Asunto(s)
Colectomía/métodos , Arteria Mesentérica Inferior/diagnóstico por imagen , Imagen Óptica/métodos , Neoplasias del Recto/cirugía , Procedimientos Quirúrgicos Robotizados/métodos , Humanos , Rayos Infrarrojos , Arteria Mesentérica Inferior/fisiología , Cavidad Peritoneal/irrigación sanguínea , Cavidad Peritoneal/diagnóstico por imagen , Flujo Sanguíneo RegionalRESUMEN
BACKGROUND: This study aims to evaluate the effectiveness of adenosine triphosphate-based chemotherapy response assay (ATP-CRA)-guided neoadjuvant chemotherapy for increasing resectability in patients with unresectable colorectal liver metastasis. PATIENTS AND METHODS: Patients were randomised into two groups: Group A was treated by conventional chemotherapy regimen and Group B was treated by chemotherapy regimen according to the ATP-CRA. Three chemotherapeutic agents (5-fluorouracil, oxaliplatin and irinotecan) were tested by ATP-CRA and more sensitive agents were selected. Either FOLFOX or FOLFIRI was administered. Between Group A and B, treatment response and resectability were compared. RESULTS: Between November 2008 and October 2010, a total 63 patients were randomised to Group A (N=32) or Group B (N=31). FOLFOX was more preferred in Group A than in Group B (26 out of 32 (81.3%) vs 20 out of 31 (64.5%)). Group B showed better treatment response than Group A (48.4% vs 21.9%, P=0.027). The resectability of hepatic lesion was higher in Group B (35.5% vs 12.5%, P=0.032). Mean duration from chemotherapy onset to the time of liver resection was 11 cycles (range 4-12) in Group A and 8 cycles (range 8-16) in Group B. CONCLUSION: This study showed that tailored-chemotherapy based on ATP-CRA could improve the treatment response and resectability in initially unresectable colorectal liver metastasis.
Asunto(s)
Adenosina Trifosfato/uso terapéutico , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapéutico , Neoplasias Colorrectales/patología , Neoplasias Hepáticas/tratamiento farmacológico , Adulto , Anciano , Neoplasias Colorrectales/tratamiento farmacológico , Terapia Combinada , Estudios de Factibilidad , Femenino , Humanos , Neoplasias Hepáticas/secundario , Neoplasias Hepáticas/cirugía , Masculino , Persona de Mediana Edad , Resultado del TratamientoRESUMEN
BACKGROUND: The aim of this study was to identify the benefits of robotic transanal specimen extraction (RTSE) compared with minilaparotomy specimen extraction (MSE). METHODS: Patients who underwent totally robotic surgery with curative intent for treatment of adenocarcinoma of the rectum below 12 cm from the anal verge were selected from the authors' database. Patients were divided into RTSE and MSE groups according to the method of specimen delivery. Clinicopathological features and perioperative surgical outcomes were compared between the two groups. RESULTS: There were 53 patients in the RTSE group and 66 in the MSE group. No differences were observed in overall complications. Postoperative recovery was faster in the RTSE group in terms of resumption of a soft diet (mean(s.d.) 3·5(1·5) versus 4·6(1·7) days; P < 0·001) and length of hospital stay (9·0(4·8) versus 11·3(5·3) days; P = 0·016). Pain scores on a visual analogue scale were significantly lower in the RTSE group than in the MSE group from day 2 to day 5 after surgery (P = 0·021 to P < 0·001). CONCLUSION: RTSE in robotic rectal cancer surgery was associated with less pain and a faster recovery than MSE.
Asunto(s)
Canal Anal , Procedimientos Quirúrgicos del Sistema Digestivo/instrumentación , Neoplasias del Recto/cirugía , Robótica , Manejo de Especímenes/métodos , Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Complicaciones Posoperatorias/etiología , Resultado del TratamientoRESUMEN
AIMS: To characterize antifungal principles from the methanol extract of Magnolia obovata and to evaluate their antifungal activities against various plant pathogenic fungi. METHODS AND RESULTS: Four neolignans were isolated from stem bark of M. obovata as antifungal principles and identified as magnolol, honokiol, 4-methoxyhonokiol and obovatol. In mycelial growth inhibition assay, both magnolol and honokiol displayed more potent antifungal activity than 4-methoxyhonokiol and obovatol. Both magnolol and honokiol showed similar in vivo antifungal spectrum against seven plant diseases tested; both compounds effectively suppressed the development of rice blast, tomato late blight, wheat leaf rust and red pepper anthracnose. 4-Methoxyhonokiol and obovatol were highly active to only rice blast and wheat leaf rust respectively. CONCLUSIONS: The extract of M. obovata and four neolignans had potent in vivo antifungal activities against plant pathogenic fungi. SIGNIFICANCE AND IMPACT OF THE STUDY: Neolignans from Magnolia spp. can be used and suggested as a novel antifungal lead compound for the development of new fungicide and directly as a natural fungicide for the control of plant diseases such as rice blast and wheat leaf rust.
Asunto(s)
Antifúngicos/farmacología , Hongos/efectos de los fármacos , Lignanos/farmacología , Magnolia/química , Extractos Vegetales/farmacología , Compuestos Alílicos , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Compuestos de Bifenilo , Cromatografía en Capa Delgada , Lignanos/química , Lignanos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Micelio/efectos de los fármacos , Éteres Fenílicos , Corteza de la Planta/química , Enfermedades de las Plantas , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificaciónRESUMEN
AIM: The aim of this study is to evaluate the accuracy of preoperative magnetic resonance imaging (MRI) in the prediction of circumferential resection margin (CRM) and to determine whether each different MRI scan plane provides an accurate CRM assessment. METHOD: Fifty-seven consecutive patients with mid-rectal cancer were enrolled prospectively. The CRM measurement from each MRI plane according to tumor location was compared with CRM measurement on whole-mount sections with the definition of threatened CRM as 2 mm in distance. The difference in performance among the sagittal, axial and oblique MR images was analyzed by using receiver operating characteristic (ROC) curves (A(z)). RESULTS: For anterior tumors (n = 17), the A(z) of the sagittal, axial and oblique MR planes were 0.66, 0.83 and 0.79, respectively. For lateral tumors (n = 17), the A(z) of the sagittal, axial and oblique MR planes were 0.53, 0.66 and 0.78, respectively. For posterior tumors (n = 23), the A(z) of the sagittal, axial and oblique MR planes were 0.76, 0.82 and 0.97, respectively. CONCLUSIONS: MRI provides an accurate prediction of preoperative CRM. There exist differences in diagnostic accuracy according to each different scan plane of MRI and tumor location within the rectum.
Asunto(s)
Imagen por Resonancia Magnética/métodos , Neoplasias del Recto/patología , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Masculino , Persona de Mediana Edad , Recurrencia Local de Neoplasia/prevención & control , Estadificación de Neoplasias , Cuidados Preoperatorios , Estudios Prospectivos , Curva ROC , Neoplasias del Recto/cirugía , Sensibilidad y EspecificidadRESUMEN
A new lanostane-type terpenoid, lucidenic acid SP1 (1), was isolated from a CHCl(3)-soluble fraction of Ganoderma lucidum spores together with four other known compounds (2 - 5). The structure of lucidenic acid SP1 was determined to be 3 beta,7 beta-dihydroxy-4,4,14 alpha-trimethyl-11,15-dioxo-5 alpha-chol-8-en-24-oic acid by spectroscopic means including 2D-NMR. Twelve triterpenes (1-12) isolated from G. lucidum spores were investigated in vitro for their anticomplementary activity. Compounds 1 - 5 were inactive, whereas ganoderiol F (8), ganodermanondiol (9) and ganodermanontriol (10) showed a strong anticomplement activity against the classical pathway (CP) of the complement system with IC(50) values of 4.8, 41.7, and 17.2 microM, respectively. The potency of these triterpene alcohols (8-10) in inhibiting CP activity was improved when the number of hydroxymethyl groups on the side chain moiety is increased. On the other hand, the ganoderic acids 1-7, which contain a carboxyl group in the side chain, and lucidumols A and B (11, 12) had little activity on this system.
Asunto(s)
Proteínas Inactivadoras de Complemento/farmacología , Lanosterol/aislamiento & purificación , Reishi , Triterpenos/aislamiento & purificación , Activación de Complemento/efectos de los fármacos , Proteínas Inactivadoras de Complemento/química , Medicamentos Herbarios Chinos , Hemólisis/efectos de los fármacos , Hemólisis/inmunología , Humanos , Lanosterol/análogos & derivados , Lanosterol/química , Lanosterol/farmacología , Espectroscopía de Resonancia Magnética , Estereoisomerismo , Triterpenos/química , Triterpenos/farmacologíaRESUMEN
Further studies on leaves of Annona montana led to isolation of one iso-acetogenin, montanacin G, three pairs of acetogenins, montanacin H-J and 34-epi-montanacin H-J, together with four known acetogenins, gigantetrocins A and B, annonacin and cis-annonacin. Montanacin G belongs to the iso-acetogenin group with a terminal 2,4-trans-ketolactone unit. Montanacin H-J and 34-epi-montanacin H-J contain the rare gamma-hydroxy-gamma-methyl-gamma-lactone moiety. The cytotoxic activities of these compounds, together with previously reported acetogenins, montanacins B and C, were examined against Meth-A and LLC tumor cell lines in vitro.
Asunto(s)
4-Butirolactona/análogos & derivados , Annonaceae , Furanos/química , Extractos Vegetales/química , 4-Butirolactona/química , 4-Butirolactona/aislamiento & purificación , 4-Butirolactona/farmacología , Animales , División Celular/efectos de los fármacos , Alcoholes Grasos/química , Alcoholes Grasos/aislamiento & purificación , Alcoholes Grasos/farmacología , Furanos/aislamiento & purificación , Furanos/farmacología , Espectroscopía de Resonancia Magnética , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Árboles/química , Células Tumorales CultivadasRESUMEN
In the search for novel anti-human immunodeficiency virus type 1 (anti-HIV-1) agents from natural sources, 49 MeOH extracts of Korean plants were screened for their inhibitory effects against RNA-dependent DNA polymerase (RT) and ribonuclease H (RNase H) activities of HIV-1 reverse transcriptase and HIV-1 protease, and anti-HIV-1 activity. Regarding the HIV-1 reverse transcriptase, Agrimonia pilosa (whole plant), Cornus kousa (stem and leaf), Limonium tetragonum (root) and Mallotus japonicus (stem) showed significant inhibitory activity on RT activity with 50% inhibitory activity (IC(50)) of 8.9, 6.3, 7.5 and 11.9 microg/mL, respectively, whereas Agrimonia pilosa was also active against RNase H activity (IC(50) = 98.4 microg/mL). Four plants, namely Agrimonia pilosa (whole plant), Atractylodes japonica (root), Clematis heracleifolia (whole plant) and Syneilesis palmata (whole plant), were appreciably active (<35%) against recombinant HIV-1 protease at a concentration of 100 microg/mL. Crinum asiaticum var. japonicum (root) showed significant anti-HIV-1 activity (ED(50) = 12.5 microg/mL) with a favourable SI value of 16.
Asunto(s)
Fármacos Anti-VIH/farmacología , VIH-1/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Proteasa del VIH/metabolismo , Transcriptasa Inversa del VIH/antagonistas & inhibidores , Medicina de Hierbas , Humanos , Corea (Geográfico) , Plantas Medicinales/clasificación , Ribonucleasa H/antagonistas & inhibidores , Ribonucleasa H/metabolismoRESUMEN
A new pyrrolophenanthridone alkaloid, criasiaticidine A (1), was isolated from the bulbs of Crinum asiaticum var. japonicum, together with pratorimine (2), lycorine (3) and 4'-hydroxy-7-methoxyflavan (4). The structure of the new alkaloid was determined to be 4,5-etheno-9,10-dihydroxy-6-phenanthridone by spectroscopic means. The cytotoxicity of the isolated compounds 1-4 was evaluated in vitro against Meth-A (mouse sarcoma) and Lewis lung carcinoma (mouse lung carcinoma) tumor cell lines. Furthermore, 3 was examined for in vivo antitumor activity with LLC tumor cells.
Asunto(s)
Alcaloides/química , Alcaloides/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Fenantrenos/farmacología , Plantas Medicinales/química , Animales , Cromatografía Liquida , Femenino , Indicadores y Reactivos , Japón , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Ratones , Trasplante de Neoplasias , Neoplasias Experimentales/tratamiento farmacológico , Fenantrenos/química , Raíces de Plantas/química , Espectrofotometría Ultravioleta , Células Tumorales CultivadasRESUMEN
Three new kaempferol glycosides, called crassirhizomosides A (1), B (2) and C (3), were isolated from the rhizome of Dryopteris crassirhizoma (Aspidiaceae), together with the known kaempferol glycoside, sutchuenoside A (4). The structures of 1-3 were determined as kaempferol 3-alpha-L-(2,4-di-O-acetyl)rhamnopyranoside-7-alpha-L-rhamnopyranoside, kaempferol 3-alpha-L-(3,4-di-O-acetyl)rhamnopyranoside, and kaempferol 3-alpha-L-(2,3-di-O-acetyl)rhamnopyranosside-7-alpha-L-rhamnopyranoside, respectively, by chemical and spectroscopic means. Inhibitory effects of 1-4 and kaempferol on human immunodeficiency virus reverse transcriptase-associated DNA polymerase (RNA-dependent DNA polymerase and DNA-dependent DNA polymerase) and RNase H activities were investigated.
Asunto(s)
Flavonoides , Glicósidos/química , VIH-1/enzimología , Quempferoles , Plantas Medicinales/química , Quercetina/química , Quercetina/farmacología , Inhibidores de la Transcriptasa Inversa/química , Inhibidores de la Transcriptasa Inversa/farmacología , Carbohidratos/análisis , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Hidrólisis , Espectroscopía de Resonancia Magnética , Metanol , Inhibidores de la Síntesis del Ácido Nucleico , Extractos Vegetales/farmacología , Raíces de Plantas/química , Quercetina/análogos & derivados , Quercetina/aislamiento & purificación , ARN Polimerasa I/antagonistas & inhibidores , Inhibidores de la Transcriptasa Inversa/aislamiento & purificación , Ribonucleasa H/antagonistas & inhibidores , Solventes , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
One new triterpene, 3beta-hydroxy-29-norcycloart-24-one (1), and four new lignans, caruilignans (2-5), together with six known compounds were isolated from the aerial part of Artemisia caruifolia BUCH.-HAM. ex TOXB. Their structures were determined by various spectroscopic means. Most of the isolated lignans were moderately cytotoxic to Meth-A cells with ED50 values of 5-10 microg/ml, but not to Lowis lung carcinoma (LLC) cells. An oxime derivative of 1 showed more potent cytotoxic activity against Meth-A and LLC cells than the original triterpene 1.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Artemisia/química , Lignanos/aislamiento & purificación , Plantas Medicinales , Triterpenos/aislamiento & purificación , Antineoplásicos Fitogénicos/química , División Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Lignanos/química , Lignanos/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura Molecular , Triterpenos/química , Triterpenos/farmacología , Células Tumorales CultivadasRESUMEN
A human intestinal bacterium, Eubacterium (E.) sp. strain SDG-2, was tested for its ability to metabolize various (3R)- and (3S)-flavan-3-ols and their 3-O-gallates. This bacterium cleaved the C-ring of (3R)- and (3S)-flavan-3-ols to give 1,3-diphenylpropan-2-ol derivatives, but not their 3-O-gallates. Furthermore, E. sp. strain SDG-2 had the ability of p-dehydroxylation in the B-ring of (3R)-flavan-3-ols, such as (-)-catechin, (-)-epicatechin, (-)-gallocatechin and (-)-epigallocatechin, but not of (3S)-flavan-3-ols, such as (+)-catechin and (+)-epicatechin.
Asunto(s)
Catequina/análogos & derivados , Catequina/metabolismo , Eubacterium/metabolismo , Compuestos Heterocíclicos/metabolismo , Biotransformación , Humanos , Hidroxilación , Intestinos/microbiología , Espectroscopía de Resonancia Magnética , EstereoisomerismoRESUMEN
Six new highly oxygenated lanostane-type triterpenes, called ganoderic acid gamma (1), ganoderic acid delta (2), ganoderic acid epsilon (3), ganoderic acid zeta (4), ganoderic acid eta (5) and ganoderic acid theta (6), were isolated from the spores of Ganoderma lucidum, together with known ganolucidic acid D (7) and ganoderic acid C2 (8). Their structures of the new triterpenes were determined as (23S)-7beta,15alpha,23-trihydroxy-3,11-dioxolanosta-8, 24(E)-diene-26-oic acid (1), (23S)-7alpha,15alpha23-trihydroxy-3,11-dioxolanosta-8, 24(E)-diene-26-oic acid (2), (23S)-3beta3,7beta, 23-trihydroxy-11,15-dioxolanosta-8,24(E)-diene-26-oic acid (3), (23S)-3beta,23-dihydroxy-7,11,15-trioxolanosta-8, 24(E)-diene-26-oic acid (4), (23S)-3beta,7beta,12beta,23-tetrahydroxy-11,15-dioxolanos ta-8,24(E)-diene-26-oic acid (5) and (23S)-3beta,12beta23-trihydroxy-7,11,15-trioxolanosta-8,24(E )-diene-26-oic acid (6), respectively, by chemical and spectroscopic means, which included the determination of a chiral center in the side chain by a modification of Mosher's method. The cytotoxicity of the compounds isolated from the Ganoderma spores was carried out in vitro against Meth-A and LLC tumor cell lines.
Asunto(s)
Antineoplásicos/farmacología , Reishi/química , Triterpenos/farmacología , Animales , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Carcinoma Pulmonar de Lewis , División Celular/efectos de los fármacos , Ratones , Sarcoma , Esporas/química , Triterpenos/química , Triterpenos/aislamiento & purificación , Células Tumorales CultivadasRESUMEN
Bioassay-guided fractionation of Crataegus pinnatifida (Rosaceae) gave two cytotoxic ursane-type triterpenes which were identified as uvaol (1) and ursolic acid (2) by physicochemical and spectroscopic methods. 3-Oxo-ursolic acid (3) was synthesized from ursolic acid (2) by Jones method. The cytotoxic activities of these compounds were tested against murine L1210 and human cancer cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15) in vitro. Compounds 1 and 2 showed moderate cytotoxicities against L1210, whereas they showed weak activities against human cancer cell lines. However, compound 3 exhibited potent cytotoxic activities both in murine and in human cancer cell lines.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Rosales/química , Triterpenos/farmacología , Animales , Antineoplásicos Fitogénicos/síntesis química , Antineoplásicos Fitogénicos/aislamiento & purificación , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Corea (Geográfico) , Espectroscopía de Resonancia Magnética , Ratones , Hojas de la Planta/química , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Triterpenos/síntesis química , Triterpenos/aislamiento & purificación , Células Tumorales Cultivadas , Ácido UrsólicoRESUMEN
From the stem-bark of Juglans mandshurica, two new naphthalenyl glucopyranosides, 1,4,8-trihydroxynaphthalene 1-O-[alpha-L-arabinofuranosyl-(1-->6)-beta-D-glucopyranoside] (1) and 1,4,8-trihydroxynaphthalene 1-O-beta-D-[6'-O-(3",5"-dihydroxy-4"-methoxybenzoyl)]glucopyranosi de (4), and two new alpha-tetralonyl glucopyranosides, 4 alpha,5,8-trihydroxy-alpha-tetralone 5-O-beta-D-[6'-O-(3",5"-dihydroxy-4"-methoxybenzoyl)]glucopyranosi de (7) and 4 alpha,5,8-trihydroxy-alpha-tetralone 5-O-beta-D-[6'-O-(3",4",5"-trihydroxybenzoyl)]glucopyranoside (8), were isolated together with three known naphthalenyl glucopyranosides (2, 3 and 5), one alpha-tetralonyl glucopyranoside (6), four flavonoids (9-12), and two galloyl glucopyranosides (13, 14). Amongst the isolated compounds, 1,2,6-trigalloylglucopyranose (13) and 1,2,3,6-tertagalloylglucopyranose (14) exhibited the most potent inhibition of reverse transcriptase (RT) activity with IC50 values of 0.067 and 0.040 microM, respectively, while the latter compound also inhibited ribonuclease H (RNase H) activity with an IC50 of 39 microM, comparable in potency to illimaquinone used as a positive control. 1,4,8-Trihydroxy-naphthalene 1-O-beta-D-glucopyranoside (2), 1,4,8-trihydroxynaphthalene 1-O-beta-D-[6'-O-(4"-hydroxy-3",5"-dimethoxybenzoyl)]glucopyranoside (3) and 8 showed moderate inhibition against both enzyme activities, and inhibitory potency of 2 against RNase H activity (IC50 = 156 microM) was slightly greater than that against the RT activity (IC50 = 290 microM). The inhibitory potencies of 4 alpha,5,8-trihydroxy-alpha-tetralone 5-O-beta-D-[6'-O-(4"-hydroxy-3",5"-dimethoxybenzoyl)] glucopyranoside (6), 7 and 8 against RT activity increased accompanied by an increase in the number of free hydroxyls on the galloyl residues, as represented by the IC50 values of > 500, 330 and 5.8 microM, respectively.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Transcriptasa Inversa del VIH/antagonistas & inhibidores , Plantas Medicinales/química , Inhibidores de la Transcriptasa Inversa/farmacología , Ribonucleasa H/antagonistas & inhibidores , Cromatografía Liquida , Dicroismo Circular , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Humanos , Hidrólisis , Corea (Geográfico) , Espectroscopía de Resonancia Magnética , Hibridación de Ácido Nucleico , Epidermis de la Planta/química , Tallos de la Planta/química , Inhibidores de la Transcriptasa Inversa/química , Inhibidores de la Transcriptasa Inversa/aislamiento & purificación , Espectrometría de Masa Bombardeada por Átomos VelocesRESUMEN
Two neolignan compounds, magnolol (5,5'-diallyl-2,2'-dihydroxybiphenyl, 1) and honokiol (5,5'-diallyl-2,4'-dihydroxybiphenyl, 2), were isolated from the stem bark of Magnolia obovata and evaluated for antifungal activity against various human pathogenic fungi. Compound 1 and 2 showed significant inhibitory activities against Trichophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Aspergillus niger, Cryptococcus neoformans, and Candida albicans with minimum inhibitory concentrations (MIC) in a range of 25-100 microg/ml. Therefore, compound 1 and 2 could be used as lead compounds for the development of novel antifungal agents.
Asunto(s)
Antifúngicos/farmacología , Compuestos de Bifenilo/farmacología , Lignanos , Humanos , Pruebas de Sensibilidad MicrobianaRESUMEN
With the aim of finding novel anti-human immunodeficiency virus agents from natural products, 93 MeOH extracts of Korean plants were screened for their inhibitory activities against HIV-1 protease. The most potent inhibition was shown by the root of Rodiola rosea with 70.4% inhibition at a concentration of 100 microg/mL.
Asunto(s)
Inhibidores de la Proteasa del VIH/farmacología , Proteasa del VIH/efectos de los fármacos , VIH-1/enzimología , Medicina Tradicional , Extractos Vegetales/farmacología , Plantas Medicinales/química , Cromatografía Líquida de Alta Presión , Inhibidores de la Proteasa del VIH/aislamiento & purificación , Humanos , Corea (Geográfico) , Extractos Vegetales/aislamiento & purificaciónRESUMEN
The methanol extracts of the leaves of Crataegus pinnatifida showed potent inhibitory activities against HIV-1 protease at a concentration of 100 micrograms/ml. The subsequent fractionation and isolation of the extract gave two active compounds. Their structures were identified as uvaol (1) and ursolic acid (2) by spectral data. These active compounds inhibit HIV-1 protease with IC50 values of 5.5 and 8.0 microM, respectively.
Asunto(s)
Fármacos Anti-VIH/farmacología , Inhibidores de la Proteasa del VIH/farmacología , Rosales/química , Triterpenos/farmacología , Fármacos Anti-VIH/química , Inhibidores de la Proteasa del VIH/química , VIH-1/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/química , Triterpenos/química , Ácido UrsólicoRESUMEN
Two triterpenoid compounds, ursolic acid and uvaol, were isolated from Crataegus pinnatifida Bunge leaves. Ursolic acid inhibits chitin synthase II from S. cerevisiae with an IC50 value of 0.84 microgram/ml and the inhibition appears to be selective for chitin synthase II, whereas uvaol has no inhibitory activity up to 280 micrograms/ml. Oleanolic acid, alpha-hederin hydrate, and betulic acid inhibited the chitin synthase II activity under the same conditions with an IC50 of 5.6, 64.3, and 98.7 micrograms/ml, respectively.
Asunto(s)
Quitina Sintasa/antagonistas & inhibidores , Inhibidores Enzimáticos/farmacología , Rosales/química , Triterpenos/farmacología , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Saccharomyces cerevisiae/enzimología , Triterpenos/química , Triterpenos/aislamiento & purificación , Ácido UrsólicoRESUMEN
Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with IC50 values of 360 and 87 microM, respectively.