Delving into the Latest Updates on Cryptotanshinone with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cryptotanshinon, CTS, Tanshinone C

+ [3]

Target

SHP2 x STING

Action

inhibitors

Mechanism

SHP2 inhibitors(Src homology phosphotyrosyl phosphatase 2 inhibitors), STING inhibitors(Stimulator of interferon genes inhibitors)

Therapeutic Areas

NeoplasmsNervous System DiseasesEye Diseases+ [1]

Active Indication

GlioblastomaRetinal DiseasesNeoplasms

Inactive Indication

FibrosisLiver CirrhosisNonalcoholic Steatohepatitis+ [1]

Originator Organization

KT&G Life Sciences Corp.

Active Organization

Shanghai University of Traditional Chinese Medicine

Jinan UniversityShanghai Jiao Tong University School of Medicine

+ [1]

Inactive Organization

KT&G Life Sciences Corp.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC19H20O3

InChIKeyGVKKJJOMQCNPGB-JTQLQIEISA-N

CAS Registry35825-57-1

Cancer, with a high incidence and mortality rate, has emerged as a major public health problem worldwide. Currently, new approaches, such as targeted therapy and immunotherapy, are giving hope to patients. However, drug resistance and adverse side effects are major barriers to cancer treatment. As a result, there is a greater focus on the development of cancer therapy strategies and medications with low toxicity and high efficacy. Cryptotanshinone (CTS), a diterpenoid quinone extracted from Salvia miltiorrhiza Bunge, exhibits a wide range of biological activities, including immunomodulatory, anti-inflammatory, and antitumor effects. In recent years, numerous studies have highlighted its significant antitumor properties, indicating potential clinical applications and development value. However, the clinical use of cryptotanshinone has been limited due to its poor water solubility and low bioavailability. To overcome these limitations, researchers are exploring new drug delivery systems, and novel formulation systems based on nanotechnology are being developed to improve the delivery and effectiveness of cryptotanshinone. In this review, we aim to consolidate the existing knowledge regarding the antitumor effects of cryptotanshinone and emphasize the latest advancements in its nanoformulation development. We hope to provide insights that will further improve the antitumor efficacy and clinical applicability of cryptotanshinone.

01 Sep 2025·Current Computer-Aided Drug Design

Study on the Mechanism of Action of the Traditional Chinese Medical Prescription Gushukang in Treating Osteoporosis Based on Network Pharmacology and Experimental Verification

Article

Author: Li, Xincheng ; Zhu, Shaowen ; Wang, Shujun ; Yang, Zhao

Background::

Gushukang (GSK), a traditional Chinese medical prescription, has made a great and extensive contribution to the treatment of different forms of osteoporosis, but polypharmacology studies of its mechanism of action are lacking. This study investigates the pharmacological mechanism of osteoporosis using network pharmacology and molecular docking. Experimental verification was carried out to confirm the efficacy of GSK on RANKLinduced osteoclast differentiation in RAW264.7 cells to verify the network pharmacology studies.

Methods::

The effective chemical components and corresponding targets of osteoporosis with oral bioavailability of more than 30% and drug-like properties greater than 0.18 were searched in the TCMSP and TCM-ID databases. DrugBank, GeneCards, OMIM, TTD, and other databases were examined for targets related to osteoporosis. Using Cytoscape software, a network of possible TCM-active ingredient-osteoporosis targets was created. STRING software was used to create the networks of protein-protein interactions. The DAVID program was carried out to conduct GO and KEGG pathway enrichment analyses of the targets. Molecular docking and pattern of action analysis were carried out using software like AutoDock Vina and Discovery Studio Visualizer. The growth media for RAW264.7 cells contained varying doses of GSK serum and 50 ng/mL RANKL. The activity of TRAP was altered. Additionally, genes related to osteoclasts were examined using an RT-PCR assay.

Results::

Network pharmacological analysis revealed that the primary efficacy targets of osteoporosis were PTGS2, PTGS1, HSP90AA1, NCOA2, ADRB2, ESR1, NCOA1, and AR. The pharmacological targets of osteoporosis may be mediated by substances including quercetin, kaempferol, luteolin, naringenin, icariin, anthocyanin, tanshinone IIA, and cryptotanshinone. GSK markedly inhibited RANKL-induced TRAP activity. qRT-PCR results revealed decreased expression of the PTGS2 and ADRB2 genes upon GSK treatment.

Conclusion::

The findings of network pharmacology, molecular docking, as well as experimental verification provide a new further study for elucidating the pharmacodynamic substance basis and polypharmacology mechanism of GSK in treating osteoporosis.

01 Sep 2025·PHYTOMEDICINE

Cryptotanshinone attenuates lactate-induced nucleus pulposus cells injury by modulating the STAT3/SIRT3 signaling axis

Article

Author: Chen, Yi-Tuo ; Li, Xi-Lei ; Yuan, Guang-Cheng ; Wu, Tao ; Huang, Yu-Kai ; Lu, Jia-Jie ; Dong, Jian ; Zhang, Qi-Chen ; Jiang, Li-Bo ; Zhang, Qian-Yi

INTRODUCTION:

Intervertebral disc degeneration (IVDD) stands out as one of the prevalent root causes of low back pain (LBP). In degenerated discs, the dysregulation of glucose metabolism and the impairment of nutrient transport result in the accumulation of lactate, which exacerbates oxidative stress in the microenvironment of the intervertebral disk thereby inducing senescence, apoptosis and metabolic imbalance of the extracellular matrix in the nucleus pulposus cells (NPCs). In this context, elucidating the precise pathogenesis of disc degeneration and advancing the development of targeted molecular therapies hold significant therapeutic implications for future medical interventions.

OBJECTIVE:

The objective is to systematically evaluate small molecule compounds that influence intracellular oxidative stress and to elucidate their pharmacological effects and underlying molecular mechanisms.

METHODS:

The small molecule compound cryptotanshinone (Cry) was identified through a comprehensive literature, and the biosignature of the drug-disease target was subsequently analyzed utilizing network pharmacology methodologies. Subsequently, the pharmacological effects and molecular mechanisms of cryptotanshinone in the treatment of IVDD were investigated by ex vivo and in vivo experiments such as RNA-seq, Western blotting, immunofluorescence, SA-β-gal, Tunel, flow cytometry, immunohistochemistry, and animal imaging.

RESULTS:

In vitro findings demonstrated that Cry mitigates lactate-induced oxidative stress through modulation of the STAT3/SIRT3 signaling pathway, thereby reducing senescence, apoptosis, and extracellular matrix (ECM) degradation in NPCs. Meanwhile, the outcomes of molecular docking and Surface plasmon resonance (SPR) analysis revealed that Cry exhibits a remarkable affinity towards STAT3. In a rat model of IVDD induced by needling, treatment with Cry significantly ameliorated the progression of IVDD.

CONCLUSIONS:

To summarize, oxidative stress induced by lactate accumulation exhibits a strong correlation with the progression of IVDD. On this foundation, we obtained Cry by screening and demonstrated through mechanistic studies that it could attenuate lactate-induced injury to NPCs and thus improve IVDD, thus Cry may be a promising candidate for the treatment of IVDD.

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	South Korea	KT&G Life Sciences Corp.	-
Nonalcoholic Steatohepatitis	Phase 2	South Korea	KT&G Life Sciences Corp.	-
Obesity	Phase 2	South Korea	KT&G Life Sciences Corp.	-
Glioblastoma	Preclinical	China	Shanghai University of Traditional Chinese Medicine	01 Jul 2025
Glioblastoma	Preclinical	China	Shanghai Jiao Tong University School of Medicine	01 Jul 2025
Retinal Diseases	Preclinical	China	Jinan University	01 Jul 2025
Neoplasms	Preclinical	United States	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)	cugxvtybiw(bdykhhnczb) = odfuskgwaf kwobrkopva (arwtkrojrz )	-	13 Nov 2010
				Sodium nitroprusside (SNP)	cugxvtybiw(bdykhhnczb) = ebpgrrewux kwobrkopva (arwtkrojrz )