Salvia miltiorrhiza,Aquilaria sinensis,Salvia grandifolia,Salvia przewalskii,Nardostachys jatamansi
TANSHINONE,CRYPTO/(R)-1,2,6,7,8,9-Hexahydro-1,6,6-trimethyl-phenanthro(1,2-b)furan-10,11-dione/Phenanthro[1,2-b]furan-10,11-dione, 1,2,6,7,8,9-hexahydro-1,6,6-trimethyl-, (1R)-/Cryptotanshinone/Cryptotanshine/(R)-(−)-1,6,6-Trimethyl-1,2,6,7,8,9-hexahydrophenanthro[1,2-b]furan-10,11-dione/(1R)-1,6,6-Trimethyl-1,2,6,7,8,9-hexahydrophenanthro[1,2-b]furan-10,11-dione/Phenanthro(1,2-b)furan-10,11-dione, 1,2,6,7,8,9-hexahydro-1,6,6-trimethyl-, (R)-
Methanol; Ethyl Acetate; Acetone
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This study is to determine the role and mechanism of cryptotanshinone (CTS) in allergic airway inflammation. Asthma induced by OVA was established in BALB/c mice. We found increased airway hyperresponsiveness (AHR), increased inflammatory cell infiltration, elevated levels of TNF-α, interleukin-1β (IL-1β), IL-4, IL-5, IL-6 and IL-13, decreased interferon gamma (IFN-γ) in lung tissue, increased content of total immunoglobulin E (IgE), OVA specific IgE, Eotaxin, ICAM-1, VCAM-1, nuclear factor-kappaB (NF-κB) and phosphorylation of p38 MAPK in lung tissue. However, the administration of CTS significantly decreased AHR in asthmatic mice, reduced inflammation around the bronchioles and inflammatory cells around airway, regulated cytokine production, reduced the total IgE and OVA-specific IgE levels, and inhibited NF-κB activation and p38 MAPK phosphorylation. In vitro experiments in 16 HBE cells revealed that CTS attenuated CAM-1 and IL-6 expression. These results indicate that CTS alleviates allergic airway inflammation by modulating p38 MAPK phosphorylation and NF-κB activation.
Cryptotanshinone; NF-κB; airway remodeling; asthma; p38 MAPKs
Cryptotanshinone attenuates allergic airway inflammation through negative regulation of NF-κB and p38 MAPK.
Li J1, Zheng M2, Wang C1, Jiang J1, Xu C1, Li L1, Li L1, Yan G1, Jin Y3.
Dan-Lou tablet (DLT) is developed from the traditional Chinese medicine (TCM) formula Gualou Xiebai Baijiu Tang which has been used for at least 2000 years in China. DLT has been widely used in clinical practice to treat cardiovascular diseases.
AIM OF THE STUDY:
This study aimed to uncover the pharmacological mechanism of the compounds absorbed into the blood of Dan-Lou tablet (DLT) on coronary heart disease (CHD) using a network pharmacology integrated pharmacokinetics strategy.
MATERIALS AND METHODS:
A rapid and sensitive method was developed for the simultaneous determination of the six compounds (puerarin, formononetin, calycosin, paeoniflorin, cryptotanshinone and tanshinone IIA) in rat plasma by liquid chromatography tandem mass spectrometry (LC-MS/MS). Then, the pharmacology network was established based on the relationship between five compounds absorbed into the blood targets (puerarin, formononetin, calycosin, cryptotanshinone and tanshinone IIA) and CHD targets.
The intra-and inter-day precision were less than 11% and the accuracy ranged from 88.2% to 112%, which demonstrated that the LC-MS/MS method could be used to evaluate the pharmacokinetic feature of the six compounds in rats after oral administration of DLT. The pathway enrichment analysis revealed that the significant bioprocess networks of DLT on CHD were positive regulation of estradiol secretion, negative regulation of transcription from RNA polymerase II promoter, lipopolysaccharide-mediated signaling pathway and cytokine activity.
The proposed network pharmacology integrated pharmacokinetics strategy provides a combination method to explore the therapeutic mechanism of the compounds absorbed into the blood of multi-component drugs on a systematic level.
Copyright © 2019 Elsevier B.V. All rights reserved.
Compounds absorbed into the blood; Dan-lou tablet; LC-MS/MS; Network pharmacology; Pharmacokinetics
A network pharmacology integrated pharmacokinetics strategy for uncovering pharmacological mechanism of compounds absorbed into the blood of Dan-Lou tablet on coronary heart disease.
Ding M1, Ma W2, Wang X3, Chen S4, Zou S5, Wei J6, Yang Y7, Li J8, Yang X9, Wang H10, Li Y11, Wang Q12, Mao H13, Gao XM14, Chang YX15.
2019 Oct 5;
Systemic lupus erythematosus (SLE) is a chronic, devastating autoimmune disorder associated with severe organ damage. Recently, the role of Signal Transducer and Activator of Transcription 3 (STAT3) in murine lupus has been described, suggesting the involvement of STAT3 signaling in the development of SLE. Cryptotanshinone (CTS) is an effective inhibitor of STAT3; however its potential as a SLE treatment remains to be explored. To determine the function of CTS in SLE, we treated MRL/lpr female mice with CTS. Firstly, we found CTS treatment reversed the elevated STAT3 signaling of spleens in lupus-prone MRL/lpr mice, accompanying with a dramatically decreased number of T cells, especially double-negative (DN) T cells. Further research showed that CTS inhibited T cell proliferation via suppressing of STAT3 activation in vitro and in vivo. Consistently, we also proved that CTS treatment significantly alleviated autoimmune response including notably diminished skin lesions, reduced spleen size and increased life span. In addition, CTS treatment decreased the levels of auto-antibodies and pro-inflammatory cytokines, as well as normalized structure and function of kidneys. All these data suggested that CTS treatment depressed STAT3 phosphorylation, which resulted in blocked DN T cell proliferation and finally attenuated the spontaneous SLE development. Taken together, our data identify CTS as a potential therapeutic drug for SLE patients.
Copyright © 2019. Published by Elsevier B.V.
Cryptotanshinone; STAT3; Systemic lupus erythematosus; T cell proliferation
Cryptotanshinone ameliorates the pathogenesis of systemic lupus erythematosus by blocking T cell proliferation.
Du Y1, Du L1, He Z1, Zhou J1, Wen C2, Zhang Y3.
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.