Disease relevance of Kusaginin

• Acteoside was an antiestrogen in breast cancer cells and osteoblasts, without any effect on endometrial cells [1].
• Acetoside, a component of Stachys sieboldii MIQ, may be a promising antinephritic agent: effect of acteoside on crescentic-type anti-GBM nephritis in rats [2].
• This novel pharmacological action if occurring in small vessels in vivo, may contribute to the reported anti-inflammatory effect of acteoside against NO-mediated vascular permeability-related acute edema [3].
• In the present study, we examined anti-amnesic activity of acteoside using scopolamine-induced (1 mg/kg body weight, s.c.) amnesic mice with both passive avoidance and Morris water maze tests [4].
• Male C57BL/6 mice were injected intravenously with 2 x 10(5) of B16 melanoma cells, while acteoside at a dose of 50 mg/kg was administered intraperitoneally every other day from 13 d before B16 melanoma cell injection until all mice had succumbed to the metastatic tumor burden in the lung [5].

Psychiatry related information on Kusaginin

• It is interesting to note that prolonged oral daily treatment of mice with much lower amount (0.1 mg/kg body weight) of acteoside for 10 d reversed the scopolamine-induced memory deficits [4].
• We suggest, therefore, that acteoside has anti-amnesic activity that may ultimately hold significant therapeutic value in alleviating certain memory impairment observed in Alzheimer's disease [4].

High impact information on Kusaginin

• Isolation and purification of acteoside and isoacteoside from Plantago psyllium L. by high-speed counter-current chromatography [6].
• Two new phenylpropanoid glycosides, caerulescenoside ( 1), and 3'-methyl crenatoside ( 2), as well as five known phenylpropanoid glycosides [acteoside ( 3), isoacteoside ( 4), campneoside II ( 5), crenatoside ( 6), and desrhamnosyl acteoside ( 7)] were isolated from the whole plant of Orobanche caerulescens [7].
• We conclude that acteoside prevents the MPP+-induced apoptosis and inhibits the apoptosis-related pathway [8].
• In this study we assessed the effect of acteoside that significantly improved cell viability and inhibited lactate dehydrogenase (LDH) release [8].
• Western blot analysis demonstrated that acteoside inhibits the active caspase-3 fragment (17 kDa) (P < 0.001) and the proteolytic poly (ADP-ribose) polymerase (PARP) fragment (85 kDa) expression (P < 0.001) following MPP + treatment in CGNs [8].

Chemical compound and disease context of Kusaginin

• We investigated the effect of acteoside in comparison with that of cyclosporin A on leukocyte accumulation in the glomeruli of rats with crescentic-type anti-glomerular basement membrane (GBM) nephritis [9].
• The result showed that acteoside and prednisolone treatments (in either early or late period) significantly reduced proteinuria, mesangial matrix expansion (the index of matrix expansion) and mesangial proliferation as determined by the number of proliferating nuclear cell antigen (PCNA)-positive cells [10].
• We examined the antimetastatic effect of acteoside, a phenylethanoid glycoside widely distributed in the plant kingdom, on lung metastasis using a mouse model injected with B16 melanoma cells intravenously [5].

Biological context of Kusaginin

• These data support the finding that acteoside inhibits the up-regulation of ICAM-1 in the nephritic glomeruli [11].
• Acteoside exhibited anti-oxidant effects on FeCl2-ascorbate induced lipid peroxidation in a mouse liver homogenate, and on superoxide radical scavenging activity [12].
• Acteoside protects endothelial cells against free radical-induced oxidative stress [13].
• The present results indicate that acteoside enhanced the evoked vasoconstriction, mainly through inhibition of endothelial NO production/release and inhibition of NO-mediated TEA(+)-sensitive activation of K(+) channels [14].
• However, in this dose, acteoside did not significantly suppress the antibody formation [9].

Anatomical context of Kusaginin

• The inhibitory effect on endothelial nitric oxide-mediated relaxation suggests that acteoside could also act on the endothelial cells to reduce nitric oxide release [15].
• Removal of endothelium enhanced the relaxing effect of acteoside [15].
• Acteoside, a component of Stachys sieboldii MIQ, may be a promising antinephritic agent (2): Effect of acteoside on leukocyte accumulation in the glomeruli of nephritic rats [9].
• Acteoside prevented the up-regulation of ICAM-1 expression mediated by inflammatory cytokines or phorbol 12-myristate 13-acetate on HUVECs and rat mesangial cells [11].
• Adhesion of neutrophils and macrophages to acteoside-treated HUVECs was suppressed to one half of that in untreated HUVECs [11].

Associations of Kusaginin with other chemical compounds

• We have previously reported that acteoside isolated from the leaves of Callicarpa dichotoma has significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultured rat cortical cells [16].
• Treatment with acteoside significantly suppressed bradykinin-induced increase in [Ca2+]i of cultured rat aortic endothelial cells [3].
• Pre-administration of acteoside at 10 or 50 mg/kg subcutaneously at 12 and 1 h prior to D-GalN/LPS intoxication significantly inhibited hepatic apoptosis, hepatitis and lethality [17].
• Changes in catalpol, aucubin, and acteoside concentrations in the leaves during the growing season and by drying after harvesting were quantitatively determined by high-performance liquid chromatography [18].
• A new iridoid glycoside, gelsemiol 6'-trans-caffeoyl-1-glucoside (1), was isolated from Verbena littoralis, together with four known phenylethanoid glycosides, acteoside (2), 2'-acetylacteoside (3), jionoside (4), and isoverbascoside (5) [19].

Gene context of Kusaginin

• The inhibitory effect of AP-1 activation by acteoside may be associated with the anti-inflammatory effects of Buddlejae Flos [20].
• Western blot and RT-PCR analyses revealed that acteoside inhibited the LPS-induced levels of the iNOS protein and mRNA [20].
• A phenylpropanoid glycoside acteoside was found to induce interleukin (IL)-1, IL-6, and tumor necrosis factor-alpha (TNF-alpha) in macrophage-like cell line J774.A1 at 1-100 ng/ml [21].
• Therefore, we investigated the effects of acteoside on the expression of intercellular adhesion molecule-1 (ICAM-1) in nephritic glomeruli, in vivo, and human umbilical vein endothelial cells (HUVECs) and rat mesangial cells, in vitro [11].
• Assessment of their antioxidant activities established that acteoside, a polyhydroxylated phenylpropanoid glycoside derivative, is the most potent free radical scavenger and showed the highest protection factor (PF(r)) against sunflower-oil-induced oxidative rancidity [22].

Analytical, diagnostic and therapeutic context of Kusaginin

• Acteoside given p.o. at a dose of 30 mg/kg once a day for 15 consecutive days after treatment with anti-GBM serum markedly suppressed the urinary protein as well as glomerular histological changes [9].
• Extensive isolation work guided by a bioassay afforded a phenylethanoid, acteoside, as an active compound [23].
• Applying the MEKC method established in this study, rapid and simultaneous determinations of acteoside together with 3 flavonoids in samples were achieved [24].
• Analysis of extracted DNA on agarose gel electrophoresis revealed that acteoside induced the internucleosomal breakdown of chromatin DNA characteristic of apoptosis [25].
• We isolated acteoside from Buddlejae Flos, which has been used as a traditional medicine to treat conjunctive congestion and sepsis [20].

References