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1.
Molecules ; 28(15)2023 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-37570790

RESUMO

The objectives of this study were (1) to investigate the effect of extracts from some plants in the families Nelumbonaceae and Nymphaeaceae on phosphodiesterase 5 (PDE5) and arginase, which have been used in erectile dysfunction treatment, and (2) to isolate and identify the compounds responsible for such activities. The characterization and quantitative analysis of flavonoid constituents in the active extracts were performed by HPLC. Thirty-seven ethanolic extracts from different parts of plants in the genus Nymphaea and Victoria of Nymphaeaceae and genus Nelumbo of Nelumbonaceae were screened for PDE5 and arginase inhibitory activities. The ethanolic extracts of the receptacles and pollens of Nelumbo nucifera Gaertn., petals of Nymphaea cyanea Roxb. ex G.Don, Nymphaea stellata Willd., and Victoria amazonica (Poepp.) Sowerby and the petals and receptacles of Nymphaea pubescens Willd. showed IC50 values on PDE5 of less than 25 µg/mL while none of the extracts showed effects on arginase. The most active extract, N. pubescens petal extract, was fractionated to isolate and identify the PDE5 inhibitors. The results showed that six flavonoid constituents including quercetin 3'-O-ß-xylopyranoside (1), quercetin 3-methyl ether 3'-O-ß-xylopyranoside (2), quercetin (3), 3-O-methylquercetin (4), kaempferol (5) and 3-O-methylkaempferol (6) inhibited PDE5 with IC50 values at the micromolar level.


Assuntos
Nelumbo , Nelumbonaceae , Nymphaea , Nymphaeaceae , Humanos , Masculino , Quercetina , Nucleotídeo Cíclico Fosfodiesterase do Tipo 5 , Arginase , Extratos Vegetais/farmacologia , Flavonoides/análise
3.
Foods ; 11(19)2022 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-36230143

RESUMO

Obesity and overweight have serious health outcomes. "Phikud Tri-Phon" (PTP) is a traditional Thai medicine comprising three dried fruits from Aegle marmelos L., Morinda citrifolia L., and Coriandrum sativum L. Whether this medicine impacts on metabolic disease is unclear. This study aimed to investigate the phenolic and flavonoid contents of PTP and each of its herbal components, and further assess their antioxidant and anti-adipogenetic activities. Oil-red O staining was measured for lipid accumulation in 3T3-L1 adipocytes. The chemical profiles of PTP and each herbal extract were determined by LC-ESI-QTOF-MS/MS. Our results show that the total phenolic and flavonoid contents of PTP water extract were 22.35-108.42 mg of gallic acid equivalents and PTP ethanolic extract was 1.19-0.93 mg of quercetin equivalents and the DPPH scavenging capacity assay of PTP ethanolic extract (1 mg/mL) was 92.45 ± 6.58 (Trolox equivalent)/g. The PTP extracts and individual herbs had inhibitory adipogenesis activity, which reduced lipid accumulation by approximately 31% in PTP water extract and 22% in PTP ethanolic extract compared with control cells. These results provided insights into the traditional preparation method of using boiling water as a vehicle for PTP. In conclusion, PTP has antioxidant and anti-adipogenesis potential, indicating it is a promising ingredient in functional food and herbal health products.

4.
Chem Biodivers ; 19(7): e202200121, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35652145

RESUMO

Eurycoma longifolia (EL) and Eurycoma harmandiana (EH) are natural medicinal plants belonging to the Simaroubaceae family, and are well-known for their ability to enhance male sexual performance. The present study investigated the phosphodiesterase-5 (PDE-5) inhibitory activity of intact roots of EL and EH. Additionally, canthin-6-one alkaloids, ß-carboline alkaloids, and quassinoids were also screened for PDE-5 inhibitory activity. We developed in vitro root and callus cultures of EL and EH to determine their PDE-5 inhibitory activity. Our results indicated that canthin-6-one alkaloids, which include canthin-6-one-9-O-ß-D-glucopyranoside, 9-methoxycanthin-6-one, canthin-6-one, and 9-hydroxycanthin-6-one, exhibited PDE-5 enzymatic inhibitory activity, with IC50 values of 2.86±0.23, 3.30±1.03, 4.31±0.52, and 4.66±1.13 µM, respectively. The ethanolic extract of the intact roots of EL and EH, and the in vitro root culture of EH had large amounts of canthin-6-one alkaloids (1.50±0.04, 2.12±0.03, and 3.48±0.08 mg/g dry weight, respectively), and showed potent PDE-5 inhibition. Our findings indicate that in vitro root cultures of EH may be used to replace intact plants, and canthin-6-one-9-O-ß-D-glucopyranoside should be further investigated for development as a health supplement.


Assuntos
Alcaloides , Eurycoma , Alcaloides/farmacologia , Carbolinas/farmacologia , Nucleotídeo Cíclico Fosfodiesterase do Tipo 5 , Alcaloides Indólicos , Extratos Vegetais/farmacologia , Raízes de Plantas
6.
J Cosmet Dermatol ; 21(11): 6109-6117, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35675125

RESUMO

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.


Assuntos
Plantas Medicinais , Humanos , Plantas Medicinais/metabolismo , Androgênios , Testosterona/metabolismo , Alopecia/tratamento farmacológico , Alopecia/metabolismo , Células Cultivadas , Colestenona 5 alfa-Redutase/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Folículo Piloso
7.
Molecules ; 27(9)2022 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-35566245

RESUMO

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.


Assuntos
Lamiaceae , Verbenaceae , 3-Oxo-5-alfa-Esteroide 4-Desidrogenase , Inibidores de 5-alfa Redutase/farmacologia , Colestenona 5 alfa-Redutase , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/farmacologia , Hexanos , Extratos Vegetais/farmacologia
8.
Arch Oral Biol ; 140: 105464, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35623115

RESUMO

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.


Assuntos
Canabidiol , Cannabis , Úlceras Orais , Animais , Anti-Inflamatórios/farmacologia , Canabidiol/farmacologia , Humanos , Hidrocortisona/farmacologia , Lipopolissacarídeos/farmacologia , Camundongos , Extratos Vegetais/farmacologia , Fator de Necrose Tumoral alfa , Cicatrização
9.
Sci Rep ; 12(1): 5992, 2022 04 09.
Artigo em Inglês | MEDLINE | ID: mdl-35397625

RESUMO

Eulophia macrobulbon (E.C.Parish & Rchb.f.) Hook.f. contains a natural PDE5A1 inhibitor, phenanthrene, 1-(4'-hydroxybenzyl)-4,8- dimethoxyphenanthrene-2,7-diol (HDP), a potential agent for the treatment of erectile dysfunction. The aim of this study was to improve the extraction efficiency of HDP from E. macrobulbon by using a more environmentally friendly extraction method, subcritical liquid dimethyl ether extraction (sDME), instead of classical solvent extraction (CSE) and ultrasound-assisted extraction (UAE). The efficiency and quality of the extracts obtained were evaluated using the following criteria: %process yield; solvent amount; extraction time; temperature; %HDP content by LC-MS, bioactivity as inhibition of phosphodiesterase-5A1 (PDE5A1) by radio-enzymatic assay; and chemical profiles by LC-QTOF-MS. sDME provided the highest content of HDP in the extract at 4.47%, much higher than the use of ethanol (0.4-0.5%), ethyl acetate (1.2-1.7%), or dichloromethane (0.7-1.4%). The process yield for sDME (1.5-2.7%) was similar to or lower than the other solvents (0.9-17%), but as long as the process yield is not prohibitively low, the concentration is a more important measure for clinical use. The optimal conditions for sDME extraction were: Extraction time, 40 min; 200% water as co-solvent; sample-to-solvent ratio of 1:8; temperature, 35 °C. Phenanthrene aglycone and glycoside derivatives were the major constituents of the sDME extracts and lesser amounts of phenolic compounds and sugars. The inhibition of PDE5A1 by sDME (IC50 0.67 ± 0.22 µg/ml) was tenfold more potent than ethanolic extract and other extraction methods, suggesting a high probability of clinical efficacy. Thus, sDME was a more efficient, faster, solvent-saving and environmentally friendly extraction method and more selective for phenanthrene when extracted from E. macrobulbon.


Assuntos
Orchidaceae , Diester Fosfórico Hidrolases , Etanol/química , Éteres Metílicos , Orchidaceae/química , Fenantrenos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Solventes
10.
Sci Rep ; 12(1): 1491, 2022 01 27.
Artigo em Inglês | MEDLINE | ID: mdl-35087085

RESUMO

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.


Assuntos
Acanthaceae/química , Alopecia/tratamento farmacológico , Glucosídeos/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Animais , Proliferação de Células/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Glucosídeos/uso terapêutico , Folículo Piloso/efeitos dos fármacos , Humanos , Macrófagos , Camundongos , Fenóis/uso terapêutico , Extratos Vegetais/uso terapêutico , Células RAW 264.7
11.
J Cosmet Dermatol ; 21(9): 4001-4008, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34965006

RESUMO

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.


Assuntos
Quitosana , Envelhecimento da Pele , Antioxidantes , Quitosana/efeitos adversos , Método Duplo-Cego , Emolientes , Emulsões , Feminino , Guanosina Trifosfato , Humanos , Melaninas , Extratos Vegetais/efeitos adversos , Chá
12.
Pharmaceuticals (Basel) ; 14(9)2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34577542

RESUMO

Recently, the herbal compress was successfully developed and applied for cellulite treatment. The aim of this study was to formulate a more convenient dosage form of herbal application from the original formula. In addition, we aimed to characterize and evaluate the stability of the developed dosage form. A gelled emulsion, or an "emgel," incorporated with 0.1 wt% tea and coffee extracts (1:1 ratio) plus 5 wt% essential oils (mixed oil) was prepared. The caffeine content in the finished product obtained from tea and coffee extracts analyzed by HPLC was 48.1 ± 2.3 µg/g. The bio-active marker monoterpenes of mixed oil characterized by headspace GCMS were camphene 50.8 ± 1.8 µg/mg, camphor 251.0 ± 3.2 µg/mg, 3-carene 46.7 ± 1.8 µg/mg, α-citral 75.0 ± 2.1 µg/mg, ß-citral 65.6 ± 1.3 µg/mg, limonene 36.8 ± 6.7 µg/mg, myrcene 53.3 ± 4.5 µg/mg, α-pinene 85.2 ± 0.6 µg/mg, ß-pinene 88.4 ± 1.1 µg/mg, and terpinene-4-ol 104.3 ± 2.6 µg/mg. The stability study was carried out over a period of 3 months at 4, 25, and 50 °C. The caffeine content showed no significant changes and passed the acceptance criteria of ≥80% at all tested temperatures. However, monoterpenes showed their stability for only 2 months at 50 °C. Therefore, the shelf-life of the emgel was, consequently, calculated to be 31 months using the Q10 method. Thus, the anti-cellulite emgel was successfully formulated. The characterization methods and stability evaluation for caffeine and monoterpenes in an emgel matrix were also successfully developed and validated.

13.
Pharmaceuticals (Basel) ; 14(7)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34358109

RESUMO

Cellulite describes unsightly skin overlying subcutaneous fat around thighs and buttocks of post-pubescent females. A herbal 'emgel' containing volatile oils and extracts of A traditional Thai herbal compress was tested in a double-blind, placebo-controlled trial with 18 women aged 20-50 year with severe cellulite. Appearance of cellulite (primary outcome), thigh circumferences, skin firmness, and cutaneous blood flow (secondary outcomes) were assessed at baseline, 2, 4, 8 and 12 weeks with a 2-week follow-up. Herbal emgel applied onto the thigh skin twice daily reduced cellulite severity scores in every time point. The score was reduced from 13.4 ± 0.3 (baseline) to 12.1 ± 0.3 (week 2) and 9.9 ± 0.6 (week 12). All secondary outcomes improved with both placebo and herbal emgels suggesting that ingredients in the base-formulation might be responsible. Querying of participants, analysis of their diaries, and physical monthly inspections found no adverse events. The herbal emgel safely improved the appearance of cellulite, while the base emgel may play a role for other endpoints. Further studies on the active constituents and their mechanism of action are needed to further explore these factors.

14.
J Basic Clin Physiol Pharmacol ; 32(4): 313-317, 2021 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-34214376

RESUMO

OBJECTIVES: Alzheimer's disease (AD) is a degenerative brain disease characterized by confusion, behavior changes, decline in memory and cognitive skills. One of the strategies in the treatment of AD is to use acetylcholinesterase (AChE) inhibitors. The current study aims to determine the AChE inhibitory activities of the extract and fractions of the root of Rauvolfia serpentina. METHODS: Extraction was carried out by maceration method using ethanol, followed by liquid-liquid partition using n-hexane, ethyl acetate and n-butanol. Further fractionation was conducted by using vacuum liquid chromatography (VLC). The AChE inhibitory assays were performed by using Ellmann's method. Phytochemical screening was carried out by TLC method. RESULTS: The ethanolic extract of R. serpentina showed inhibition against AChE enzyme with an IC50 value of 7.46 µg/mL. The extract and fractions showed higher inhibition against butyrylcholinesterase (BChE) compared to AChE. Amongst three fractions obtained, the n-butanol fraction showed the strongest inhibition with an IC50 value of 5.99 µg/mL against AChE. VLC fractionation of the n-butanol fraction yielded 13 subfractions (VLC 1-VLC 13). Four out of 13 subfractions gave more than 80% inhibition against AChE, namely subfractions 4-7, with IC50 values ranging from 4.87 to 47.22 µg/mL. The phytochemical screening of these subfractions suggested the presence of alkaloids. CONCLUSIONS: The ethanolic extract, as well as fractions of R. serpentina root, are potential for AChE inhibitor. The alkaloid compound may be responsible for this activity.


Assuntos
Acetilcolinesterase/metabolismo , Alcaloides , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , Rauwolfia , 1-Butanol , Butirilcolinesterase , Compostos Fitoquímicos
15.
Molecules ; 26(10)2021 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-34063409

RESUMO

Brahmi essence, developed from Bacopa monnieri (L.) Wettst. standardized extract and mulberry juice, was proven to improve the memory speed of healthy participants aged 55-80 years old, following a 12-week dietary program. However, the metabolites have not yet been reported. Our objective was to characterize the altered metabolites in the plasma, urine, and feces of healthy volunteers after consumption of Brahmi essence for 12 weeks, using the LC-MS metabolomics approach. The altered metabolites were selected from OPLS-DA S-plots; 15 metabolites in the plasma, 7 in the urine, and 17 in the feces samples were tentatively identified by comparison with an online database and literature. The metabolites in the plasma samples were in the classes of amino acids, acylcarnitine, and phospholipids. Benzeneactamide-4-O-sulphate and 3-hydroxyhippuric acid were found in urine samples. The metabolites in the class of amino acids, together with jujubogenin and pseudojujubogenin, were identified in the fecal samples. The aminoacyl-tRNA, aromatic amino acids, and branched-chain amino acid biosynthetic pathways were mainly related to the identified metabolites in all three samples. It could be implied that those metabolites and their pathways might be linked with the effect of Brahmi essence on memory speed.


Assuntos
Bacopa/química , Fezes/química , Metabolômica/métodos , Morus/química , Extratos Vegetais/administração & dosagem , Plasma/química , Urina/química , Idoso , Idoso de 80 Anos ou mais , Cromatografia Líquida , Método Duplo-Cego , Feminino , Sucos de Frutas e Vegetais , Voluntários Saudáveis , Humanos , Masculino , Pessoa de Meia-Idade , Extratos Vegetais/farmacocinética
16.
Pharmaceuticals (Basel) ; 14(3)2021 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-33799756

RESUMO

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.

17.
Molecules ; 26(5)2021 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-33668176

RESUMO

Colorectal cancer is a common cancer worldwide and reduced expression of the DNA repair endonuclease XPF (xeroderma pigmentosum complementation group F) is associated with colorectal cancer. Bacopa monnieri extracts were previously found to exhibit chemical-genetic synthetic lethal effects in a Saccharomyces cerevisiae model of colorectal cancer lacking Rad1p, a structural and functional homologue of human XPF. However, the mechanisms for B. monnieri extracts to limit proliferation and promote an apoptosis-like event in RAD1 deleted yeast was not elucidated. Our current analysis has revealed that B. monnieri extracts have the capacity to promote mutations in rad1∆ cells. In addition, the effects of B. monnieri extracts on rad1∆ yeast is linked to disruption of the vacuole, similar to the mammalian lysosome. The absence of RAD1 in yeast sensitizes cells to the effects of vacuole disruption and the release of proteases. The combined effect of increased DNA mutations and release of vacuolar contents appears to induce an apoptosis-like event that is dependent on the meta-caspase Yca1p. The toxicity of B. monnieri extracts is linked to sterol content, suggesting saponins may be involved in limiting the proliferation of yeast cells. Analysis of major constituents from B. monnieri identified a chemical-genetic interaction between bacopasaponin C and rad1∆ yeast. Bacopasaponin C may have potential as a drug candidate or serve as a model for the development of analogs for the treatment of colorectal cancer.


Assuntos
Bacopa/química , Enzimas Reparadoras do DNA/metabolismo , Endonucleases/metabolismo , Glicosídeos/farmacologia , Extratos Vegetais/farmacologia , Proteínas de Saccharomyces cerevisiae/metabolismo , Triterpenos/farmacologia , Vacúolos/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Enzimas Reparadoras do DNA/deficiência , Enzimas Reparadoras do DNA/genética , Endonucleases/deficiência , Endonucleases/genética , Glicosídeos/química , Extratos Vegetais/química , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/metabolismo , Proteínas de Saccharomyces cerevisiae/genética , Triterpenos/química , Vacúolos/metabolismo
18.
Nat Prod Res ; 35(19): 3220-3225, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31762341

RESUMO

A new alkaloid, amabiloid A (1) was isolated from Crinum amabile along with eleven known compounds. Their structures were determined by 1D and 2D NMR spectroscopic data. In addition, the acetyl- and butyrylcholinesterase inhibitory activities of the isolated compounds were evaluated.


Assuntos
Alcaloides de Amaryllidaceae , Inibidores da Colinesterase/farmacologia , Crinum , Alcaloides de Amaryllidaceae/isolamento & purificação , Alcaloides de Amaryllidaceae/farmacologia , Butirilcolinesterase , Inibidores da Colinesterase/isolamento & purificação , Crinum/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais
19.
Clin Exp Rheumatol ; 39(5): 1003-1010, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33025883

RESUMO

OBJECTIVES: The effect of coffee on serum uric acid (SUA) has shown conflicting results. This study was to determine the effects of caffeinated coffee (CC) and decaffeinated coffee (DC) on SUA, serum xanthine oxidase activity (sXOA) and urine uric acid clearance (UAC). METHODS: This was a prospective randomised within-subject experimental study design of 51 healthy male participants. Each study period consisted of 3 periods, including a control, an intervention, and washout period for 1, 3 and 1 week, respectively. During the intervention period, the participants received 2, 4 or 6 gram/day of coffee, either CC or DC. RESULTS: For DC groups, SUA significantly decreased by 6.5 (±1.1) mg/dL to 6.2 (±1.1) mg/dL during the intervention period (p=0.014). sXOA significantly increased by 0.05 (±0.07) nmol/min/mL to 0.20 (±0.38) nmol/min/mL during the intervention period (p=0.010) of CC. For UAC, there was no significant change with CC or DC. In hyperuricaemic participants, SUA significantly decreased by 7.7 (±0.7) mg/dL to 7.2 (±0.7) mg/dL during the intervention period (p=0.028) of DC. For non-hyperuricaemic, CC significantly increased SUA by 5.9 (±0.7) mg/dL to 6.2 (±0.9) mg/dL during the intervention period (p=0.008) and significantly decreased SUA to 6.0 (±0.8) mg/dL (p=0.049) during the withdrawal period. A significant increase of sXOA according with SUA in CC groups from 0.05 (±0.07) nmol/min/mL to 0.25 (±0.44) nmol/min/mL during the intervention period (p=0.040) was presented in non-hyperuricaemic participants. CONCLUSIONS: DC had a significant decrease of SUA during the intervention period. However, in non-HUS participants, SUA significantly increased in CC.


Assuntos
Hiperuricemia , Ácido Úrico , Café , Humanos , Hiperuricemia/induzido quimicamente , Masculino , Estudos Prospectivos
20.
Molecules ; 25(21)2020 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-33113908

RESUMO

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.


Assuntos
Glucosídeos/química , Extratos Vegetais/química , Folhas de Planta/química , Lectinas de Plantas/química , Temperatura , Thymelaeaceae/química , Xantonas/química , Concentração de Íons de Hidrogênio , Cinética
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