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1.
Int J Biol Macromol ; 273(Pt 2): 133119, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38880452

RESUMEN

Ethyl cellulose (EC)-based composite sponges were developed for oil spillage treatment. The EC sponge surface was decorated with helical carbon nanotubes (HCNTs) and molybdenum disulfide (MoS2) (1 phr) using the inside-out sugar templating method. The inside surface of a sugar cube was coated with HCNTs and MoS2. After filling the sugar cube pores with EC and the subsequent sugar leaching, the decorating materials presented on the sponge surface. The EC/HCNT/MoS2 sponge had a high level of oil removal based on its adsorption capacity (41.68 g/g), cycled adsorption (∼75-79 %), separation flux efficiency (∼85-95 %), and efficiency in oil/water emulsion separation (92-94 %). The sponge maintained adsorption capacity in acidic, basic, and salty conditions, adsorbed oil under water, and functioned as an oil/water separator in a continuous pump-assisted system. The compressive stress and Young's modulus of the EC sponge increased following its decoration using HCNTs and MoS2. The composite sponge was robust based on cycled compression and was thermally stable up to ∼120 οC. Based on the eco-friendliness of EC, the low loading of HCNTs and MoS2, and sponge versatility, the developed EC/HCNT/MoS2 sponge should be good candidate for use in sustainable oil adsorption and separation applications.


Asunto(s)
Celulosa , Disulfuros , Molibdeno , Nanotubos de Carbono , Celulosa/química , Celulosa/análogos & derivados , Disulfuros/química , Nanotubos de Carbono/química , Adsorción , Molibdeno/química , Agua/química , Aceites/química , Purificación del Agua/métodos
2.
Int J Biol Macromol ; 268(Pt 2): 131789, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38677708

RESUMEN

Polysaccharides have gained attention as valuable supplements and natural medicinal resources, particularly for their anti-tumor properties. Their low toxicity and potent anti-tumor effects make them promising candidates for cancer prevention and treatment. The tumor microenvironment is crucial in tumor development and offers potential avenues for novel cancer therapies. Research indicates that polysaccharides can positively influence the tumor microenvironment. However, the structural complexity of most anti-tumor polysaccharides, often heteropolysaccharides, poses challenges for structural analysis. To enhance their pharmacological activity, researchers have modified the structure and properties of natural polysaccharides based on structure-activity relationships, and they have discovered that many polysaccharides exhibit significantly enhanced anti-tumor activity after chemical modification. This article reviews recent strategies for targeting the tumor microenvironment with polysaccharides and briefly discusses the structure-activity relationships of anti-tumor polysaccharides. It also summarises the main chemical modification methods of polysaccharides and discusses the impact of chemical modifications on the anti-tumor activity of polysaccharides. The review aims to lay a theoretical foundation for the development of anti-tumor polysaccharides and their derivatives.


Asunto(s)
Neoplasias , Polisacáridos , Microambiente Tumoral , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/uso terapéutico , Microambiente Tumoral/efectos de los fármacos , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Animales , Relación Estructura-Actividad , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Productos Biológicos/farmacología , Productos Biológicos/química , Productos Biológicos/uso terapéutico
3.
Int J Biol Macromol ; 262(Pt 1): 130257, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38423904

RESUMEN

The genus Schisandra, a member of the Magnoliaceae family, is a well-known tonic traditional Chinese medicine with a long history of traditional medicinal and functional food used in China. Polysaccharides are one of its main active constituents, which have a wide range of bioactivities, such as anti-inflammatory, anti-tumor, neuroprotection, anti-diabetes, hepatoprotection, immunomodulation, and anti-fatigue. In this paper, we review the extraction, isolation, purification, structural characterization, bioactivities, as well as structure-activity relationship of polysaccharides from the genus Schisandra. In conclusion, we hope that this review could provide reference for the subsequent research on structural, bioactivities, development and application of the genus Schisandra polysaccharides.


Asunto(s)
Ciclooctanos , Lignanos , Compuestos Policíclicos , Schisandra , Schisandra/química , Polisacáridos/química , Extractos Vegetales/química , Antioxidantes
4.
Plants (Basel) ; 11(24)2022 Dec 14.
Artículo en Inglés | MEDLINE | ID: mdl-36559626

RESUMEN

Leaves of guava (Psidium guajava L.) have been used in Thai folk medicine without any supporting evidence as a traditional herbal remedy for hair loss. Androgenetic alopecia (AGA) is chronic hair loss caused by effects of androgens in those with a genetic predisposition, resulting in hair follicle miniaturization. Our objectives were to provide the mechanistic assessment of guava leaf extract on gene expressions related to the androgen pathway in well-known in vitro models, hair follicle dermal papilla cells (HFDPC), and human prostate cancer cells (DU-145), and to determine its bioactive constituents and antioxidant activities. LC-MS analysis demonstrated that the main components of the ethanolic extract of guava leaves are phenolic substances, specifically catechin, gallic acid, and quercetin, which contribute to its scavenging and metal chelating abilities. The guava leaf extract substantially downregulated SRD5A1, SRD5A2, and SRD5A3 genes in the DU-145 model, suggesting that the extract could minimize hair loss by inhibiting the synthesis of a potent androgen (dihydrotestosterone). SRD5A suppression by gallic acid and quercetin was verified. Our study reveals new perspectives on guava leaf extract's anti-androgen properties. This extract could be developed as alternative products or therapeutic adjuvants for the treatment of AGA and other androgen-related disorders.

5.
Molecules ; 27(10)2022 May 16.
Artículo en Inglés | MEDLINE | ID: mdl-35630643

RESUMEN

The present study aimed to develop a nicotine microemulsion (NCT-ME) and incorporate it into a fast-dissolving film. The NCT-ME was prepared by mixing the specified proportions of nicotine (NCT), surfactant, co-solvent, and water. The NCT-ME was measured by its average droplet size, size distribution, zeta potential, and morphology. NCT-ME fast-dissolving films were prepared by the solvent casting technique. The films were characterized by morphology, weight, thickness, disintegration time, and mechanical strength properties and the determined NCT loading efficiency and in vitro drug release. The results showed that almost all NCT-MEs presented droplet sizes of less than 100 nm with a spherical form, narrow size distribution, and zeta potentials of -10.6 to -73.7 mV. There was no difference in weight and thickness between all NCT-ME films, but significant changes in the disintegration times were noticed in NCT40-Smix[PEG-40H(2:1)]10 film. The mechanical properties of films varied with changes in type of surfactant. About 80% of the drug release was observed to be between 3 and 30 min. The drug release kinetics were fitted with the Higuchi matrix model. The NCT40-Smix[P-80(1:1)]10 film showed the highest dissolution rate. It was concluded that the developed ME-loaded fast-dissolving film can increase drug release to a greater extent than the films without ME.


Asunto(s)
Nicotina , Cese del Hábito de Fumar , Excipientes , Solubilidad , Solventes , Tensoactivos
6.
Molecules ; 27(5)2022 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-35268636

RESUMEN

Oily skin from overactive sebaceous glands affects self-confidence and personality. There is report of an association between steroid 5-alpha reductase gene (SRD5A) expression and facial sebum production. There is no study of the effect of Asparagus racemosus Willd. root extract on the regulation of SRD5A mRNA expression and anti-sebum efficacy. This study extracted A. racemosus using the supercritical carbon dioxide fluid technique with ethanol and investigated its biological compounds and activities. The A. racemosus root extract had a high content of polyphenolic compounds, including quercetin, naringenin, and p-coumaric acid, and DPPH scavenging activity comparable to that of the standard L-ascorbic acid. A. racemosus root extract showed not only a significant reduction in SRD5A1 and SRD5A2 mRNA expression by about 45.45% and 90.86%, respectively, but also a reduction in the in vivo anti-sebum efficacy in male volunteers, with significantly superior percentage changes in facial sebum production and a reduction in the percentages of pore area after 15 and 30 days of treatment. It can be concluded that A. racemosus root extract with a high content of polyphenol compounds, great antioxidant effects, promising downregulation of SRD5A1 and SRD5A2, and predominant facial sebum reduction and pore-minimizing efficacy could be a candidate for an anti-sebum and pore-minimizing active ingredient to serve in functional cosmetic applications.


Asunto(s)
Asparagus , Dióxido de Carbono , 3-Oxo-5-alfa-Esteroide 4-Deshidrogenasa/genética , 3-Oxo-5-alfa-Esteroide 4-Deshidrogenasa/metabolismo , Asparagus/química , Dióxido de Carbono/metabolismo , Humanos , Masculino , Proteínas de la Membrana/metabolismo , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacología , ARN Mensajero/genética , ARN Mensajero/metabolismo , Sebo
7.
Plants (Basel) ; 11(3)2022 Jan 26.
Artículo en Inglés | MEDLINE | ID: mdl-35161311

RESUMEN

Androgenetic alopecia (AGA), a hair loss disorder, is a genetic predisposition to sensitive androgens, inflammation, and oxidative stress. Unfortunately, current treatments with synthetic medicines contain a restricted mechanism along with side effects, whereas the bioactive constituents of plant extracts are multifunctional, with fewer side effects. The massive amounts of rice husk and bran are agricultural wastes that may cause pollution and environmental problems. Owing to these rationales, the local rice variety, Bue Bang 3 CMU (BB3CMU), which is grown in northern Thailand, was evaluated for the valuable utilization of rice by-products, husk (BB3CMU-H) and bran (BB3CMU-RB) extracts, for AGA treatment regarding antioxidant, anti-inflammatory, anti-androgenic activities, and the characterization of bioactive compounds. Our study verified that BB3CMU-H had the highest level of polyphenols, contributing to its greater antioxidant activity. Conversely, BB3CMU-RB was the predominant source of tocopherols, resulting in better anti-androgenic activities regarding the downregulation of steroid 5α-reductase genes (SRD5A). Notably, anti-inflammation via the attenuation of nitric oxide productions was observed in BB3CMU-H (0.06 ± 0.13 µM) and BB3CMU-RB (0.13 ± 0.01 µM), which were significantly comparable to diclofenac sodium salt (0.13 ± 0.19 µM). Therefore, the combination of BB3CMU-H and BB3CMU-RB could be utilized in cosmeceutical and pharmaceutical applications for AGA patients.

8.
J Fungi (Basel) ; 7(12)2021 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-34947082

RESUMEN

Dictyophora indusiata or Phallus indusiatus is widely used as not only traditional medicine, functional foods, but also, skin care agents. Biological activities of the fruiting body from D. indusiata were widely reported, while the studies on the application of immature bamboo mushroom extracts were limited especially in the wound healing effect. Wound healing process composed of 4 stages including hemostasis, inflammation, proliferation, and remodelling. This study divided the egg stage of bamboo mushroom into 3 parts: peel and green mixture (PGW), core (CW), and whole mushroom (WW). Then, aqueous extracts were investigated for their nucleotide sequencing, biological compound contents, and wound healing effect. The anti-inflammatory determination via the levels of cytokine releasing from macrophages, and the collagen stimulation activity on fibroblasts by matrix metalloproteinase-2 (MMP-2) inhibitory activity were determined to serve for the wound healing process promotion in the stage 2-4 (wound inflammation, proliferation, and remodelling of the skin). All D. indusiata extracts showed good antioxidant potential, significantly anti-inflammatory activity in the decreasing of the nitric oxide (NO), interleukin-1 (IL-1), interleukin-1 (IL-6), and tumour necrosis factor-α (TNF-α) secretion from macrophage cells (p < 0.05), and the effective collagen stimulation via MMP-2 inhibition. In particular, CW extract containing high content of catechin (68.761 ± 0.010 mg/g extract) which could significantly suppress NO secretion (0.06 ± 0.02 µmol/L) better than the standard anti-inflammatory drug diclofenac (0.12 ± 0.02 µmol/L) and their MMP-2 inhibition (41.33 ± 9.44%) was comparable to L-ascorbic acid (50.65 ± 2.53%). These findings support that CW of D. indusiata could be an essential natural active ingredient for skin wound healing pharmaceutical products.

9.
Polymers (Basel) ; 13(20)2021 Oct 17.
Artículo en Inglés | MEDLINE | ID: mdl-34685337

RESUMEN

A hydrogel scaffold is a localized drug delivery system that can maintain the therapeutic level of drug concentration at the tumor site. In this study, the biopolymer hydrogel scaffold encapsulating doxorubicin was fabricated from gelatin, sodium carboxymethyl cellulose, and gelatin/sodium carboxymethyl cellulose mixture using a lyophilization technique. The effects of a crosslinker on scaffold morphology and pore size were determined using scanning electron microscopy. The encapsulation efficiency and the release profile of doxorubicin from the hydrogel scaffolds were determined using UV-Vis spectrophotometry. The anti-proliferative effect of the scaffolds against the lung cancer cell line was investigated using an MTT assay. The results showed that scaffolds made from different types of natural polymer had different pore configurations and pore sizes. All scaffolds had high encapsulation efficiency and drug-controlled release profiles. The viability and proliferation of A549 cells, treated with gelatin, gelatin/SCMC, and SCMC scaffolds containing doxorubicin significantly decreased compared with control. These hydrogel scaffolds might provide a promising approach for developing a superior localized drug delivery system to kill lung cancer cells.

10.
Insects ; 12(7)2021 Jul 13.
Artículo en Inglés | MEDLINE | ID: mdl-34357294

RESUMEN

In this work, the chemical compositions of basils oils, including those of lemon basil, white holy basil, Thai basil, tree basil and red holy basil, were analysed. Methyl eugenol was detected in all types of basils. The essential oils of red and white holy basils possessed a comparable ability (~25%) to attract male Oriental fruit fly to the synthesised fruit fly attractant in the laboratory experiment. To control the release of the active ingredients, the white holly basil oil (WBO) was encapsulated with maltodextrin (MD) and gum arabic (GA) by paste method. The essential oil is retained in the wall complex much longer with the addition of MD. The results also revealed that the combination of the MD:GA (25:75) had the highest loading efficiency of the oil (9.40%) as observed by the numerous porous structures by scanning electron microscopy. Fourier-transform infrared spectra of the encapsulated polymer confirmed traces of essential oil functional groups. The field test study advised that WBO-encapsulated products improved fruit fly attractive efficiency by maintaining the release rate of basil essential oil.

11.
Int J Biol Macromol ; 188: 283-289, 2021 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-34343586

RESUMEN

Oil resistant thermoplastic elastomers (TPE) were prepared using mung bean thermoplastic starch (MTPS) blending with rubbers and sericin. Sericin was incorporated into MTPS as a compatibilizer. MTPS with sericin (MTPSS) was blended with natural rubber (NR) and epoxidized NR (ENR). Sericin at 5% improved the tensile strength (10 MPa), elastic recovery (52%) and morphology of the MTPSS/ENR blend. The mechanical properties, elastic recovery and morphology of the MTPSS5/NR blend were improved by the addition of ENR. The MTPSS/ENR showed palm (28%) and motor oils (8%) swelling resistance because of the hydrophilicity of MTPS and high polarity of ENR. The MTPSS/ENR/NR showed gasoline swelling resistance (104%) because of the hydrophilicity of MTPS and low polarity of NR. FTIR confirmed a reaction between the -NH groups of sericin and the epoxy groups of ENR. This reaction improved the compatibility, mechanical properties, elastic recovery, morphology and oils swelling resistance of the blends.


Asunto(s)
Elastómeros/química , Aceites/efectos adversos , Plásticos/química , Fenómenos Bioquímicos , Compuestos Epoxi/química , Aceites/química , Goma/química , Almidón/química , Temperatura , Resistencia a la Tracción/efectos de los fármacos
12.
Membranes (Basel) ; 11(6)2021 May 28.
Artículo en Inglés | MEDLINE | ID: mdl-34071396

RESUMEN

Nicotine (NCT), administered in the form of a fast dissolving oral delivery system, can be a potential alternative to nicotine replacement therapy. NCT was extracted by maceration and acid-base extraction methods from Burley tobacco leaves with different stalk positions and extraction yield and NCT content were further determined. The extract with the highest nicotine content was selected for incorporation into a fast dissolving film formulation. The optimized film was evaluated for its physical and mechanical properties, in vitro disintegration, and drug release profile. The results demonstrated that the extract from the upper part of tobacco leaves using the acid-base extraction method had the highest amount of NCT. NCT fast dissolving film consisting of this extract as the active ingredient and HPMC E15 as a film polymer resulted in a homogeneous translucent film with a light brown color. The addition of NCT significantly affected the film properties in terms of weight, disintegration time, tensile strength, percentage elongation at break, and Young's modulus values. The drug release of NCT fast dissolving film showed a rapid initial release of 80% within three minutes, and its kinetics followed the Higuchi matrix model. The results suggest that these NCT films can be employed in the development of NCT fast dissolving films for clinical use.

13.
Sci Pharm ; 86(3)2018 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-30200490

RESUMEN

This study aimed to encapsulate Celastrus paniculatus seed oil (CPSO) in 2-hydroxypropyl-ß-cyclodextrin (HPßCD) cavities and investigate their biological activity, physicochemical stability, and skin penetration by vertical Franz diffusion cells of the CPSO-HPßCD inclusion complex formulations. For biological activity studies-including 2,2-diphenyl-1-picryhydrazyl radical (DPPH) scavenging, metal ion chelating, and inhibition of lipid and tyrosinase inhibition activities-the CPSO-HPßCD inclusion complex exhibited lower inhibition activity than free CPSO. CPSO-HPßCD dispersion, serum, and gel formulations were prepared. All formulations containing the CPSO-HPßCD inclusion complex showed no significant changes in physical characteristics after three months' storage. The percentages of oleic acid remaining in all formulations were over 80% of the initial amount during a three-month stability study. For the skin-penetration study, compared to other formulations, the CPSO-HPßCD serum formulation exhibited the highest cumulative amount of oleic acid in the whole skin and flux through receptor fluid, after six hours, of 32.75 ± 1.25 µg/cm² and 1.02 ± 0.15 µg/cm²/h, respectively. The CPSO-HPßCD serum formulation also showed the proper viscosity. Hence, the CPSO-HPßCD inclusion complex will be beneficial for the further development of cosmeceutical products.

14.
Nanomaterials (Basel) ; 8(7)2018 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-30029478

RESUMEN

The purpose of this study was to prepare orange oil microemulsion (ME) and to investigate the antimicrobial activity of film containing orange oil ME. First, surfactants and co-surfactants were screened on their efficiency to form ME using pseudo-ternary phase diagrams. The influences of surfactant and co-surfactant mass ratios were studied and optimized ME-loaded-films were prepared. Then, films containing orange oil ME were characterized by SEM and texture analyzer, and then evaluated for antimicrobial activity against Staphylococcus aureus and Propionibacterium acnes using an agar disc diffusion method. The results showed that Tween 80 as surfactant and propylene glycol as co-surfactant at a 1:1 ratio possessed the maximum ME area. Three ME formulations of ME 20, ME 25, and ME 30, which consisted of 20, 25, and 30% w/v of orange oil were prepared, respectively. All ME formulations showed particle sizes of about 60.26⁻80.00 nm, with broad a polydispersity index of 0.42. The orange oil ME films exhibited higher elastic values than the control. The diameters of inhibition zones for FME 20, FME 25, and FME 30 against P. acnes were 13.64, 15.18, and 16.10 mm, respectively. Only the FME 30 had an antimicrobial activity against S. aureus with 8.32 mm of inhibition zone. Contrarily, the control film had no antimicrobial activity against both bacteria. In conclusion, the present study found that the antibacterial activity of orange oil in pectin thin film could be enhanced by preparing orange oil as an ME before loading into pectin thin film.

15.
Polymers (Basel) ; 10(10)2018 Oct 14.
Artículo en Inglés | MEDLINE | ID: mdl-30961069

RESUMEN

This study aims to develop orange oil loaded in thin mango peel pectin films and evaluate their antibacterial activity against Staphylococcus aureus. The mango peel pectin was obtained from the extraction of ripe Nam Dokmai mango peel by the microwave-assisted method. The thin films were formulated using commercial low methoxy pectin (P) and mango pectin (M) at a ratio of 1:2 with and without glycerol as a plasticizer. Orange oil was loaded into the films at 3% w/w. The orange oil film containing P and M at ratio of 1:2 with 40% w/w of glycerol (P1M2GO) showed the highest percent elongation (12.93 ± 0.89%) and the lowest Young's modulus values (35.24 ± 3.43 MPa). For limonene loading content, it was found that the amount of limonene after the film drying step was directly related to the final physical structure of the film. Among the various tested films, P1M2GO film had the lowest limonene loading content (59.25 ± 2.09%), which may be because of the presence of numerous micropores in the P1M2GO film's matrix. The inhibitory effect against the growth of S. aureus was compared in normalized value of clear zone diameter using the normalization value of limonene content in each film. The P1M2GO film showed the highest inhibitory effect against S. aureus with the normalized clear zone of 11.75 mm but no statistically significant difference. This study indicated that the orange oil loaded in mango peel pectin film can be a valuable candidate as antibacterial material for food packaging.

16.
Pak J Pharm Sci ; 30(5): 1521-1527, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29084668

RESUMEN

The cellular mechanisms underlying the anti-inflammatory activity of rutin which has been found to have in vivo inhibitory effects merit more evaluation. The effects of rutin and encapsulated-rutin on lipopolysaccharide (LPS)-induced IL-6 secretion, NF-κB expression, as well as protein denaturation were investigated. The secretion of IL-6 was not found to have significantly reduced upon incubation with either rutin or encapsulated-rutin at all concentrations. At 100 µg/mL, the cells treated with encapsulated-rutin brought about slightly reduced IL-6 secretion but significantly inhibited NF-kB protein expression and protein denaturation in comparison with rutin. Inflammation can be resolved through many mechanisms. The inhibition of IL-6 and NF-kB can serve not only to terminate inflammation but also to inhibit other cytokines or mechanisms. Further investigations are necessary to clarify, verify and establish the anti-inflammatory mechanisms of rutin. Additionally, the encapsulation is an interesting technique for enhancing rutin activity.


Asunto(s)
Antiinflamatorios/farmacología , Portadores de Fármacos , Mediadores de Inflamación/metabolismo , Inflamación/prevención & control , Macrófagos/efectos de los fármacos , Rutina/farmacología , Animales , Antiinflamatorios/química , Composición de Medicamentos , Inflamación/inducido químicamente , Inflamación/inmunología , Inflamación/metabolismo , Mediadores de Inflamación/inmunología , Interleucina-6/metabolismo , Lipopolisacáridos/toxicidad , Macrófagos/inmunología , Macrófagos/metabolismo , Ratones , FN-kappa B/metabolismo , Células RAW 264.7 , Rutina/química , Tecnología Farmacéutica/métodos
17.
J Ethnopharmacol ; 161: 11-7, 2015 Feb 23.
Artículo en Inglés | MEDLINE | ID: mdl-25481081

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Thai/Lanna region has its own folklore wisdoms including the traditional medicinal plant recipes. Thai/Lanna medicinal plant recipe database "MANOSROI III" has been developed by Prof. Dr. Jiradej Manosroi. It consists of over 200,000 recipes for all diseases including cancer. To investigate the anti-proliferative and apoptotic activities on human colon cancer cell line (HT-29) as well as the cancer cell selectivity of the methanolic extracts (MEs) and fractions of the 23 selected plants from the "MANOSROI III" database. MATERIALS AND METHODS: The 23 selected plants were extracted with methanol under reflux and evaluated for their anti-proliferative activity by sulforhodamine B assay. The 5 plants (Gloriosa superba, Caesalpinia sappan, Fibraurea tinctoria, Ventilago denticulata and Psophocarpus tetragonolobus) with potent anti-proliferative activity were fractionated by liquid-liquid partition to give 4 fractions including each hexane (HF), methanol-water (MF), n-butanol (BF) and water (WF) fractions. They were tested for anti-proliferative activity and cancer cell selectivity. The ME and fractions of G. superba which showed potent anti-proliferative activity were further examined for morphological changes and apoptotic activities by acridine orange (AO)/ethidium bromide (EB) staining. RESULTS: The ME of G. superba root showed active with the highest anti-proliferative activity at 9.17 and 1.58 folds of cisplatin and doxorubicin, respectively. After liquid-liquid partition, HF of V. denticulata, MFs of F. tinctoria, V. denticulata and BF of P. tetragonolobus showed higher anti-proliferative activities than their MEs. The MF of G. superba indicated the highest anti-proliferative activity at 7.73 and 1.34 folds of cisplatin and doxorubicin, respectively, but only 0.86 fold of its ME. The ME and HF, MF and BF of G. superba and MF of F. tinctoria demonstrated high cancer cell selectivity. At 50 µg/ml, ME, HF, MF and BF of G. superba demonstrated higher apoptotic activities than the two standard drugs. CONCLUSIONS: This present study has not only confirmed the traditional use of the Thai/Lanna medicinal plant recipes for cancer treatments, but also the potential of the selected plant, G. superba for the further development as a modern anti-cancer drug.


Asunto(s)
Antineoplásicos/farmacología , Magnoliopsida , Extractos Vegetales/farmacología , Plantas Medicinales , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Bases de Datos Factuales , Células HT29 , Humanos , Tailandia
18.
Chem Biodivers ; 10(8): 1448-63, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-23939793

RESUMEN

Nine phenolic compounds, including two phenolic carboxylic acids, 1 and 2, seven hydrolyzable tannins, 3-9, eight triterpenoids, including four oleanane-type triterpene acids, 10-13, and four of their glucosides, 14-17, isolated from a MeOH extract of the gall of Terminalia chebula Retz. (myrobalan tree; Combretaceae), were evaluated for their inhibitory activities against melanogenesis in B16 melanoma cells induced by α-melanocyte-stimulating hormone (α-MSH), against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells, and against TPA-induced inflammation in mice. Their 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activities and cytotoxic activities against four human cancer cell lines were also evaluated. Compounds 6-9 and 12 exhibited potent inhibitory activities against melanogenesis (39.3-66.3% melanin content) with low toxicity to the cells (74.5-105.9% cell viability) at a concentration of 10 µM. Western-blot analysis revealed that isoterchebulin (8) reduced the protein levels of MITF (=microphtalmia-associated transcription factor), tyrosinase, and TRP-1 (=tyrosine-related protein 1), mostly in a concentration-dependent manner. Eight triterpenoids, 10-17, showed potent inhibitory effects on EBV-EA induction with the IC50 values in the range of 269-363 mol ratio/32 pmol TPA, while these compounds exhibited no DPPH scavenging activities (IC50 >100 µM). On the other hand, the nine phenolic compounds, 1-9, exhibited potent radical-scavenging activities (IC50 1.4-10.9 µM) with weak inhibitory effects on EBV-EA induction (IC50 460-518 mol ratio/32 pmol TPA). The tannin 6 and seven triterpenoids, 10-16, have been shown to inhibit TPA-induced inflammation (1 µg/ear) in mice with the ID50 values in the range of 0.06-0.33 µmol/ear. Arjungenin (10) exhibited inhibitory effect on skin-tumor promotion in an in vivo two-stage mouse-skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator and with TPA as promoter. Compounds 1, 2, 4, 5, 7-9, 12, and 13, against HL60 cell line, compounds 1 and 4, against AZ521 cell line, and compounds 1, 11, and 12, against SK-BR-3 cell line, showed moderate cytotoxic activities (IC50 13.9-73.2 µM).


Asunto(s)
Fenoles , Terminalia/química , Triterpenos , Animales , Western Blotting , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Células HL-60 , Humanos , Hiperpigmentación/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Melaninas/antagonistas & inhibidores , Metanol/química , Ratones , Estructura Molecular , Neoplasias/tratamiento farmacológico , Fenoles/química , Fenoles/farmacología , Triterpenos/química , Triterpenos/farmacología
19.
Pharm Biol ; 50(11): 1397-407, 2012 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-22849519

RESUMEN

UNLABELLED: "Longkong"(Lansium domesticum Corr., Family: Meliaceae) is a fruit found in the south of Thailand. This plant has been used in traditional medicines. OBJECTIVES: To investigate the antiproliferative activities and the phytoconstituents of Longkong extracts. MATERIALS AND METHODS: Cytotoxicity and apoptotic activity of 48 extracts were tested using the SRB assay and acridine orange (AO)/ethidium bromide (EB) staining, respectively. The extracts which gave the highest anticancer activity were selected to prepare the semipurified extracts and analysis for the constituents by gas chromatography-mass spectrometry (GC/MS). RESULTS: The highest percentage yield (59.38%) was from the cold water extract of Longkong ripe fruits (RFWC). The highest total phenolic and flavonoid contents were observed in cold and hot methanol extract of Longkong stalks (STMC and STMH). The hot and cold chloroform young Longkong fruit extracts (YFCH and YFCC) exhibited a cytotoxic effect (IC(50) < 1 mg/mL) against cancer cells. For apoptotic induction, YFCH demonstrated the highest activity against KB of 13.84 ± 4.21% at 0.5 mg/mL which was 0.88 and 1.35 times of cisplatin and 5-FU, respectively, while apoptotic cells in HT-29 were 8.68 ± 1.85% at 5 mg/mL, which was 0.61 and 1.43 times of cisplatin and 5-FU, respectively. YFCC showed the highest apoptotic effect against KB cells at 10.70 ± 2.15% at 0.5 mg/mL, which was 0.68 and 1.07 times of cisplatin and 5-FU, respectively. The major phytoconstituents in YFCH were hexadecanoic acid (11.53%) and ethyl oleate (10.58%). DISCUSSION AND CONCLUSION: The crude extracts of Longkong showed anticancer activities and may provide new lead compounds for the development of anticancer products.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Meliaceae/química , Neoplasias/tratamiento farmacológico , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Cisplatino/farmacología , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Fluorouracilo/farmacología , Frutas , Cromatografía de Gases y Espectrometría de Masas , Humanos , Concentración 50 Inhibidora , Ratones , Neoplasias/patología , Fenoles/aislamiento & purificación , Fenoles/farmacología , Extractos Vegetales/administración & dosificación , Tailandia
20.
Pharm Biol ; 49(11): 1190-203, 2011 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-22014267

RESUMEN

CONTEXT: The galls of Terminalia chebula Retz. (Combretaceae) frequently appear in many Thai Lanna medicinal plant recipes for promotion of longevity. OBJECTIVE: The objective of this study was to evaluate the skin anti-aging of gel containing niosomes loaded with a semi-purified fraction containing gallic acid from T. chebula galls. METHOD: The semi-purified fraction containing phenolic compounds including gallic acid isolated from T. chebula galls loaded in non-elastic or elastic niosomes, and its developed gel, were evaluated for rabbit skin irritation by the closed patch test and skin anti-aging in human volunteers by measuring skin elasticity and roughness. RESULTS: Gel containing the fraction unloaded (SS) or loaded in non-elastic (SN) or elastic (SE) niosomes and gallic acid loaded in non-elastic (GN) or elastic (GE) niosomes showed no skin irritation, whereas the unloaded gallic acid (GS) gave the irritation in rabbit's skin by the closed patch test. The % parameter changes of skin elastic recovery and skin elastic extension when applied with SN and SE gels were +28.73 and +32.57; -21.25 and -22.63%, respectively. SN and SE gel also showed a significant decrease of the maximum and average roughness values with the parameter changes of -29.43 and -32.38; -39.47 and -35.28%, respectively. CONCLUSION: The semi-purified fraction loaded in niosomes indicated not only higher chemical stability of gallic acid containing in the fraction, but also more in vivo anti-aging activities than the unloaded fraction when incorporated in gel.


Asunto(s)
Fármacos Dermatológicos/farmacología , Ácido Gálico/farmacología , Extractos Vegetales/farmacología , Envejecimiento de la Piel/efectos de los fármacos , Piel/efectos de los fármacos , Terminalia , Administración Cutánea , Adulto , Animales , Compuestos de Bifenilo/química , Células Cultivadas , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/química , Fármacos Dermatológicos/aislamiento & purificación , Fármacos Dermatológicos/toxicidad , Relación Dosis-Respuesta a Droga , Estabilidad de Medicamentos , Elasticidad , Femenino , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Ácido Gálico/administración & dosificación , Ácido Gálico/química , Ácido Gálico/aislamiento & purificación , Ácido Gálico/toxicidad , Geles , Humanos , Liposomas , Masculino , Metaloproteinasa 2 de la Matriz/metabolismo , Inhibidores de la Metaloproteinasa de la Matriz , Persona de Mediana Edad , Picratos/química , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Tumores de Planta , Plantas Medicinales , Conejos , Piel/metabolismo , Piel/patología , Pruebas de Irritación de la Piel , Pigmentación de la Piel/efectos de los fármacos , Terminalia/química , Tailandia , Factores de Tiempo
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