Delving into the Latest Updates on Cryptotanshinone with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cryptotanshinon, Tanshinone C, MB 11055

+ [2]

Target

SHP2

Mechanism

SHP2 inhibitors(Src homology phosphotyrosyl phosphatase 2 inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication

FibrosisLiver CirrhosisNonalcoholic Steatohepatitis+ [1]

Originator Organization

KT&G Life Sciences Corp.

Active Organization

Case Western Reserve University

Inactive Organization

KT&G Life Sciences Corp.

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC19H20O3

InChIKeyGVKKJJOMQCNPGB-JTQLQIEISA-N

CAS Registry35825-57-1

Membranes have been used as versatile tools for the separation of various natural products; however, the selective separation of structural analogs of natural products using membranes remains challenging. In this study, biocomposite membranes based on poly(ionic liquids) and different natural fibers (jute, cotton, or wool) were successfully prepared. Natural fibers can regulate the microstructure and improve the mechanical properties of membranes. Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, scanning electron microscopy, X-ray photoelectron spectroscopy, atomic force microscopy, Brunauer-Emmett-Teller analysis, and thermo gravimetric analysis were used to characterize the membranes. The membranes were used to separate tanshinone homologs (tanshinone I, tanshinone IIA, cryptotanshinone, and dihydrotanshinone I), allowing cryptotanshinone to penetrate the membrane while rejecting tanshinone I. A maximal selectivity of 44.57 % was obtained for the tanshinone homologs using a one-step separation protocol. These poly(ionic liquids)/natural fiber membranes possess high water flux, good self-cleaning, and good antibacterial properties. The membranes were effective in separating tanshinone homologs and have the potential to separate other natural homologs.

01 Feb 2025·JOURNAL OF ETHNOPHARMACOLOGY

P2Y12 receptor-independent antiplatelet mechanism of cryptotanshinone: Network pharmacology and experimental validation of multi-target signaling pathways

Article

Author: Zhang, Rui ; Yuan, Yujing ; Guo, Fang ; Zhang, Li ; Wu, Meng ; Liu, Gang ; Yang, Zhanzhan ; Liu, Jian ; Hua, Chaoying ; Xiao, Yi

ETHNOPHARMACOLOGICAL RELEVANCE:

Cryptotanshinone serves as the principal bioactive constituent of Salvia miltiorrhiza Bunge, possesses a wide range of pharmacological activities. Salvia miltiorrhiza Bunge, a long-standing therapeutic agent in traditional Chinese medicine (TCM) practice, is renowned for its efficacy in enhancing blood circulation and alleviating blood stasis and infarction, thereby treating cardiovascular and cerebrovascular diseases.

AIM OF THE STUDY:

Platelet activation, when excessive or aberrant, poses a significant risk, catalyzing the onset of various thrombotic disorders. Thus, this investigation is meticulously designed to assess the antiplatelet pharmacological activity of cryptotanshinone, delving into its mechanisms of action that operate independently of the P2Y12 receptor.

MATERIALS AND METHODS:

We employed a combination of isolated human platelet functional analysis, network pharmacology, molecular docking, and animal experiments to explore the P2Y12 receptor-independent antiplatelet targets and the biological mechanisms by which cryptotanshinone improves thrombosis.

RESULTS:

Utilizing the ADP-hydrolyzing enzyme apyrase, we isolated the direct effects of cryptotanshinone on platelet function. The findings reveal that cryptotanshinone can effectively inhibit platelet activation in a manner that is independent of the P2Y12 receptor, all the while maintaining normal tail bleeding times in murine models and not exacerbating mesenteric thrombosis. These effects appear to be mediated through intricate signaling pathways, including PI3K-AKT, MAPK, and STAT3.

CONCLUSION:

This study compellingly confirms the capacity of cryptotanshinone to suppress platelet function independently of the P2Y12 receptor, establishing a robust theoretical foundation for innovative strategies in thrombosis prevention.

01 Jan 2025·PHYTOMEDICINE

Bioinformatics and molecular docking reveal Cryptotanshinone as the active anti-inflammation component of Qu-Shi-Xie-Zhuo decoction by inhibiting S100A8/A9-NLRP3-IL-1β signaling

Article

Author: Zhu, Jun-Qing ; Zheng, Song-Yuan ; Liao, Xiao-Zhong ; Fan, Cui-Ling ; Xie, Rui-Xia ; Chen, Shi-Xian ; Li, Juan ; Zuo, Meng-Yue

BACKGROUND:

Gout is a common type of arthritis marked by monosodium urate (MSU) crystal deposition in joints, triggering an inflammatory response. Qu-Shi-Xie-Zhuo (QSXZ), a traditional Chinese medicine (TCM) formula, has been clinically used for the treatment of gouty arthritis (GA).

PURPOSE:

The study sought to examine the impact of QSXZ on GA and to delve into the pharmacological mechanisms that underlie its effects.

METHODS:

The chemical constituents of QSXZ were analyzed through UPLC-MS. MSU-induced acute gouty arthritis (AGA) and subcutaneous (SC) air pouch models in mice were employed to evaluate the anti-inflammatory properties of QSXZ and its primary active compound, Cryptotanshinone (CTS). To investigate the therapeutic mechanisms of QSXZ, we used MS-based network pharmacology, transcriptomic analysis, molecular docking and multiscale bioassays.

RESULTS:

Treatment of QSXZ revealed a significant reduction of inflammatory cell infiltration and the expression of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α) and interleukin -1β (IL-1β). Based on UPLC/MS/MS results, 49 components were considered the active ingredients of QSXZ. Network pharmacology analysis indicated that QSXZ regulates multiple inflammation-related pathways. Subsequent transcriptomic analysis showed that QSXZ regulates gene expression of S100A8 and S100A9. Our investigation observed an increased expression of S100A8 and S100A9 in monocytes derived from gout patients. Molecular docking and molecular dynamics simulation analysis revealed the binding pattern and interaction between QSXZ active compound CTS and S100A8/A9, and subsequent surface plasmon resonance (SPR) and cell thermal shift assay (CETSA) experiments verified the direct interaction between them. To investigate the mechanisms of action, we conducted RT-PCR, Western blotting, immunohistochemistry, flow cytometry, and measured the inflammatory response. Our findings highlight the pathogenic role of S100A8/A9 mediated TLR4-NLRP3 axis in gout and review outstanding therapeutic effects of QSXZ and its primary active compound CTS on MSU-induced experimental models.

CONCLUSIONS:

In summary, this study substantiates the therapeutic potential of QSXZ and its primary active compound CTS, as promising alternative treatments for GA. Our findings provide valuable insight into the critical pharmacological mechanism of QSXZ in regulating inflammation, highlighting its potential therapeutic effects in GA management.

100 Deals associated with Cryptotanshinone

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB15579

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fibrosis	Phase 2	-	KT&G Life Sciences Corp.	-
Liver Cirrhosis	Phase 2	KR	KT&G Life Sciences Corp.	-
Nonalcoholic Steatohepatitis	Phase 2	KR	KT&G Life Sciences Corp.	-
Obesity	Phase 2	KR	KT&G Life Sciences Corp.	-
Neoplasms	Preclinical	US	Case Western Reserve University	26 Sep 2013

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SFN2010	Not Applicable	-	-	Cryptotanshinone (CRY)	fvewtoetir(mfsiytqpyd) = ccivwchpma ockfbnddsw (plehmltzir )	-	13 Nov 2010
				Sodium nitroprusside (SNP)	fvewtoetir(mfsiytqpyd) = zotolklwdz ockfbnddsw (plehmltzir )