Abstract:
:Before the design of brucine-containing transdermal formulations, the pharmacodynamics and pharmacokinetics of brucine following transdermal administration should be evaluated. In this study, the effect of addition of ethanol on solubility of bruicne was investigated and 20% ethanol was added into PBS to obtain 10mg/mL brucine solution. Then three transdermal doses (10, 20 and 40 mg/kg) were administered to mice to evaluate pharmacological activity. It had been demonstrated that brucine possessed analgesic and anti-inflammatory activity in a dose-dependent manner. Cytotoxicities of brucine against various tumor cells including skin tumor cell were also compared in vitro. Brucine was found to possess antitumor activity in a concentration and time-dependent manner and gastrointestinal tumor cells seemed to be more sensitive to brucine. Then in vitro skin permeation behavior and in vivo pharmacokinetics following transdermal administration were further investigated. The cumulative amounts of brucine across mouse skin in vitro were found to be higher than 90%. The absolute bioavailability of brucine was determined to be 40.83%. And compared with intravenous administration, MRT and T1/2 values were increased about 8~12-fold by transdermal route. Moreover, fluctuations of drug levels were found to be significantly decreased in tissues, especially in brain. Finally, no dermal toxicity of brucine was observed. The results of this study indicated that transdermal administration might be beneficial for the sustained efficacy and reduced toxicity of brucine.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
Chen J,Hu W,Qu YQ,Dong J,Gu W,Gao Y,Fang Y,Fang F,Chen ZP,Cai BCdoi
10.1016/j.fitote.2013.03.007subject
Has Abstractpub_date
2013-04-01 00:00:00pages
193-201eissn
0367-326Xissn
1873-6971pii
S0367-326X(13)00064-6journal_volume
86pub_type
杂志文章相关文献
FITOTERAPIA文献大全abstract::Curcuphenol is a sesquiterpene isolated from sponges and plants having several significant biological activities. The present study explored its effect on cell proliferation and apoptosis in Caco-2 human colon cancer cells. It was demonstrated that curcuphenol in concentrations in the range of 29-116 µg/ml inhibited c...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2010.04.001
更新日期:2010-10-01 00:00:00
abstract::Besides the unquestionable positive effects of solar exposure for human health, UV rays have been widely investigated for toxicology aspects related to excessive UVB and UVA doses, which involve sunburns, skin aging, DNA skin damage and tumorigenesis. At present, synthetic and mineral sunscreens are used to protect ag...
journal_title:Fitoterapia
pub_type: 杂志文章,评审
doi:10.1016/j.fitote.2016.09.003
更新日期:2016-10-01 00:00:00
abstract::European Hawthorn species (Crataegus spp.) are traditionally used for their demonstrated cardioprotective benefits. Most products are based on the compendial leaf and flower drug (LFD), which is standardised on the total flavonoid content (TF). In order to reduce variability associated with the wild plant origin and t...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2007.06.010
更新日期:2008-01-01 00:00:00
abstract::The purpose of this investigation was to study the modulator and efflux pump inhibitor activity of coumarins isolated from Mesua ferrea against clinical strains as well as NorA-over expressed strain of Staphylococcus aureus 1199B. Seven coumarins were tested for modulator activity using ethidium bromide (EtBr) as a su...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2013.07.015
更新日期:2013-10-01 00:00:00
abstract::The ecological role of maytansine, an important antineoplastic and antimicrobial compound with high cytotoxicity, particularly as a chemical defense compound has remained elusive since its discovery in the 1970s in Maytenus and Putterlickia plants. In the present study, we have used MALDI-imaging-HRMS to visualize the...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2017.03.014
更新日期:2017-06-01 00:00:00
abstract::The cytotoxic effects of seven constituents isolated from Duguetia glabriuscula were evaluated against Hep2 human larynx carcinoma cells. The cytotoxicity exhibited by beta-sitosterol was as strong as that of cis-platin. (+)-Alloaromadendran-10,14beta-diol caused inhibition of cellular growth with IC50 values lower th...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2006.01.013
更新日期:2006-04-01 00:00:00
abstract::We investigated the effect of caffeoylserotonin (CaS) on THP-1 monocyte migration and adhesion to fibronectin in response to MCP-1. CaS decreased monocyte adhesion and migration induced by MCP-1, together with CCR2 expression and α5β1 integrin, and activated β1 integrin expression on the cell surface. CaS also inhibit...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2012.04.025
更新日期:2012-12-01 00:00:00
abstract::Diterpene alkaloids neoline (1), napelline (2), isotalatizidine (3), karakoline (4), senbusine A (5), senbusine C (6), aconitine (7) and taurenine (8) were identified from Aconitum napellus L. subsp. firmum, four (2-4, 6) of which are reported for the first time from this plant. The structures were determined by means...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2013.07.010
更新日期:2013-10-01 00:00:00
abstract::Two triglycerides, both bearing polyunsaturated fatty acid residues, were isolated from the hexane extract of Urena lobata. One of them is characterized by the presence of three different polyunsaturated fatty acids. Their structures were studied with spectral methods. ...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2006.03.010
更新日期:2006-06-01 00:00:00
abstract::Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than pa...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2013.10.015
更新日期:2014-01-01 00:00:00
abstract::The objective of this study was to evaluate potential hepatoprotective capabilities of quercetin in relation to its modulation of the HO-1 and NOS-2 activities in an experimental model of fulminant liver failure. Liver insult was induced by in vivo administration of D-galactosamine (d-GalN, 400 mg/kg, i.p.) and lipopo...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2013.03.016
更新日期:2013-06-01 00:00:00
abstract::Acteoside, which belongs to the family of phenylethanoid glycosides (PhGs), has extensive biological activities, including strong antioxidant, anti-inflammatory, hepatoprotect, and cell apoptosis regulation. Like other PhGs compounds, the fate of acteoside in the gut for both parent polyphenols and their degradation p...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2016.05.004
更新日期:2016-07-01 00:00:00
abstract::Since the extract from berries of Aronia melanocarpa presents antioxidative properties in plasma and in blood platelets, not only from healthy group, but also from patients with benign breast diseases and in patients with invasive breast cancer before surgery, the aim of our present study was to evaluate the oxidative...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2011.11.007
更新日期:2012-03-01 00:00:00
abstract::Natural products chemistry is the discipline that lies at the heart of modern pharmacognosy. The field encompasses qualitative and quantitative analytical tools that range from spectroscopy and spectrometry to chromatography. Among other things, modern research on crude botanicals is engaged in the discovery of the ph...
journal_title:Fitoterapia
pub_type: 杂志文章,评审
doi:10.1016/j.fitote.2010.09.011
更新日期:2011-01-01 00:00:00
abstract::Five new aromatic compounds, designed as lucidumins A-D (1-4) and lucidimine E (9), along with seven known aromatic compounds (5-8, 10-12) were isolated from Ganoderma lucidum. Their structures were determined by spectroscopic method. Bioactive evaluation showed that compounds 2-4 and 6-10 displayed remarkable neuropr...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2019.01.013
更新日期:2019-04-01 00:00:00
abstract::Centella asiatica (L.) Urban is a medicinal herb traditionally used in Asiatic countries for its multiple therapeutic properties, essentially due to its accumulation of specific pentacylic triterpenoid saponins, mainly asiaticoside and madecassoside and the corresponding sapogenins. This review summarizes the updated ...
journal_title:Fitoterapia
pub_type: 杂志文章,评审
doi:10.1016/j.fitote.2016.07.011
更新日期:2016-10-01 00:00:00
abstract::The effect of Cyclovirobuxine D, an active ingredient from Buxus microphylla, was investigated in the potential prevention of cardiac dysfunction in rats with congestive heart failure. Heart failure was induced by left coronary artery occlusion and verified using echocardiography. Cyclovirobuxine D was administered fo...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2011.04.016
更新日期:2011-09-01 00:00:00
abstract::Three new glucosides, namely, (-)-7R8S-7',8'-dihydroxy-dihydrodehydroconiferyl alcohol-9-O-β-D-glucopyranoside (1), (+)-7S8R-7',8'-dihydroxy-dihydrodehydroconiferyl alcohol-9-O-β-D-glucopyranoside (2) and 4-hydroxy-2-methoxyphenyl 1-O-[6-(hydrogen 3-hydroxy-3-methylpentanedioate)]-β-D-glucopyranoside (3), along with 6...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2014.09.020
更新日期:2014-12-01 00:00:00
abstract::The essential oil from the aerial parts of Seseli annuum, wild-growing in Serbia, was obtained by hydrodistillation and analyzed using GC and GC/MS. A total of 43 components were identified representing 96.5% of S. annuum oil. The most abundant compounds were germacrene D (29.8%), sabinene (10.3%), beta-ocimene Z (9.8...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2007.03.014
更新日期:2007-06-01 00:00:00
abstract::Influenza poses a particular risk of severe outcomes in the elderly, the very young and those with underlying diseases. Tea polyphenols are the natural phenolic compounds in teas, and principally consist of catechins, proanthocyanidins, flavonols, and theaflavins, which antiviral activities have been reported recently...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2013.12.011
更新日期:2014-03-01 00:00:00
abstract::The effect of berberine hydrochloride (BBR) on inducible cyclooxygenase-2 (COX-2) in small intestinal mucosa and related mechanisms was investigated in a rat model of acute endotoxemia. The results showed that lipopolysaccharide (LPS) increased COX-2 expression, whereas SB202190 and BBR curtailed it. LPS increased pho...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2011.05.013
更新日期:2011-10-01 00:00:00
abstract::The composition of the essential oil of Lindera neesiana Kurz fruit was examined by GC-MS, (1)H, (13)C and bidimensional NMR techniques (HMQC, HMBC, COSY, TOCSY). Forty compounds were identified, representing approximately 86% of the oil: Z-citral (15.08%), E-citral (11.89%), eucalyptol (8.75%), citronellal (6.72%), a...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2009.06.017
更新日期:2010-01-01 00:00:00
abstract::Methanol extract of the stem bark of Hymenodictyon parvifolium was tested for its antifungal and antibacterial activity. The extract was found to have inhibitory effect against all the pathogens tested. ...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/s0367-326x(02)00176-4
更新日期:2002-10-01 00:00:00
abstract::Fruit's decoctions of Passiflora edulis and P. foetida var. albiflora were evaluated for the inhibition of activity of gelatinase MMP-2 and MMP-9, two metallo-proteases involved in the tumour invasion, metastasis and angiogenesis. Both water extracts, at different concentrations, inhibited the enzymes. ...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/s0367-326x(03)00023-6
更新日期:2003-04-01 00:00:00
abstract::The furanocoumarin imperatorin has been reported to have hypotensive effect, and we have investigated its activity on myocardial hypertrophy. Imperatorin displayed similar chromatographic retention peak to verapamil in the model of cardiac muscle/cell membrane chromatography, and could reduce in a concentration-depend...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2010.07.023
更新日期:2010-12-01 00:00:00
abstract::Cyperenoic acid (1) is one of the major sesquiterpenes isolated from Croton crassifolius, which exhibited potent anti-angiogenic activity. Traditional structural modification of 1 is difficult to perform by chemical technology due to the remarkable stability of the patchoulane skeleton. In order to overcome chemical s...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2017.02.004
更新日期:2017-04-01 00:00:00
abstract::Seven new lignan glycosides (1-3, 8-10, and 14) and 17 known compounds were isolated from the branches of Alangium kurzii Craib var. laxifolium. Their structures were established by spectroscopic analysis and circular dichroism (CD) and X-ray analysis. The isolated compounds were evaluated for their antibacterial acti...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2017.07.009
更新日期:2017-09-01 00:00:00
abstract::Ten new highly oxygenated lanostane triterpenoids, stereinones A-J (1-10), were isolated from the fruiting bodies of the basidiomycete Stereum sp. Compounds 3 and 4 are structurally characterized as intact lanostane-type triterpenoids containing unusual 1,2-diketone functionality at C-11 and C-12, while compound 10 is...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2017.11.020
更新日期:2018-03-01 00:00:00
abstract::Commiphoins A-C (1-3), three new cadinane-type sesquiterpenes, together with two known cadinane-type sesquiterpenes (4 and 5) were isolated from the resinous exudates of Commiphora myrrha. Their structures and relative configurations were established on the basis of comprehensive spectroscopic methods, including HRESI...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2020.104536
更新日期:2020-04-01 00:00:00
abstract::Two new isocoumarins (1 and 2), a new alkaloid (3), and a known N-acetyldopamine dimer (4) were isolated from the ethyl acetate extract of Chinese insect medicine Eupolyphaga sinensis. Their structures were elucidated on the basis of detailed spectroscopic investigations, such as 1D- and 2D NMR spectroscopy, as well a...
journal_title:Fitoterapia
pub_type: 杂志文章
doi:10.1016/j.fitote.2012.06.005
更新日期:2012-10-01 00:00:00