 95.3 ± 4.8 mM FeSO4/g extract) and lipid peroxidation prevention (IC50: 0.40 ± 0.11 mg/mL). IF had a three-times higher EC1 value than ascorbic acid and significantly higher elastase inhibition than epigallocatechin gallate. DISCUSSION AND CONCLUSIONS: IF is proposed as a powerful natural extract with antioxidant and anti-wrinkle properties; therefore, it is suggested for further use in pharmaceutical, cosmeceutical, and nutraceutical industries.

Anti-Inflammatory and Antimicrobial Activities of Fermented Ocimum sanctum Linn. Extracts against Skin and Scalp Microorganisms.

This study aimed to revealed anti-inflammatory and antimicrobial activities of fermented Ocimum sanctum Linn. (FE). The fermentation process with Lactobacillus plantarum was compared with the solvent extraction methods. Antimicrobial activity against the growth of Staphylococcus aureus, Staphylococcus epidermidis, Propionibacterium acnes, Candida albicans, and Malassezia furfur was investigated via broth dilution method. High performance thin layer chromatography was used to determine eugenol content. The anti-inflammation was investigated by means of nuclear factor kappa B (NF-κB) expression inhibition by Western blot analysis. FE yielded the highest amount (11.93 % w/w), the highest eugenol content (39.3±12.6 % w/w), and the highest antimicrobial activities comparing to the extracts obtained from the solvent extractions. The fungal inhibition against M. furfur 656 was equivalent to that of ketoconazole. Furthermore, the bacterial inhibition on S. aureus and S. epidermidis was compared to that of Penicillin G at minimum inhibitory concentration (MIC) of 0.125 mg/mL and 0.25 mg/mL, respectively. Interestingly, FE had lower MIC and minimum bactericidal concentration against P. acnes than Penicillin G and also possessed comparable anti-inflammatory activity to indomethacin with the NF-κB suppression of 42.7±4.6 %. Therefore, FE are potentially natural anti-inflammation and antimicrobial agents for topical applications in the pharmaceutical and cosmetic industries.

Enhancement of phenolics content and biological activities of longan (Dimocarpus longan Lour.) treated with thermal and ageing process.

This study is the first to compare the chemical compositions and biological activities of a conventional dried Dimocarpus longan with a novel black D. longan that underwent a thermal ageing process. Pericarp, aril, and seed of both D. longan were macerated in 95% v/v ethanol. Their chemical compositions were investigated using a Folin-Ciocalteu assay, aluminum chloride assay, and high-performance liquid chromatography. Antioxidant activities were evaluated in terms of radical scavenging and iron (III) reduction capacity. An enzyme inhibition assay was used to evaluate the hyaluronidase inhibition. Inflammatory cytokine secretion was evaluated with an enzyme-linked immunosorbent assay. After being exposed to a heating and ageing procedure, gallic acid and ellagic acid content were increased tenfold, while the corilagin content was doubled. Black D. longan seed extract was the most potent anti-hyaluronidase and antioxidant with the strongest free radical scavenging and reduction power, while black D. longan aril extract resulted in the highest inhibition of inflammatory cytokine secretion. Black D. longan contained more biologically active compounds and possessed more potent biological activities than conventional dried D. longan. Therefore, thermal ageing treatment is suggested for producing black D. longan, for which seed extract is suggested as a cosmeceutical active ingredient and aril extract for anti-inflammation.

Herbal Extracts as Potential Antioxidant, Anti-Aging, Anti-Inflammatory, and Whitening Cosmeceutical Ingredients.

The aim of this research was to investigate and compare the antioxidant, anti-tyrosinase, anti-aging, and anti-inflammatory activities of 16 herbal extracts for topical application in cosmetic/cosmeceutical products. Herbal plant materials were extracted by infusion in boiled water for 15 min. The total phenolic content and total flavonoid content of each extract were investigated by the Folin-Ciocalteu and aluminum chloride methods, respectively. Antioxidant activities were investigated using 2,2'-diphenyl-1-picrylhydrazyl and a ferric reducing antioxidant power assay. Anti-tyrosinase and anti-aging activities were investigated using an in vitro enzymatic-spectrophotometric method. Anti-inflammatory activities were investigated using an enzyme-linked immunosorbent assay. The findings show that the Stevia rebaudiana extract has the most significant levels of both phenols and flavonoids (p<0.05). The S. rebaudiana, Rosa damascene, and Phyllanthus emblica extracts possessed the most significant antioxidant activities (p<0.05) and a promising whitening effect with moderate anti-tyrosinase activities. Furthermore, the Echinacea purpurea extract possessed the most significant anti-collagenase (78.5±0.0 %), anti-elastase (69.0±1.4 %), and anti-hyaluronidase activity (64.2±0.3 %). The Morus alba extract possessed the most significant anti-inflammatory activity since it could inhibit the secretion of interleukin-6 and tumor necrosis factor-α (p<0.05). Therefore, these herbal extracts have promising skin benefits and have potential for use as active ingredients in cosmetic/cosmeceutical products.

Nutricosmetic effects of Asparagus officinalis: a potent matrix metalloproteinase-1 inhibitor.

This study aimed to investigate the nutricosmetic effect of Asparagus officinalis extracts. The tip and spear of A. officinalis were successively extracted with 95% ethanol. The rutin, phenolic, and flavonoid contents of A. officinalis extracts were investigated. The antioxidant activities were determined by 2,2-azinobis (3-ethylbenzothiazoline-6-sulphonic acid) and a ferric reducing antioxidant power assay. Matrix metalloproteinase-1 (MMP-1), elastase, and hyaluronidase inhibition were determined by in vitro enzyme reaction assay. The cytotoxicity was analyzed on peripheral blood mononuclear cellss. Findings revealed that drying temperature and drying duration had significant effects on the chemical composition and biological activity of A. officinalis extract. A. officinalis tips dried at 50 °C for 24 h contained the (significantly) highest flavonoid and rutin content. The most potent extract was from A. officinalis spears since it possessed the (significantly) highest MMP-1, elastase, and hyaluronidase inhibition rates of 83.4 ± 1.5%, 70.4 ± 4.1%, and 75.2 ± 1.0%, respectively. Interestingly, at the same concentration, the A. officinalis spear extract was more potent in MMP-1 inhibition than oleanolic acid and epigallocatechin gallate, the well-known natural MMP-1 inhibitors. The results show that A. officinalis extract is an attractive source of natural anti-skin-wrinkle ingredients.

Cytotoxic and Antiproliferative Effects of Diarylheptanoids Isolated from Curcuma comosa Rhizomes on Leukaemic Cells.

Curcuma comosa belongs to the Zingiberaceae family. In this study, two natural compounds were isolated from C. comosa, and their structures were determined using nuclear magnetic resonance. The isolated compounds were identified as 7-(3,4-dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene (1) and trans-1,7-diphenyl-5-hydroxy-1-heptene (2). Compound 1 showed the strongest cytotoxicity effect against HL-60 cells, while its antioxidant and anti-inflammatory properties were stronger than those of compound 2. Compound 1 proved to be a potent antioxidant, compared to ascorbic acid. Neither compounds had any effect on red blood cell haemolysis. Furthermore, compound 1 significantly decreased Wilms' tumour 1 protein expression and cell proliferation in KG-1a cells. Compound 1 decreased the WT1 protein levels in a time- and dose- dependent manner. Compound 1 suppressed cell cycle at the S phase. In conclusion, compound 1 has a promising chemotherapeutic potential against leukaemia.

Isolation and biological activity of agrostophillinol from kaffir lime (Citrus hystrix) leaves.

The leaves of the kaffir lime (Citrus hystrix) are commonly used in cuisine and folk medicine. The aim of this study was to isolate a bioactive compound in kaffir lime leaves and characterize its biological activity. The compound was isolated from a hexane fractional extract and identified as agrostophillinol. This is the first report of agrostophillinol isolated from kaffir lime leaves. In terms of cytotoxicity, agrostophillinol exhibited IC50 values of 36.27 ± 7.30 and 53.44 ± 10.63 µg/mL against EoL-1 and HL60 cells, respectively. Agrostophillinol also exhibited potent anti-inflammatory activity, significantly inhibiting IL-6 secretion.

Enhancement of the Antioxidant, Anti-Tyrosinase, and Anti-Hyaluronidase Activity of Morus alba L. Leaf Extract by Pulsed Electric Field Extraction.

In this study we aimed to compare the chemical composition and biological activity between Morus alba L. leaf extract obtained with 95% v/v ethanol using a pulsed electric field (PEF) and the conventional maceration method. Extracts of M. alba leaves collected from Chiang Mai (CM), Sakon Nakon (SK), and Buriram (BR), Thailand, were investigated for 1-deoxynojirimycin content by high-performance liquid chromatography and for total phenolic content by the Folin-Ciocalteu method. Antioxidant activity was investigated by 2,2'-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethylbenzothiazoline-6-sulphonate (ABTS), and ferric reducing antioxidant power (FRAP) assay. Anti-tyrosinase and anti-hyaluronidase activity was investigated by in vitro spectrophotometry. The results show that this is the first study to indicate PEF as a novel method for enhancing the phenolic content and antioxidant, anti-tyrosinase, and anti-hyaluronidase activity of M. alba leaf extract (P < 0.05). PEF extract of M. alba leaves collected from BR had comparable ABTS•+ scavenging activity to l-ascorbic acid and comparable anti-tyrosinase activity to kojic acid (P > 0.05). On the other hand, PEF extract of M. alba leaves collected from SK exhibited significantly high anti-hyaluronidase activity, comparable to that of oleanolic acid (P > 0.05). Therefore, PEF is suggested for further M. alba leaf extraction in the production of natural whitening and anti-aging cosmetic ingredients.

Chemical Constituents, Antioxidant, Anti-MMPs, and Anti-Hyaluronidase Activities of Thunbergia laurifolia Lindl. Leaf Extracts for Skin Aging and Skin Damage Prevention.

This study aimed to investigate the potential usage of Thunbergia laurifolia Lindl. leaf extracts in the cosmetic industry. Matrix metalloproteinases (MMPs) and hyaluronidase inhibition of T. laurifolia leaf extracts, prepared using reflux extraction with deionized water (RE) and 80% v/v ethanol using Soxhlet's apparatus (SE), were determined. Rosmarinic acid, phenolics, and flavonoids contents were determined using high-performance liquid chromatography, Folin-Ciocalteu, and aluminum chloride colorimetric assays, respectively. Antioxidant activities were determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and linoleic acid-thiocyanate assays. MMP-1 inhibition was investigated using enzymatic and fluorescent reactions, whereas MMP-2, MMP-9, and hyaluronidase inhibition were investigated using gel electrophoresis. Cytotoxicity on human fibroblast cell line was also investigated. The results demonstrated that SE contained significantly higher content of rosmarinic acid (5.62% ± 0.01%) and flavonoids (417 ± 25 mg of quercetin/g of extract) but RE contained a significantly higher phenolics content (181 ± 1 mg of gallic acid/g of extract; p < 0.001). SE possessed higher lipid peroxidation inhibition but less DPPH• scavenging activity than RE. Both extracts possessed comparable hyaluronidase inhibition. SE was as potent an MMP-1 inhibitor as gallic acid (half maximal inhibitory concentration values were 12.0 ± 0.3 and 8.9 ± 0.4 mg/cm3, respectively). SE showed significantly higher MMP-2 and MMP-9 inhibition than RE (p < 0.05). Therefore, SE is a promising natural anti-ageing ingredient rich in rosmarinic acid and flavonoids with antioxidant, anti-hyaluronidase, and potent MMPs inhibitory effects that could be applied in the cosmetic industry.

In-vitro investigation of anti-acne properties of Mangifera indica L. kernel extract and its mechanism of action against Propionibacterium acnes.

Propionibacterium acnes has been recognized as a main target for medical treatment of acne since this bacterium promotes acne inflammation by inducing upregulation of pro-inflammatory cytokines production, resulting in an accumulation of neutrophils and oxygen-free radicals produced by neutrophils within acne lesion. The aims of this study were to evaluate the biological activities of Mangifera indica kernel extracts grown in Northern Thailand (Kaew-Moragot cultivar), related to anti-acne properties including antimicrobial effect against acne-inducing bacteria together with the first elucidation of the mechanism of action against Propionibacterium acnes, anti-oxidation, and anti-inflammation. The kernels of M. indica, obtained from raw and ripe fruits, were macerated using various solvents. Agar diffusion and broth microdilution methods were performed to investigate the antibacterial activities of the extracts against P. acnes, Staphylococcus aureus, and Staphylococcus epidermidis. The ethanolic fractions exhibited the strongest antimicrobial effect against P. acnes with minimum inhibitory concentration and minimum bactericidal concentration of 1.56 mg/mL and 12.50 mg/mL, respectively. Bactericidal effect against P. acnes of these extracts could be observed after 3 h of incubation from time-kill curve. The chromatograms of high-performance liquid chromatography showed that the extracts existed gallic acid with high total phenolic content. These extracts additionally showed strong free radical scavenging properties on 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) as well as a notable inhibitory effect on linoleic acid peroxidation, which highly correlated to their antimicrobial effect, total phenolic, and gallic acid contents. The images, studied through using transmission electron microscopy, revealed that the extract certainly disrupted P. acnes cell membrane after exposure for 1 h as well as induced the consequent leakage of cytoplasmic materials. The inhibitory effects of the extracts on IL-8 secretion from LPS-inducing RAW 264.7 cells were also presented. In conclusion, the kernel extracts of raw M. indica fruit were effective against aerobic and anaerobic acne-inducing bacteria particularly P. acnes and exerted antioxidant along with anti-inflammatory activities. Therefore, the extracts might be potential agents for inflammatory acne treatment. However, clinical study is needed for further investigation.

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.

Characterization and in vitro permeation study of microemulsions and liquid crystalline systems containing the anticholinesterase alkaloidal extract from Tabernaemontana divaricata.

The aims of the present study were to characterize the microstructure and study the skin permeation enhancement of formulations containing the alkaloidal extract from Tabernaemontana divaricata. The extract was loaded in the formulations composed of Zingiber cassumunar oil, Triton X-114, ethanol and water with the oil:surfactant ratios of 1:5 and 2:5. The formulations were characterized by photon correlation spectroscopy, polarizing light microscopy, differential scanning calorimetry, and viscosity measurement. A reverse micellar phase, w/o microemulsions, liquid crystalline systems, liquid crystal in microemulsion systems and coarse emulsions were formed along the aqueous dilution line of both oil:surfactant ratios. Formulations with the ratio of 1:5 containing 0.1 µg/ml extract showed a significantly higher acetylcholinesterase inhibition than those with the ratio of 2:5. The skin of stillborn piglet was used in the permeation study. The liquid crystalline and microemulsion systems significantly increased the transdermal delivery of the extract within 24h. It was concluded that the alkaloidal extract from T. divaricata stem loaded in liquid crystalline or microemulsion systems comprising Z. cassumunar oil/Triton X-114/ethanol/water may act as an alternative percutanous formulations for enhancing the acetylcholine level in Alzheimer's patients.

3'-R/S-hydroxyvoacamine, a potent acetylcholinesterase inhibitor from Tabernaemontana divaricata.

Guided by the acetylcholinesterase inhibiting activity, the bisindole alkaloid 3'-R/S-hydroxyvoacamine was isolated from a stem extract of Tabernaemontana divaricata, a plant used in Thailand in traditional rejuvenation remedies for improving the memory. The structure of the alkaloid was elucidated by extensive use of NMR spectroscopy and the complete assignment of the (1)H and (13)C NMR spectra is reported. The alkaloid acted as a non-competitive inhibitor against AChE with an IC50 value of 7.00±1.99 µM. An HPLC method was developed for the quantitative analysis of the AChE inhibitor. It suggested that there was 12.4% (w/w) of 3'-R/S-hydroxyvoacamine in the alkaloid enriched fraction of T. divaricata stem.

Inhibition of cholinesterase by essential oil from food plant.

Inhibition of cholinesterase has attracted much attention recently because of its potential for the treatment of Alzheimer's disease. In this work, the anticholinesterase activities of plant oils were investigated using Ellman's colorimetric method. The results indicate that essential oils obtained from Melissa officinalis leaf and Citrus aurantifolia leaf showed high acetylcholinesterase and butyrylcholinesterase co-inhibitory activities. C. aurantifolia leaf oil revealed in this study has an IC(50) value on acetylcholinesterase and butyrylcholinesterase of 139 ± 35 and 42 ± 5 µg/ml, respectively. GC/MS analysis revealed that the major constituents of C. aurantifolia leaf oil are monoterpenoids including limonene, l-camphor, citronellol, o-cymene and 1,8-cineole.