InterPAD - DETAILS

artesunate, Dihydroartemisinin, Succinyl, Dihydroartemisinine 12 alpha succinate, dihydroartemisinine-12-alpha-succinate, Malacef, malartin, SM 804, SM-804, SM804, sodium artesunate, succinyl dihydroartemisinin

No.	Title	Href
1	DDInter: an online drug-drug interaction database towards improving clinical decision-making and patient safety. Nucleic Acids Res. 2022;50(D1):D1200-D1207. doi:10.1093/nar/gkab880	`Click`
2	Artesunate alleviates 5-fluorouracil-induced intestinal damage by suppressing cellular senescence and enhances its antitumor activity. Discov Oncol. 2023 Jul 27;14(1):139. doi: 10.1007/s12672-023-00747-7.	`Click`
3	Artesunate Regulates Neurite Outgrowth Inhibitor Protein B Receptor to Overcome Resistance to Sorafenib in Hepatocellular Carcinoma Cells. Front Pharmacol. 2021 Feb 25;12:615889. doi: 10.3389/fphar.2021.615889.	`Click`
4	Artesunate Exhibits Synergy With Cisplatin and Cytotoxicity for Upper Tract and Bladder Urothelial Carcinoma Cells. Anticancer Res. 2023 Mar;43(3):1175-1184. doi: 10.21873/anticanres.16263.	`Click`
5	Artesunate and cisplatin synergistically inhibit HNSCC cell growth and promote apoptosis with artesunate‑induced decreases in Rb and phosphorylated Rb levels. Oncol Rep. 2023 Aug;50(2):154. doi: 10.3892/or.2023.8591.	`Click`
6	Artesunate exhibits synergistic anti-cancer effects with cisplatin on lung cancer A549 cells by inhibiting MAPK pathway. Gene. 2021 Jan 15;766:145134. doi: 10.1016/j.gene.2020.145134.	`Click`
7	Artesunate Sensitizes human hepatocellular carcinoma to sorafenib via exacerbating AFAP1L2-SRC-FUNDC1 axis-dependent mitophagy. Autophagy. 2023 Sep 21:1-16. doi: 10.1080/15548627.2023.2261758.	`Click`
8	Artesunate synergistically promotes sorafenib‑induced apoptosis and ferroptosis in non‑Hodgkin lymphoma cells through inhibition of the STAT3 pathway. Oncol Rep. 2023 Jul;50(1):147. doi: 10.3892/or.2023.8584.	`Click`
9	Mesenchymal-epithelial transition and AXL inhibitor TP-0903 sensitise triple-negative breast cancer cells to the antimalarial compound, artesunate. Sci Rep. 2024 Jan 3;14(1):425. doi: 10.1038/s41598-023-50710-3.	`Click`
10	Lower dose of metformin combined with artesunate induced autophagy-dependent apoptosis of glioblastoma by activating ROS-AMPK-mTOR axis. Exp Cell Res. 2023 Sep 1;430(1):113691. doi: 10.1016/j.yexcr.2023.113691.	`Click`
11	Artesunate improves venetoclax plus cytarabine AML cell targeting by regulating the Noxa/Bim/Mcl-1/p-Chk1 axis. Cell Death Dis. 2022 Apr 20;13(4):379. doi: 10.1038/s41419-022-04810-z.	`Click`

No.

Title

Href

DDInter: an online drug-drug interaction database towards improving clinical decision-making and patient safety. Nucleic Acids Res. 2022;50(D1):D1200-D1207. doi:10.1093/nar/gkab880

Click

Artesunate alleviates 5-fluorouracil-induced intestinal damage by suppressing cellular senescence and enhances its antitumor activity. Discov Oncol. 2023 Jul 27;14(1):139. doi: 10.1007/s12672-023-00747-7.

Click

Artesunate Regulates Neurite Outgrowth Inhibitor Protein B Receptor to Overcome Resistance to Sorafenib in Hepatocellular Carcinoma Cells. Front Pharmacol. 2021 Feb 25;12:615889. doi: 10.3389/fphar.2021.615889.

Click

Artesunate Exhibits Synergy With Cisplatin and Cytotoxicity for Upper Tract and Bladder Urothelial Carcinoma Cells. Anticancer Res. 2023 Mar;43(3):1175-1184. doi: 10.21873/anticanres.16263.

Click

Artesunate and cisplatin synergistically inhibit HNSCC cell growth and promote apoptosis with artesunate‑induced decreases in Rb and phosphorylated Rb levels. Oncol Rep. 2023 Aug;50(2):154. doi: 10.3892/or.2023.8591.

Click

Artesunate exhibits synergistic anti-cancer effects with cisplatin on lung cancer A549 cells by inhibiting MAPK pathway. Gene. 2021 Jan 15;766:145134. doi: 10.1016/j.gene.2020.145134.

Click

Artesunate Sensitizes human hepatocellular carcinoma to sorafenib via exacerbating AFAP1L2-SRC-FUNDC1 axis-dependent mitophagy. Autophagy. 2023 Sep 21:1-16. doi: 10.1080/15548627.2023.2261758.

Click

Artesunate synergistically promotes sorafenib‑induced apoptosis and ferroptosis in non‑Hodgkin lymphoma cells through inhibition of the STAT3 pathway. Oncol Rep. 2023 Jul;50(1):147. doi: 10.3892/or.2023.8584.

Click

Mesenchymal-epithelial transition and AXL inhibitor TP-0903 sensitise triple-negative breast cancer cells to the antimalarial compound, artesunate. Sci Rep. 2024 Jan 3;14(1):425. doi: 10.1038/s41598-023-50710-3.

Click

Lower dose of metformin combined with artesunate induced autophagy-dependent apoptosis of glioblastoma by activating ROS-AMPK-mTOR axis. Exp Cell Res. 2023 Sep 1;430(1):113691. doi: 10.1016/j.yexcr.2023.113691.

Click

Artesunate improves venetoclax plus cytarabine AML cell targeting by regulating the Noxa/Bim/Mcl-1/p-Chk1 axis. Cell Death Dis. 2022 Apr 20;13(4):379. doi: 10.1038/s41419-022-04810-z.

Click

Name	Artesunate
PubChem CID	6917864
Molecular Weight	384.4g/mol
Synonyms	artesunate, Dihydroartemisinin, Succinyl, Dihydroartemisinine 12 alpha succinate, dihydroartemisinine-12-alpha-succinate, Malacef, malartin, SM 804, SM-804, SM804, sodium artesunate, succinyl dihydroartemisinin
Formula	C₁₉H₂₈O₈
SMILES	CC1CCC2C(C(OC3C24C1CCC(O3)(OO4)C)OC(=O)CCC(=O)O)C
InChI	1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1
InChIKey	FIHJKUPKCHIPAT-AHIGJZGOSA-N
CAS Number	88495-63-0
ChEMBL ID	CHEMBL361497
ChEBI ID	CHEBI:63918
Herb ID	HBIN016977
Drug Bank ID	DB09274
Toxicity	Organism	Test Type	Route(Dose)
	rat	LD50	intraperitoneal(165 mg/kg)
	mouse	LD50	intraperitoneal(254 mg/kg)
	rat	LD50	oral(322 mg/kg)
Structure			Download 2D MOL 3D MOL

Chineses Pinyin	QingHao
Use Part	Whole Grass
Habitat	China
Flavor	Bitter, Pungent
Meridian Tropism	Liver, Gallbladder
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Asterales 　　　　-->Family: Asteraceae 　　　　　-->Genus: Artemisia 　　　　　　-->Species: Artemisia annua

Chineses Pinyin	QINGHao
Use Part	Whole herb
Habitat	China
Flavor	Pungent; Bitter
Meridian Tropism	Liver; Gallbladder
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Asterales 　　　　-->Family: Asteraceae 　　　　　-->Genus: Artemisia 　　　　　　-->Species: Artemisia annua

Pair Name	Artesunate, Sorafenib
Partner Name	Sorafenib
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Gene Regulation	Down-regulation	Expression	NUS1	hsa116150
In Vitro Model	Hep-G2	Hepatoblastoma	Homo sapiens (Human)	CVCL_0027
Result	We report that sorafenib treatment in combination with artesunate overcomes HCC resistance to sorafenib alone in a cell culture model.

Pair Name	Artesunate, Cisplatin
Partner Name	Cisplatin
Disease Info	[ICD-11: 2C9Z]	Urothelial carcinoma		Investigative
Biological Phenomena	Induction-->Blockade of cell cycle in G2/M phase
In Vitro Model	HT-1376	Bladder carcinoma	Homo sapiens (Human)	CVCL_1292
In Vitro Model	BFTC-909	Renal pelvis urothelial carcinoma	Homo sapiens (Human)	CVCL_1084
Result	Artesunate Exhibits Synergy With Cisplatin and Cytotoxicity for Upper Tract and Bladder Urothelial Carcinoma Cells

Pair Name	Artesunate, TP-0903
Partner Name	TP-0903
Disease Info	[ICD-11: 2C60]	Breast cancer		Investigative
Biological Phenomena	Induction-->DNA damage and cell death
Gene Regulation	Up-regulation	Cleavage	CASP3	hsa836
	Up-regulation	Activity	CDH3	hsa1001
	Down-regulation	Expression	GPX8	hsa493869
	Up-regulation	Phosphorylation	H2AX	hsa3014
	Down-regulation	Expression	SOD2	hsa6648
	Down-regulation	Expression	ZEB1	hsa6935
In Vitro Model	MCF-7	Invasive breast carcinoma of no special type	Homo sapiens (Human)	CVCL_0031
	T-47D	Invasive breast carcinoma of no special type	Homo sapiens (Human)	CVCL_0553
	ZR-75-1	Invasive breast carcinoma of no special type	Homo sapiens (Human)	CVCL_0588
	SK-BR-3	Breast adenocarcinoma	Homo sapiens (Human)	CVCL_0033
	MDA-MB-231	Breast adenocarcinoma	Homo sapiens (Human)	CVCL_0062
	MDA-MB-436	Invasive breast carcinoma	Homo sapiens (Human)	CVCL_0623
	BT-549	Invasive breast carcinoma of no special type	Homo sapiens (Human)	CVCL_1092
	HBL-100	Healthy	Homo sapiens (Human)	CVCL_4362
	MCF-10A	Healthy	Homo sapiens (Human)	CVCL_0598
Result	Synergistic interactions between TP-0903 and ART indicate that combination approaches involving these compounds can have therapeutic prospects for TNBC treatment.

Pair Name	Artesunate, Metformin
Partner Name	Metformin
Disease Info	[ICD-11: 2A00]	Glioblastoma multiforme		Investigative
Biological Phenomena	Induction-->Autophagy
Gene Regulation	Up-regulation	Expression	CASP9	hsa842
	Down-regulation	Expression	MAP1LC3A	hsa84557
	Up-regulation	Expression	MAP1LC3B	hsa81631
	Down-regulation	Phosphorylation	MTOR	hsa2475
	Up-regulation	Phosphorylation	PRKAA1	hsa5562
	Down-regulation	Expression	SQSTM1	hsa8878
In Vitro Model	U-118MG	Astrocytoma	Homo sapiens (Human)	CVCL_0633
In Vitro Model	U-251MG	Astrocytoma	Homo sapiens (Human)	CVCL_0021
Result	The study findings suggest that MET used in combination with ART can induce autophagy-dependent apoptosis in GBM cells by activating the ROS-AMPK-mTOR pathway, providing a potential new treatment for GBM.

Pair Name	Artesunate, Venetoclax
Partner Name	Venetoclax
Disease Info	[ICD-11: 2A60.Z]	Acute myeloid leukemia		Investigative
Biological Phenomena	Induction-->DNA damage
Gene Regulation	Up-regulation	Expression	BCL2L11	KEGG ID N.A.
	Up-regulation	Cleavage	CASP3	hsa836
	Down-regulation	Phosphorylation	CHEK1	hsa1111
	Up-regulation	Expression	H2AX	hsa3014
	Down-regulation	Expression	MCL1	hsa4170
	Up-regulation	Cleavage	PARP1	hsa142
	Down-regulation	Expression	PMAIP1	hsa5366
In Vitro Model	THP-1	Childhood acute monocytic leukemia	Homo sapiens (Human)	CVCL_0006
In Vitro Model	MOLM-13	Adult acute myeloid leukemia	Homo sapiens (Human)	CVCL_2119
In Vivo Model	NOD/SCID mice (8 weeks) were injected with 5×10⁶ log-phase MOLM-13 cells subcutaneously in the right flank.
Result	We provide a new triple combination for AML treatment by targeting the Noxa/Mcl-1/Bim axis to reverse Mcl-1/p-Chk1 resistance of cytarabine therapy.

Pair Name	Artesunate, Fluorouracil
Partner Name	Fluorouracil
Disease Info	[ICD-11: 2B91]	Colorectal cancer		Investigative
Biological Phenomena	Induction-->Cell senescence
Gene Regulation	Down-regulation	Expression	CDKN1A	hsa1026
	Down-regulation	Expression	CDKN2A	hsa1029
	Down-regulation	Phosphorylation	MAPK14	hsa1432
	Down-regulation	Phosphorylation	MTOR	hsa2475
	Down-regulation	Phosphorylation	PRKAA1	hsa5562
	Down-regulation	Phosphorylation	RELA	hsa5970
	Down-regulation	Expression	TP53	hsa7157
In Vitro Model	HCT 116	Colon carcinoma	Homo sapiens (Human)	CVCL_0291
In Vitro Model	HIEC-6	Healthy	Homo sapiens (Human)	CVCL_6C21
In Vivo Model	HCT116 cells (1×10⁷) were subcutaneously inoculated into the left thigh dorsal region of nude mice, and tumor size was measured every 2 days for xenograft model establishment.
Result	Our findings point to the crucial treatment effect of Arte on inflammation, intestinal cell senescence, and CRC cell proliferation and offer a new option for CRC treatment.

Pair Name	Artesunate, Nevirapine
Partner Name	Nevirapine
Result	Coadministration with nevirapine may decrease the peak plasma concentration (Cmax) and systemic exposure (AUC) of dihydroartemisinin (DHA), an active metabolite of artesunate. The mechanism is unknown. Reduced efficacy of artesunate may occur.