The anti-HIV-1 effect of scutellarin

Zhang, Gao-Hong; Wang, Qian; Chen, Ji‐Jun; Zhang, Xuemei; Tam, Siu-Cheung; Zheng, Yong‐Tang

doi:10.1016/j.bbrc.2005.06.166

Cited by 93 publications

(53 citation statements)

References 20 publications

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“…Scutellarin produces an anti-inflammatory effect via actions on arachidonic acid metabolism [6] . The compound has also been shown to have some anti-HIV effects [7] and to attenuate hepatocellular damage [8] . It is interesting that scutellarin exhibits weak estrogenic properties [9,10] , similar to genistein and apigenin.…”

Section: Introductionmentioning

confidence: 99%

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

et al. 2011

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Aim: To study the metabolic and pharmacokinetic profile of scutellarin, an active component from the medical plant Erigeron breviscapus (Vant) Hand-Mazz, and to investigate the mechanisms underlying the low bioavailability of scutellarin though oral or intravenous administration in rats. Methods: HPLC method was developed for simultaneous detection of scutellarin and scutellarein (the aglycone of scutellarin) in rat plasma, urine and feces. The in vitro metabolic stability study was carried out in rat liver microsomes from different genders. Results: After a single oral dose of scutellarin (400 mg/kg), the plasma concentrations of scutellarin and scutellarein in female rats were significantly higher than in male ones. Between the female and male rats, significant differences in AUC, t max2 and C max2 for scutellarin were found. The pharmacokinetic parameters of scutellarin in the urine also showed significant gender differences. After a single oral dose of scutellarin (400 mg/kg), the total percentage excretion of scutellarein in male and female rats was 16.5% and 8.61%, respectively. The total percentage excretion of scutellarin and scutellarein in the feces was higher with oral administration than with intravenous administration. The in vitro t 1/2 and CL int value for scutellarin in male rats was significantly higher than that in female rats. Conclusion:The results suggest that a large amount of ingested scutellarin was metabolized into scutellarein in the gastrointestinal tract and then excreted with the feces, leading to the extremely low oral bioavailability of scutellarin. The gender differences of pharmacokinetic parameters of scutellarin and scutellarein are due to the higher CL int and lower absorption in male rats.

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Section: Introductionmentioning

confidence: 99%

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

et al. 2011

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“…After alkaline hydrolysis of 3 with 5 M NaOH solvent, 11 was detected in reaction mixture by TLC. The rings AD and side chain of 3 were identical to those of 11 by detailed analysis of the 13 Comparison of NMR data of 4 (Tables 15) with those of jinfushanoside B revealed great similarity. 4 The difference was that the C-6' position of the sugar unit in 4 was ester-linked to a HMG functionality, on the basis of the HMBC correlations from δ H 5.04 (d, J = 11.3 Hz, H a -6') and δ H 4.72 (m, H b -6') to δ C 171.7 (s, C-1''), from δ H 3.11 (d, J = 14.0 Hz, H a -2'') and δ H 3.08 (d, J = 14.0 Hz, H b -2'') to δ C 171.7 (s, C-1''), 70.2 (s, C-3''), 47.0 (t, C-4''), and 28.4 (q, C-6''), and from δ H 3.17 (br.…”

Section: Resultsmentioning

confidence: 77%

“…Jinfushanencin A (1) 8 , 533.3114) and 13 C NMR spectroscopic data. The IR spectrum revealed absorptions at 3436, 1696, and 1648 cm -1 , suggestive of hydroxyl and conjugated carbonyl groups.…”

Section: Resultsmentioning

confidence: 99%

“…Jinfushanoside E (3) had a molecular formula of C 42 H 66 O 12 determined by HRESIMS, 13 C NMR, and DEPT experiments. The molecular weight of 3 was 144 mass units more than that of delavanoside D (11).…”

Section: Resultsmentioning

confidence: 99%

“…The anti-HIV-1 activity was evaluated by the inhibition assay for the cytopathic effects of HIV-1 (EC 50 ), and cytotoxicity assay against C8166 cells (IC 50 ) was assessed using the MTT method as described in the literature. 13 …”

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confidence: 99%

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Cucurbitane triterpenoids from Hemsleya penxianensis

Chen

Zhou

Wang

et al. 2012

Nat. Prod. Bioprospect.

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Two new cucurbitacins, jinfushanencins A (1) and B (2), seven new cucurbitane glycosides, jinfushanosides EK (39), along with nine known analogues, were obtained from the tubers of Hemsleya penxianensis. Their structures were elucidated on the basis of extensive spectroscopic and chemical methods. Selected isolates were tested their anti-HIV-1 activities, and compound 5 showed weak anti-HIV-1 in C8166 cell (EC 50 = 5.9 μg/mL) with a selectivity index of 13.5.

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Scutellarin inhibits hypoxia‐induced epithelial‐mesenchymal transition in bladder cancer cells

Liu

et al. 2019

Journal Cellular Physiology

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Scutellarin, an active component of flavonoid, displays a variety of physiological actions and has been applied for the treatment of diverse diseases including hypertension and cerebral infarction as well as cerebral thrombosis. In recent time, Scutellarin has been demonstrated to possess the anticancer activity. But the biological significance of Scutellarin in bladder cancer (BC) remains to be elucidated. In the current study, we explored the specific effect of Scutellarin on BC progression. We found that Scutellarin inhibited hypoxia-induced BC cell migration and invasion in vitro as well as suppressed hypoxia-induced BC metastasis in vivo. Moreover, Scutellarin significantly reversed hypoxia-promoted epithelial-mesenchymal transition (EMT) in BC cells and the PI3K/Akt and MAPK pathways were implicated in the suppressive effect. Taken together, we suggested the potential value of Scutellarin as a novel anticancer agent for BC treatment. K E Y W O R D S bladder cancer (BC), epithelial-mesenchymal transition (EMT), hypoxia, Scutellarin

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The anti-HIV-1 effect of scutellarin

Cited by 93 publications

References 20 publications

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

Cucurbitane triterpenoids from Hemsleya penxianensis

Scutellarin inhibits hypoxia‐induced epithelial‐mesenchymal transition in bladder cancer cells

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