RESUMEN

BACKGROUND: Semen preservation by cooling is less expensive, simpler and results in less sperm damage than freezing does. However, spermatozoa can only be preserved for a short period due to the excessive formation of reactive oxygen species (ROS). Although several antioxidants can protect sperms from ROS damage during storage at low temperatures, the use of natural antioxidants derived from plants would be a better alternative. OBJECTIVE: To assess the effects of chamuangone, which can reduce oxidation reactions in cells, on cat semen quality after preservation at 4 degree C for 15 days. MATERIALS AND METHODS: Epididymal sperm samples were collected before being diluted with tris-citric-fructose-egg yolk (TCFE) extender containing different concentrations of chamuangone (0, 50, 100, 150 and 200 ug/mL) and preserved at 4 degree C. Semen samples were evaluated before chilling and then every 3 days after chilling for up to 15 days. Each sample was assessed for sperm motility, viability, DNA integrity, plasma membrane integrity and percentage of spermatozoa with intact acrosomes. RESULTS: A significantly higher sperm motility was observed in the group supplemented with 100 ug/mL chamuangone compared to the control after 6 days of storage. However, the chamuangone concentration at 200 ug/mL did not significantly increase the sperm motility when compared to the control for the entire storage period. CONCLUSION: 100 µg/mL chamuangone can improve sperm characteristics during 15 days of preservation at 4 degree C, keeping sperm alive (49.3 ± 5.2%) and moving (7.1 ± 2.4%). These results can be used for the development of breeding programs using technologically advanced reproductive procedures in domestic and wild cats. https://doi.org/10.54680/fr24110110212.

Asunto(s)

Análisis de Semen , Preservación de Semen , Análisis de Semen/veterinaria , Especies Reactivas de Oxígeno , Motilidad Espermática , Criopreservación/veterinaria , Criopreservación/métodos , Semillas , Espermatozoides , Preservación de Semen/veterinaria , Preservación de Semen/métodos , Suplementos Dietéticos , Extractos Vegetales/farmacología

RESUMEN

Artocarpin-rich extract (ARE) was prepared using a green technology and standardized to contain 49·6% w/w artocarpin, while lawsone methyl ether was prepared using a green semi-synthesis. ARE, LME and ampicillin exhibited weak anti-MRSA activity with the MICs of 31·2-62·5 µg/ml. Based on the checkerboard assay, the synergistic interaction between ARE (0·03 µg/ml) and LME (0·49 µg/ml) against four MRSA isolates were observed with the fractional inhibitory concentration index (FICI) value of 0·008, while those of ARE (1·95-7·81 µg/ml) and ampicillin (0·49 µg/ml) as well as LME (0·49-1·95 µg/ml) and ampicillin (0·49 µg/ml) were 0·016-0·257. The time kill confirmed the synergistic interactions against MRSA with different degrees. The combination of ARE and LME as well as its combinations with ampicillin altered the membrane permeability of MRSA, which led to release of the intracellular materials. In addition, each compound inhibited the biofilm formation of standard MRSA (DMST 20654) and the clinical isolate (MRSA 1096). These findings suggested that cocktails containing ARE and LME might be used to overcome problems associated with MRSA. Additionally, the results implied that combination of either ARE or LME with available conventional antibiotic agents might be effective in countering these perilous pathogens.

Asunto(s)

Staphylococcus aureus Resistente a Meticilina , Ampicilina/farmacología , Antibacterianos/farmacología , Biopelículas , Sinergismo Farmacológico , Lectinas de Unión a Manosa , Pruebas de Sensibilidad Microbiana , Naftoquinonas , Extractos Vegetales/farmacología , Lectinas de Plantas

RESUMEN

α-Mangostin-rich extract (AME) exhibited satisfactory inhibitory activities against all tested MRSA strains, with minimum inhibitory concentrations (MICs) of 7·8-31·25 µg ml-1 , whereas lawsone methyl ether (LME) and ampicillin revealed weak antibacterial activity with MICs of 62·5-125 µg ml-1 . However, the combination of AME and LME showed synergistic effects against all tested MRSA strains with fractional inhibitory concentration index (FICI) values of 0·008-0·009, while the combination of AME and ampicillin, as well as LME and ampicillin produced synergistic effects with FICIs of 0·016-0·257. A time-kill assay against MRSA (DMST 20654 strain) revealed a 6-log reduction in CFU per ml, which completely inhibited bacterial growth for the combinations of AME and LME, AME and ampicillin, and LME and ampicillin at a 8-h incubation, while those against MRSA (2468 strain) were at 10-h incubation. The combination of α-mangostin and LME as well as the combinations of each compound with ampicillin synergized the alteration of membrane permeability. In addition, α-mangostin, LME and ampicillin inhibited the biofilm formation of MRSA. These findings indicated that the combinations of AME and LME or each of them in combination with ampicillin had enhanced antibacterial activity against MRSA. Therefore, these compounds might be used as the antibacterial cocktails for treatment of MRSA.

Asunto(s)

Ampicilina/farmacología , Antibacterianos/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Naftoquinonas/farmacología , Xantonas/farmacología , Sinergismo Farmacológico , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología , Infecciones Estafilocócicas/tratamiento farmacológico

RESUMEN

OBJECTIVE: To investigate the in vitro effects of ellagic acid on HIV-1 replication. METHODS: Anti-HIV-1 activity of ellagic acid was determined in vitro using X4-tropic HIV-1NPO3 and R5-tropic pBaL Env-recombinant virus. Anti-HIV-1NPO3 activity of ellagic acid was investigated at a multiplicity of infection (MOI) of 0.01. Anti-HIV-1 integrase and protease activities of ellagic acid were tested using in vitro integration and proteolytic cleavage assays. RESULTS: Ellagic acid, added either before or after HIV-1NPO3 exposure, suppressed replication of the virus in C8166 cells up to 34%. Ellagic acid showed an anti-integrase IC50 of 8.7 µM. No cytotoxicity of ellagic acid at concentrations ranging from 12.5 to 100 µM was observed. CONCLUSION: We conclude that ellagic acid can inhibit HIV-1 infection without cytotoxicity. Thus, it may be a new effective agent that has potential to be developed as a novel microbicide against HIV-1.

Asunto(s)

Ácido Elágico/farmacología , Infecciones por VIH/prevención & control , VIH-1/efectos de los fármacos , Replicación Viral/efectos de los fármacos , Linfocitos T CD4-Positivos/fisiología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Integrasa de VIH/efectos de los fármacos , Proteasa del VIH/efectos de los fármacos , VIH-1/enzimología , Humanos

RESUMEN

Context Ixora megalophylla Chamch. (Rubiaceae) is a new plant species recently found in southern Thailand. Ethyl acetate extracts of its leaves and stems showed antimicrobial activities. Objectives To isolate and identify the antimicrobial compounds from I. megalophylla leaves and stems. Materials and methods The dried leaves (1.7 kg) and stems (3.5 kg) were consecutively extracted with petroleum ether (5 L × 4), ethyl acetate (5 L × 3) and ethanol (5 L × 4) under reflux conditions. The ethyl acetate extract was subjected to an antimicrobial assay guided isolation with Candida albicans and Streptococcus mutans. Compounds 1-10 were identified by (1)H NMR, (13)C NMR and EI-MS. Minimal lethal concentration (MLC) against C. albicans and Streptococcus spp. was determined using a broth microdilution method for 48 and 24 h, respectively. Results and discussion On the basis of the antimicrobial assay guided isolation, 10 known compounds, including vanillic acid (1), syringic acid (2), 4-hydroxy benzaldehyde (3), scopoletin (4), loliolide (5), syringaldehyde (6), sinapaldehyde (7), coniferaldehyde (8), syringaresinol (9) and 2,2'-dithiodipyridine (10), were identified. Compounds 1-5 were purified from the ethyl acetate extract of the leaves, while 6-9 and 10 were from the ethyl acetate and ethanol extracts of the stems, respectively. Among these isolates, 10 showed the strongest antibacterial activities against S. mutans and Streptococcus mitis, with minimum inhibitory concentrations (MICs) of 2-4 µg/mL, and MLC of 4 µg/mL, as well as having a weak antifungal activity against C. albicans (MIC of 125 µg/mL). This is the first report of the antimicrobial activities of 10.

Asunto(s)

Antibacterianos/farmacología , Antifúngicos/farmacología , Bioensayo , Fraccionamiento Químico/métodos , Boca/microbiología , Extractos Vegetales/farmacología , Rubiaceae , Streptococcus mitis/efectos de los fármacos , Streptococcus mutans/efectos de los fármacos , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Candida albicans/efectos de los fármacos , Candida albicans/crecimiento & desarrollo , Espectroscopía de Resonancia Magnética con Carbono-13 , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta , Tallos de la Planta , Plantas Medicinales , Espectroscopía de Protones por Resonancia Magnética , Rubiaceae/química , Solventes/química , Streptococcus mitis/crecimiento & desarrollo , Streptococcus mutans/crecimiento & desarrollo

RESUMEN

CONTEXT: Medicinal plants involved in traditional Thai longevity formulations are potential sources of antimicrobial compounds. OBJECTIVE: To evaluate the antimicrobial activities of some extracts from medicinal plants used in traditional Thai longevity formulations against some oral pathogens, including Streptococcus pyogenes, Streptococcus mitis, Streptococcus mutans, and Candida albicans. An extract that possessed the strongest antimicrobial activity was fractionated to isolate and identify the active compounds. MATERIALS AND METHODS: Methanol and ethyl acetate extracts of 25 medicinal plants used as Thai longevity formulations were evaluated for their antimicrobial activity using disc diffusion (5 mg/disc) and broth microdilution (1.2-2500 µg/mL) methods. The ethyl acetate extract of Ficus foveolata Wall. (Moraceae) stems that exhibited the strongest antibacterial activity was fractionated to isolate the active compounds by an antibacterial assay-guided isolation process. RESULTS AND DISCUSSION: The ethyl acetate extract of F. foveolata showed the strongest antibacterial activity with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 19.5-39.0 and 39.0-156.2 µg/mL, respectively. On the basis of an antibacterial assay-guided isolation, seven antibacterial compounds, including 2,6-dimethoxy-1,4-benzoquinone (1), syringaldehyde (2), sinapaldehyde (3), coniferaldehyde (4), 3ß-hydroxystigmast-5-en-7-one (5), umbelliferone (6), and scopoletin (7), were purified. Among these isolated compounds, 2,6-dimethoxy-1,4-benzoquinone (1) exhibited the strongest antibacterial activities against S. pyogenes, S. mitis, and S. mutans with MIC values of 7.8, 7.8, and 15.6 µg/mL, and MBC values of 7.8, 7.8, and 31.2 µg/mL, respectively. In addition, this is the first report of these antibacterial compounds in the stems of F. foveolata.

Asunto(s)

Antibacterianos/farmacología , Antifúngicos/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Ficus/química , Medicina Tradicional de Asia Oriental , Pruebas de Sensibilidad Microbiana , Tailandia

RESUMEN

CONTEXT: Integrase (IN) is one of the three human immunodeficiency virus type 1 (HIV-1) enzymes that, together with a reverse transcriptase and protease, allow the virus to reproduce itself after infecting the host cells. Any new knowledge on inhibitors of this enzyme could provide essential clues for the development of anti-HIV drugs. OBJECTIVE: To evaluate the anti-HIV-1 IN activity of some Thai medicinal plant extracts, and to isolate the active compounds from the extract that possessed the strongest anti-HIV-1 IN activity. MATERIALS AND METHODS: Ethanol extracts of eight Thai medicinal plants (10-100 µg/mL) were evaluated for their inhibitory effect against HIV-1 IN. An extract of Mimusops elengi L. (Sapotaceae) leaves that possessed the strongest anti-HIV-1 IN activity was fractionated to isolate the active compounds by an anti-HIV-1 IN assay-guided isolation process. RESULTS AND DISCUSSION: The leaf extract from M. elengi had the strongest anti-HIV-1 IN activity with an IC50 value of 62.1 µg/mL. A bioassay-guided isolation of the active compounds from M. elengi leaf extract resulted in the isolation of active compounds, identified as a mixture of gallocatechin and epigallocatechin. This mixture of gallocatechin and epigallocatechin showed satisfactory anti-HIV-1 IN activity with an IC50 value of 35.0 µM. A flavanol glycoside, mearnsitrin was also isolated but was inactive at a concentration of 100 µM.

Asunto(s)

Inhibidores de Integrasa VIH/farmacología , Integrasa de VIH/efectos de los fármacos , Mimusops/química , Extractos Vegetales/farmacología , Bioensayo , Catequina/análogos & derivados , Catequina/aislamiento & purificación , Catequina/farmacología , Relación Dosis-Respuesta a Droga , Integrasa de VIH/metabolismo , Inhibidores de Integrasa VIH/administración & dosificación , Concentración 50 Inhibidora , Oxazinas/aislamiento & purificación , Oxazinas/farmacología , Extractos Vegetales/administración & dosificación , Plantas Medicinales/química , Tailandia

RESUMEN

CONTEXT: Plumbagin is a major active constituent of Plumbago indica L. (Plumbaginaceae). It possesses various pharmacological activities that have been shown to assist in the treatment of various diseases. OBJECTIVES: This work is focused on increasing the production of plumbagin in P. indica root cultures using low doses of gamma ray irradiation as an elicitor. MATERIALS AND METHODS: The effect of low doses of gamma ray irradiation (0, 5, 10, 15, 20, 25 Gy) and ages of the root cultures (0, 5, 10, 15, 20 days) for elicitation of plumbagin production was determined. The stability of the elicited root cultures to produce plumbagin was also determined during three cycles of subculture. RESULTS AND DISCUSSION: Treatment of the root cultures with a low dose of gamma ray at 20 Gy gave the highest level of plumbagin production (1.04 mg/g DW) when compared to all other treated groups. The appropriate age of the root cultures for maximum production of plumbagin was found to be 10 days. However, treatment of 5-day-old root cultures resulted in a significant increase of dried root biomass that also had a high plumbagin production. Based on the total biomass per culture flask, the amounts of plumbagin produced by the 5- and 10-day-old treated roots were 0.59 and 0.37 mg/250 mL flask, respectively, which were 4.2- and 2.6-fold higher than the level in the control. Subculturing the root cultures until the third generation still showed an increase in plumbagin production without any effects on their growth.

Asunto(s)

Rayos gamma , Naftoquinonas/química , Plumbaginaceae/química , Relación Dosis-Respuesta a Droga , Relación Dosis-Respuesta en la Radiación , Naftoquinonas/aislamiento & purificación , Naftoquinonas/efectos de la radiación , Raíces de Plantas , Factores de Tiempo

RESUMEN

On the basis of a leishmanicidal assay-guided isolation, two new monoterpene coumarins, minutin A and minutin B, were purified from Micromelum minutum leaves together with four known coumarins, 8,4″-dihydroxy-3″,4″-dihydrocapnolactone-2',3'-diol, 8-hydroxyisocapnolactone-2',3'-diol, 8-hydroxy-3″,4″-dihydrocapnolactone-2',3'-diol, and clauslactone E. Among these compounds, minutin A, minutin B, 8-hydroxyisocapnolactone-2',3'-diol and clauslactone E showed a significant cytotoxic activity against Leishmania major with IC50 values of 26.2, 20.2, 12.1, and 9.8 µM, respectively, while 8,4″-dihydroxy-3″4″-dihydrocapnolactone-2',3'-diol and 8-hydroxy-3″,4″-dihydrocapnolactone-2',3'-diol were not active. However, all these compounds exhibited some inhibitory activity against one or more lung adenocarcinoma (SBC3 and A549) and leukaemia (K562, and K562/ADM) cell lines. Amongst these, clauslactone E, minutin B and 8-hydroxyisocapnolactone-2',3'-diol possessed the strongest cytotoxic activity against SBC3, A549, K562, and K562/ADM cell lines, with IC50 values of 3.7, 10.4, 12.1, and 10.8 µM for clauslactone E; 9.6, 17.5, 8.7 and 6.7 µM for minutin B; 8.8, 10.1, 16.9, and 10.1 µM for 8-hydroxyisocapnolactone-2',3'-diol, respectively.

Asunto(s)

Antineoplásicos Fitogénicos/farmacología , Antiprotozoarios/farmacología , Cumarinas/farmacología , Citotoxinas/farmacología , Hojas de la Planta/química , Rutaceae/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antiprotozoarios/química , Antiprotozoarios/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Cumarinas/química , Cumarinas/aislamiento & purificación , Citotoxinas/química , Citotoxinas/aislamiento & purificación , Humanos , Leishmania major/efectos de los fármacos , Estructura Molecular , Neoplasias/fisiopatología

RESUMEN

CONTEXT: Lawsone, lawsone methyl ether and 3,3'-methylelnebislawsone are the main active compounds of Impatiens balsamina L. (Balsaminaceae). These compounds possess various pharmacological activities that have been shown to assist with the treatment of skin diseases. OBJECTIVE: This work focused on increased naphthoquinone production in I. basamina root cultures using methionine feeding. MATERIALS AND METHODS: I. balsamina root cultures were maintained in liquid Gamborg's B5 medium supplemented with 0.1 mg/L α-naphthalene acetic acid, 0.1 mg/L kinetin, 1.0 mg/L 6-benzyladenine and 20 g/L sucrose. The effect of methionine concentration (50, 100, 300, 500 and 1000 mg/L) on naphthoquinone production of I. basamina root cultures was determined. Isolation of secondary metabolites from I. balsamina root cultures was also carried out. RESULTS AND DISCUSSION: Feeding of 300 mg/L methionine to the root cultures at the beginning of the growth cycle increased the production of 3,3'-methylelnebislawsone almost two-fold (0.63 mg/g dry weight, compared to the control group 0.32 mg/g dry weight). Optimization of the feeding conditions showed that adding 500 mg/L methionine to a 21-day old root cultures increased production of lawsone methyl ether and 3,3'-methylenebislawsone up to 2.6- and 3.1-fold higher, respectively, compared to the controls. In addition, various pharmacologically interesting secondary metabolites were isolated from I. balsamina root cultures, such as a flavonoid, luteolin, a naphthoquinone, 2,3-dihydroxy-1,4-naphthoquinone, and a triterpenoid, echinocystic acid. This is the first report of the occurrence of these compounds in this plant.

Asunto(s)

Impatiens/metabolismo , Metionina/farmacología , Naftoquinonas/aislamiento & purificación , Técnicas de Cultivo , Relación Dosis-Respuesta a Droga , Flavonoides/aislamiento & purificación , Impatiens/crecimiento & desarrollo , Metionina/administración & dosificación , Raíces de Plantas , Triterpenos/aislamiento & purificación

RESUMEN

CONTEXT: Pentacyclic triterpenes, mainly, asiatic acid, madecassic acid, asiaticoside, and madecassoside are the active constituents of Centella asitica (L.) Urban. (Apiaceae). These compounds possess various pharmacological activities that have been shown to assist with wound healing and brain enrichment. OBJECTIVE: Determination of these active pentacyclic triterpenes in extracts from the various parts of C. asiatica plants harvested at different times of the year and grown in different environments. MATERIALS AND METHODS: The separate plant parts selected were leaves, stolons, petioles, flowers, fruits, and nodes with roots. Dried powder from each part was extracted with ethanol by microwave-assisted extraction and subjected to determination of their content of the four pentacyclic triterpenes using a HPLC method. The effects of the places of cultivation as well as harvesting periods on the content of the four pentacyclic triterpenes in the extracts were also determined. RESULTS AND DISCUSSION: Among the various parts of C. asiatica, the leaves contained the highest amount of pentacyclic triterpenes with a total content of pentacyclic triterpenes of 19.5 mg/g dry powder. However, the contents of the pentacyclic triterpenes in C. asiatica varied according to the place of cultivation and the harvesting period. C. asiatica collected from Trang, Thailand gave the highest content of total pentacyclic triterpenes (37.2 mg/g dry powder) when harvested in March, while those collected from Songkhla, Thailand gave the highest value (37.4 mg/g dry powder) when collected in December. C. asiatica collected from Nakornsrithammarat and Ratchaburi, Thailand gave the lowest content of total pentacyclic triterpenes in all experimental harvesting periods.

Asunto(s)

Centella/química , Triterpenos Pentacíclicos/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Agricultura , Cromatografía Líquida de Alta Presión , Etanol/química , Flores/química , Frutas/química , Microondas , Hojas de la Planta/química , Raíces de Plantas/química , Plantas Medicinales , Polvos , Estaciones del Año , Solventes/química , Tailandia , Triterpenos/aislamiento & purificación

RESUMEN

Rhinacanthus nasutus (L.) Kurz (Acanthaceae) has long been used in Thai traditional medicine for treatment of tinea versicolor, ringworm, pruritic rash, and abscess. The active constituents are known as a group of naphthoquinone esters, rhinacanthins. This work focused on establishment of R. nasutus root cultures and determination of rhinacanthin production. Induction of R. nasutus root formation was accomplished on solid Gamborg's B5 (B5) medium, supplied with 0.1 mg/L indole-3-butyric acid (IBA) and 20 g/L sucrose. The effects of explants (whole leaf explants and four-side excised leaf explants), light and medium composition on root and rhinacanthin formation were investigated. The root formation from the whole leaf explants was 10 times higher than that from the four-side excised leaf explants. In addition, light possessed an inhibitory effect on the root and rhinacanthin formation of R. nasutus. Medium manipulation found that Murashige and Skoog (MS) medium supplied with 3 mg/L IBA and 30 g/L sucrose was the most suitable for induction of the root formation. Unfortunately, the obtained root cultures produced only rhinacanthin-C in very low amount, 0.026 mg/g dry weight (DW), when they were transferred into the same MS liquid medium. With semisolid medium (4 g/L agar) of the same MS composition, however, the root cultures appeared to produce higher content of rhinacanthin-C, -D and -N (3.45, 0.07 and 0.07 mg/g DW, respectively). Our finding suggests that culturing in semisolid medium is capable of improving of rhinacanthin production in R. nasutus root cultures.

Asunto(s)

Acanthaceae/efectos de los fármacos , Acanthaceae/efectos de la radiación , Medios de Cultivo , Luz , Naftoquinonas/metabolismo , Raíces de Plantas/efectos de los fármacos , Raíces de Plantas/efectos de la radiación , Acanthaceae/crecimiento & desarrollo , Acanthaceae/metabolismo , Técnicas de Cultivo , Naftoquinonas/aislamiento & purificación , Raíces de Plantas/crecimiento & desarrollo , Raíces de Plantas/metabolismo

RESUMEN

Ethyl acetate and methanol extracts of 18 Thai medicinal plants were investigated for their antibacterial activity against Propionibacterium acnes, Stapylococcus aureus, and S. epidermidis. Thirteen plant extracts were capable of inhibiting the growth of P. acnes and S. epidermidis, while 14 plant extracts exhibited an inhibitory effect on S. aureus. Based on the broth dilution method, the ethyl acetate extract of Alpinia galanga (L.) Wild. (Zingiberaceae) rhizome showed the strongest antibacterial effect against P. acnes, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 156.0 and 312.0 microg/mL, respectively. On the basis of bioassay-guided purification, the ethyl acetate extract was isolated to afford the antibacterial active compound, which was identified as 1'-acetoxychavicol acetate (1'-ACA). 1'-ACA had a strong inhibitory effect on P. acnes with MIC and MBC values of 62.0 and 250.0 microg/mL, respectively. Thus, 1'-ACA was used as an indicative marker for standardization of A. galanga extract using high performance liquid chromatography. These results suggest that A. galanga extract could be an interesting agent for further studies on an alternative treatment of acne.

Asunto(s)

Acné Vulgar/microbiología , Alpinia/química , Antibacterianos/farmacología , Extractos Vegetales/farmacología , Propionibacterium acnes/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos , Acné Vulgar/tratamiento farmacológico , Antibacterianos/aislamiento & purificación , Antibacterianos/uso terapéutico , Cromatografía Líquida de Alta Presión , Relación Dosis-Respuesta a Droga , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/uso terapéutico , Propionibacterium acnes/crecimiento & desarrollo , Propionibacterium acnes/aislamiento & purificación , Rizoma/química , Staphylococcus aureus/crecimiento & desarrollo , Staphylococcus aureus/aislamiento & purificación , Staphylococcus epidermidis/crecimiento & desarrollo , Staphylococcus epidermidis/aislamiento & purificación , Tailandia

RESUMEN

Rhinacanthins-rich Rhinacanthus nasutus (RRn) extract was prepared and standardized to contain total rhinacantins not less than 70% w/w. In this study, antimicrobial activities of the RRn extract as well as rhinacanthin-C against Streptococcus mutans, Propionibacterium acnes, Helicobacter pylori, Staphylococcus aureus, S. epidermidis and Candida albicans were evaluated by microdilution assay. It was found that the RRn extract exhibited potent bactericidal activity against S. mutans with MIC and MBC of 4 microg/ml, and potent bacteriostatic activity against S. epidermidis, P. acnes and S. aureus with the MICs of 8-16 microg/ml. However, the RRn extract was not active against C. albicans at concentration up to 2000 microg/ml. The antimicrobial activities of the RRn extract was almost equal to those of rhinacanthin-C. Stability evaluations of the RRn extract through a period of 4 months found that the RRn extracts were stable when kept in a well-closed container protected from light and stored either under 4+/-2 degrees C or 30+/-2 degrees C. The RRn extracts that were exposed to light were not stable after 1 week of storage. Under accelerated conditions at 45 degrees C with 75% relative humidity, the RRn extracts were not stable after 8 weeks of storage. Study on the effect of pH on the stability of the aqueous methanolic solution of the RRn extract found that the solutions were not stable at pH 5.5, pH 7.0, and pH 8.0. However, the rhinacanthin solution at pH 5.5 was more stable than those at pH 7.0 and pH 8.0.

Asunto(s)

Acanthaceae/química , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Naftoquinonas/farmacología , Extractos Vegetales/farmacología , Estabilidad de Medicamentos , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química

RESUMEN

A reversed-phase high-performance liquid chromatographic method is described for the simultaneous determination of rhinacanthin-C, rhinacanthin-D, and rhinacanthin-N in Rhinacanthus nasutus leaves. The method involved the use of a TSK-gel ODS-80Ts column (5 microm, 4.6 x 150 mm i.d.) with the mixture of methanol and 5% aqueous acetic acid (80:20, v/v) as the mobile phase. The parameters of linearity, repeatability, accuracy, and specificity of the method were evaluated. The recovery of the method was 94.3-100.9%, and good linearity (r(2) > or = 0.9999) was obtained for all rhinacanthins. A high degree of specificity as well as repeatability and reproducibility (relative standard deviation values less than 5%) were also achieved. The limit of detection and quantification of all rhinacanthins were 0.75 and 3.0 microg/mL, respectively. The solvents for extraction of rhinacanthins from R. nasutus leaves were examined in order to obtain the leaf extract with high rhinacanthin content. It was found that ethyl acetate was an appropriate solvent for rhinacanthin extraction. Fractionation of the ethyl acetate extract using a basic anion exchange resin (Amberlite IRA-67) eluted with 10% acetic acid in methanol afforded a rhinacanthin-rich extract (HRn). The total content of rhinacanthins was increased from 37.4% w/w to 77.5% w/w. The antifungal activities of HRn against Trichophyton rubrum, T. mentagrophytes, and Microsporum gypseum were also improved.

Asunto(s)

Acanthaceae/química , Cromatografía Líquida de Alta Presión/métodos , Naftoquinonas/química , Naftoquinonas/aislamiento & purificación , Extractos Vegetales/sangre , Extractos Vegetales/aislamiento & purificación , Estructura Molecular , Reproducibilidad de los Resultados

RESUMEN

The antiulcer effect of bisdemethoxycurcumin, a yellow pigment found mainly in rhizomes of Curcuma longa, was compared with curcumin in gastric ulcer model systems to validate its clinical application as a remedy for peptic ulcer. Western blot analysis of mouse macrophage cell line RAW 264.7 activated with lipopolysaccharide showed that bisdemethoxycurcumin inhibited inducible nitric oxide synthase (iNOS) production significantly but had no effect on tumor necrosis factor-alpha (TNF-alpha) production, whereas curcumin showed stronger suppression of iNOS protein production and inhibited TNF-alpha protein production significantly. However, bisdemethoxycurcumin and curcumin possessed similar potency in scavenging nitric oxide generated from mouse macrophage cell line RAW 264.7. Reverse-transcriptase polymerase chain reaction (RT-PCR) analysis showed that both curcuminoids inhibited the induction of iNOS dose-dependently at the transcriptional level and curcumin also appeared to inhibit the induction of TNF-alpha at post-transcriptional level. In an animal model, intraduodenal administration of bisdemethoxycurcumin (5-80 mg/kg body wt.) showed a strong inhibitory effect on gastric acid secretion in pylorus-ligated rats whereas curcumin (5-20 mg/kg body wt.) showed a less inhibitory effect, with maximum potency at a dose of 20mg/kg body wt. Moreover, oral administration of bisdemethoxycurcumin at doses of 20-80 mg/kg body wt. twice daily for 10 days showed a significant curative efficacy in accelerating the healing of acetic acid-induced chronic gastric ulcer and promotion of mucosal regeneration in the ulcerated portion in a dose-related manner with potency equal to curcumin. In contrast, the curative potency of curcumin tended to decrease at doses over 160 mg/kg body wt./day. Western blot analysis in ulcerated gastric mucosa showed that bisdemethoxycurcumin dose-dependently reduced the increased protein expression level of iNOS but not TNF-alpha. These results indicated that bisdemethoxycurcumin directly accelerates gastric ulcer healing with potency equal to curcumin. Its antiulcer effect might be due to its properties of decreasing gastric acid secretion and enhancing the mucosal defensive mechanism through suppression of iNOS-mediated inflammation.

Asunto(s)

Antiulcerosos/uso terapéutico , Curcuma , Curcumina/análogos & derivados , Curcumina/uso terapéutico , Ácido Gástrico/metabolismo , Preparaciones de Plantas/uso terapéutico , Úlcera Gástrica/tratamiento farmacológico , Animales , Antiulcerosos/farmacología , Línea Celular , Curcumina/farmacología , Diarilheptanoides , Modelos Animales de Enfermedad , Mucosa Gástrica/efectos de los fármacos , Lipopolisacáridos , Macrófagos/efectos de los fármacos , Masculino , Ratones , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Fitoterapia , Preparaciones de Plantas/farmacología , ARN Mensajero/metabolismo , Ratas , Ratas Wistar , Rizoma , Úlcera Gástrica/inducido químicamente , Factor de Necrosis Tumoral alfa/metabolismo

RESUMEN

Se desarrolló un método de cromatografía líquida de alto rendimiento cuantitativa y de separaciónutilizando una columna RP-18 eluida isocráticamente con metanol y agua (73:27, v/v) para analizar loscompuestos activos isoméricos indigotina e indirubina presentes en el extracto de cloroformo del índigonatural. Se utilizaron soluciones estandarizadas de indigotina e indirubina para evaluar la linealidad, laprecisión (replicabilidad), la exactitud y la especificidad del método. Los resultados mostraron unalinealidad (r2 > 0,999) de entre 1,8 y 16,2 mg/ml para la indigotina y entre 1,6 y 14,4 ìg/ml para laindirubina. También se obtuvo un alto grado de especificidad, robustez, replicabilidad (desviaciónestándar relativa inferior al 5% para estándares y extractos) y exactitud (% de recuperaciones superioral 95%)

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A high-performance liquid chromatographic separation and quantitative method using a RP-18 columneluted isocratically with methanol and water (73:27, v/v) was developed to analyze the isomeric activecompounds, indigotin and indirubin, present in the chloroform extract of indigo naturalis. Standardizedsolutions of indigotin and indirubin were used to evaluate linearity, precision (repeatability), accuracyand specificity of the method were evaluated. The results exhibited a linearity (r2 > 0.999) of between1.8 - 16.2 ìg/ml and 1.6 - 14.4 mg/ml for indigotin and indirubin, respectively. A high degree ofspecificity and robustness, as well as repeatability (relative standard deviation less than 5% for bothstandards and the extracts) and accuracy (% recoveries greater than 95%) were also achieved

Asunto(s)

Cromatografía Líquida de Alta Presión/métodos , Cloroformo/análisis , Cloroformo/química , Carmin de Índigo/análisis , Carmin de Índigo/química , Reproducibilidad de los Resultados , Isomerismo , Calidad de los Medicamentos Homeopáticos

RESUMEN

A new biscoumarin, 4,4'-biisofraxidin has been isolated from the root cultures of Impatiens balsamina (Balsaminaceae). The structure was elucidated by 1D and 2D NMR techniques.