InterPAD - DETAILS

lasidonin, oridonin, oridonin, (1alpha,5alpha,6alpha,7beta,8beta,9alpha,10beta,13beta,14S)-isomer, oridonin, (1alpha,6beta,7alpha,11alpha)-isomer, oridonin, (1alpha,6beta,7alpha,11beta)-isomer

No.	Title	Href
1	Oridonin enhances antitumor effects of doxorubicin in human osteosarcoma cellsOridonin enhances antitumor effects of doxorubicin in human osteosarcoma cells. Pharmacol Rep. 2022 Feb;74(1):248-256. doi: 10.1007/s43440-021-00324-1.	`Click`
2	Oridonin synergistically enhances the anti-tumor efficacy of doxorubicin against aggressive breast cancer via pro-apoptotic and anti-angiogenic effects. Pharmacol Res. 2019 Aug;146:104313. doi: 10.1016/j.phrs.2019.104313.	`Click`
3	Oridonin enhances the cytotoxicity of 5-FU in renal carcinoma cells by inducting necroptotic death. Biomed Pharmacother. 2018 Oct;106:175-182. doi: 10.1016/j.biopha.2018.06.111.	`Click`
4	Selective synergistic anticancer effects of cisplatin and oridonin against human p53-mutant esophageal squamous carcinoma cells. Anticancer Drugs. 2022 Jan 1;33(1):e444-e452. doi: 10.1097/CAD.0000000000001237.	`Click`
5	Combined oridonin with cetuximab treatment shows synergistic anticancer effects on laryngeal squamous cell carcinoma: involvement of inhibition of EGFR and activation of reactive oxygen species-mediated JNK pathway. Int J Oncol. 2016 Nov;49(5):2075-2087. doi: 10.3892/ijo.2016.3696.	`Click`
6	Synergistic antitumor activity of oridonin and arsenic trioxide on hepatocellular carcinoma cells. Int J Oncol. 2012;40(1):139-147. doi:10.3892/ijo.2011.1210	`Click`
7	Oridonin in combination with imatinib exerts synergetic anti-leukemia effect in Ph+ acute lymphoblastic leukemia cells in vitro by inhibiting activation of LYN/mTOR signaling pathway. Cancer Biol Ther. 2012 Nov;13(13):1244-54. doi: 10.4161/cbt.21460.	`Click`
8	Oridonin Synergistically Enhances the Pro-Apoptotic Effect of Venetoclax on Acute Myeloid Leukemia Cells by Inhibiting AKT Signaling. Front Biosci (Landmark Ed). 2023 Sep 6;28(9):195. doi: 10.31083/j.fbl2809195.	`Click`

No.

Title

Href

Oridonin enhances antitumor effects of doxorubicin in human osteosarcoma cellsOridonin enhances antitumor effects of doxorubicin in human osteosarcoma cells. Pharmacol Rep. 2022 Feb;74(1):248-256. doi: 10.1007/s43440-021-00324-1.

Click

Oridonin synergistically enhances the anti-tumor efficacy of doxorubicin against aggressive breast cancer via pro-apoptotic and anti-angiogenic effects. Pharmacol Res. 2019 Aug;146:104313. doi: 10.1016/j.phrs.2019.104313.

Click

Oridonin enhances the cytotoxicity of 5-FU in renal carcinoma cells by inducting necroptotic death. Biomed Pharmacother. 2018 Oct;106:175-182. doi: 10.1016/j.biopha.2018.06.111.

Click

Selective synergistic anticancer effects of cisplatin and oridonin against human p53-mutant esophageal squamous carcinoma cells. Anticancer Drugs. 2022 Jan 1;33(1):e444-e452. doi: 10.1097/CAD.0000000000001237.

Click

Combined oridonin with cetuximab treatment shows synergistic anticancer effects on laryngeal squamous cell carcinoma: involvement of inhibition of EGFR and activation of reactive oxygen species-mediated JNK pathway. Int J Oncol. 2016 Nov;49(5):2075-2087. doi: 10.3892/ijo.2016.3696.

Click

Synergistic antitumor activity of oridonin and arsenic trioxide on hepatocellular carcinoma cells. Int J Oncol. 2012;40(1):139-147. doi:10.3892/ijo.2011.1210

Click

Oridonin in combination with imatinib exerts synergetic anti-leukemia effect in Ph+ acute lymphoblastic leukemia cells in vitro by inhibiting activation of LYN/mTOR signaling pathway. Cancer Biol Ther. 2012 Nov;13(13):1244-54. doi: 10.4161/cbt.21460.

Click

Oridonin Synergistically Enhances the Pro-Apoptotic Effect of Venetoclax on Acute Myeloid Leukemia Cells by Inhibiting AKT Signaling. Front Biosci (Landmark Ed). 2023 Sep 6;28(9):195. doi: 10.31083/j.fbl2809195.

Click

Name	Oridonin
PubChem CID	5321010
Molecular Weight	364.4g/mol
Synonyms	lasidonin, oridonin, oridonin, (1alpha,5alpha,6alpha,7beta,8beta,9alpha,10beta,13beta,14S)-isomer, oridonin, (1alpha,6beta,7alpha,11alpha)-isomer, oridonin, (1alpha,6beta,7alpha,11beta)-isomer
Formula	C₂₀H₂₈O₆
SMILES	CC1(CCC(C23C1C(C(C45C2CCC(C4O)C(=C)C5=O)(OC3)O)O)O)C
InChI	1S/C20H28O6/c1-9-10-4-5-11-18-8-26-20(25,19(11,14(9)22)15(10)23)16(24)13(18)17(2,3)7-6-12(18)21/h10-13,15-16,21,23-25H,1,4-8H2,2-3H3/t10-,11-,12-,13+,15+,16-,18+,19-,20+/m0/s1
InChIKey	SDHTXBWLVGWJFT-XKCURVIJSA-N
CAS Number	28957-04-2
ChEMBL ID	CHEMBL1164920
ChEBI ID	CHEBI:138236
Herb ID	HBIN038254
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	DongLingCao
Use Part	Whole Grass
Habitat	HeNan, HeBei, ShanXi, GanSu, SiChuan, GuiZhou, HuNan, HuBei, GuangXi, GuangDong, JiangXi, AnHui, ZheJiang
Flavor	Bitter, Sweet
Meridian Tropism	Lung, Stomach, Liver

Chineses Pinyin	LuShanXiangChaCai
Habitat	JiangSu, AnHui, ZheJiang, JiangXi, FuJian, TaiWan, HuBei, GuangDong, GuangXi, GuiZhou
Flavor	Pungent, Bitter
Meridian Tropism	Liver, Kidney

Chineses Pinyin	MaoYeXiangChaCai
Use Part	Leaf
Habitat	JiangSu, HeNan, SiChuan, GuiZhou, YunNan, XiZang, ChongQing, GanSu
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Lamiales 　　　　-->Family: Lamiaceae 　　　　　-->Genus: Isodon 　　　　　　-->Species: Isodon japonicus

Chineses Pinyin	XianMaiXiangChaCai
Use Part	Whole Herb
Habitat	Shaanxi, HeNan, HuBei, JiangSu, ZheJiang, AnHui, JiangXi, GuangDong, GuangXi, GuiZhou, SiChuan
Flavor	Mildly pungent, Bitter

Chineses Pinyin	ZhouYeXiangChaCai
Use Part	Leaf
Habitat	XiZang, SiChuan, YunNan, Shaanxi, GanSu, QingHai, NingXia, XinJiang

Pair Name	Oridonin, Fluorouracil
Partner Name	Fluorouracil
Disease Info	[ICD-11: 2C90.Z]	Renal carcinoma		Investigative
Biological Phenomena	Induction-->Necroptosis
Gene Regulation	Up-regulation	Activity	MAPK1	hsa5594
	Up-regulation	Activity	MAPK14	hsa1432
	Up-regulation	Activity	MAPK8	hsa5599
In Vitro Model	786-O	Renal cell carcinoma	Homo sapiens (Human)	CVCL_1051
In Vivo Model	786-O cells (1×10⁶) were subcutaneously injected into the right flank.
Result	Oridonin enhances the cytotoxicity of 5-FU in renal cancer cells partially through inducing necroptosis, providing evidence of using necroptosis inducers in combination with chemotherapeutic agents for cancer treatment.

Pair Name	Oridonin, Cisplatin
Partner Name	Cisplatin
Disease Info	[ICD-11: 2B70]	Esophageal cancer		Investigative
Biological Phenomena	Induction-->DNA damage
Gene Regulation	Down-regulation	Expression	GSH	KEGG ID N.A.
	Up-regulation	Expression	H2AX	hsa3014
	Down-regulation	Expression	RAD51	hsa5888
	Up-regulation	Expression	ROS1	hsa6098
In Vitro Model	KYSE-30	Esophageal squamous cell carcinoma	Homo sapiens (Human)	CVCL_1351
Result	These results suggest that ORI can synergistically enhance the effect of CIS, and GSH deficiency and p53 mutation, might be biomarkers for the combinational usage of ORI and CIS.

Pair Name	Oridonin, Cetuximab
Partner Name	Cetuximab
Disease Info	[ICD-11: 2C23.Z]	Laryngeal cancer		Investigative
Biological Phenomena	Induction-->Blockade of cell cycle in G2/M phase
Gene Regulation	Down-regulation	Phosphorylation	EGFR	hsa1956
	Down-regulation	Expression	FAS	hsa355
	Up-regulation	Expression	MAPK8	hsa5599
	Down-regulation	Expression	ROS1	hsa6098
In Vitro Model	HEp-2	Human papillomavirus-related cervical adenocarcinoma	Homo sapiens (Human)	CVCL_1906
In Vitro Model	Tu 212	Head and neck squamous cell carcinoma	Homo sapiens (Human)	CVCL_4915
In Vivo Model	Logarithmically growing HEp-2 cells were harvested by trypsinization, and each mouse was given injections of 1×10⁶ cells subcutaneously into the right flank.
Result	Combined oridonin with cetuximab treatment shows synergistic anticancer effects on laryngeal squamous cell carcinoma: Involvement of inhibition of EGFR and activation of reactive oxygen species-mediated JNK pathway

Pair Name	Oridonin, Arsenic oxide (As2O3)
Partner Name	Arsenic oxide (As2O3)
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	AKT1	hsa207
	Down-regulation	Activity	NFKB1	hsa4790
	Down-regulation	Expression	XIAP	hsa331
In Vivo Model	The two drug combination enhanced tumor suppression activity in murine HCC model compared with single agent treatment in vivo.
Result	The combination treatment induced ROS-dependent decrease in mitochondrial membrane potential (MMP) decrease, and relocation of Bax and cytochrome C. Besides, oridonin dramatically increased the intracellular Ca2+ overload triggered by As2O3. Furthermore, the co-treatment of oridonin and As2O3 induced ROS-mediated down-regulation of Akt and XIAP, and inhibition of NF-κB activation. The two drug combination enhanced tumor suppression activity in murine HCC model compared with single agent treatment in vivo.

Pair Name	Oridonin, Imatinib
Partner Name	Imatinib
Disease Info	[ICD-11: 2B33.3]	Acute lymphoblastic leukemia		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	AKT1	hsa207
	Up-regulation	Expression	BAX	hsa581
	Up-regulation	Expression	BCL2	hsa596
	Down-regulation	Expression	JTK8	hsa4067
	Down-regulation	Expression	MEK1	hsa5604
	Down-regulation	Expression	MTOR	hsa2475
	Down-regulation	Expression	RAF1	hsa5894
	Down-regulation	Expression	STAT5B	hsa6777
In Vitro Model	SUP-B15	Childhood B acute lymphoblastic leukemia with t	Homo sapiens (Human)	CVCL_0103
Result	Our data showed that oridonin remarkably suppressed activations of Akt/mTOR, Raf/MEK and STAT5 pathway in these primary specimens and oridonin with imatinib exerted synergetic suppressive effects on mTOR, STAT5 and LYN signaling in one imatinib resistant patient specimen. Additional evaluation of oridonin as a potential therapeutic agent for Ph+ ALL seems warranted.

Pair Name	Oridonin, Venetoclax
Partner Name	Venetoclax
Disease Info	[ICD-11: 2A60.Z]	Acute myeloid leukemia		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Phosphorylation	AKT1	hsa207
	Down-regulation	Expression	BAD	hsa572
	Up-regulation	Expression	BAX	hsa581
	Down-regulation	Expression	BCL-xL	hsa598
	Up-regulation	Expression	BIM	hsa10018
	Up-regulation	Cleavage	CASP3	hsa836
	Down-regulation	Expression	CCND1	hsa595
	Down-regulation	Phosphorylation	CDK2	hsa1017
	Up-regulation	Expression	CDKN1A	hsa1026
	Down-regulation	Phosphorylation	GSK3B	hsa2932
	Up-regulation	Expression	H2AX	hsa3014
	Down-regulation	Expression	MCL1	hsa4170
	Down-regulation	Expression	MDM2	hsa4193
	Down-regulation	Expression	MYC	hsa4609
	Up-regulation	Cleavage	PARP1	hsa142
	Up-regulation	Expression	TP53	hsa7157
In Vitro Model	MOLM-13	Adult acute myeloid leukemia	Homo sapiens (Human)	CVCL_2119
	OCI-AML-3	Adult acute myeloid leukemia	Homo sapiens (Human)	CVCL_1844
	U-937	Adult acute monocytic leukemia	Homo sapiens (Human)	CVCL_0007
	THP-1	Childhood acute monocytic leukemia	Homo sapiens (Human)	CVCL_0006
In Vivo Model	5×10⁶ OCI-AML3 cells stably expressing luciferase were injected into the tail vein of NTG mice, and in vivo imaging was performed on the fourth day to confirm successful establishment of the AML xenografts.
Result	Oridonin and venetoclax synergistically promote AML cell apoptosis by inhibiting AKT signaling.

Pair Name	Oridonin, Doxorubicin
Partner Name	Doxorubicin
Disease Info	[ICD-11: 2B51]	Osteosarcoma		Investigative
Biological Phenomena	Induction-->ROS generation
Gene Regulation	Up-regulation	Expression	ROS1	hsa6098
In Vitro Model	SaOS-2	Osteosarcoma	Homo sapiens (Human)	CVCL_0548
Result	The combined use of oridonin and doxorubicin could help to reduce the clinical dosage of doxorubicin and its dangerous side effects.

Pair Name	Oridonin, Doxorubicin
Partner Name	Doxorubicin
Disease Info	[ICD-11: 2C60]	Breast cancer		Investigative
Biological Phenomena	Inhibition-->Angiogenesis
Gene Regulation	Down-regulation	Expression	KDR	hsa3791
In Vitro Model	MDA-MB-231	Breast adenocarcinoma	Homo sapiens (Human)	CVCL_0062
In Vivo Model	A breast tumor xenograft model was established via subcutaneous flank inoculation of BALB/c female nude mice with 1×10⁶ MDA-MB-231 cells in 100 μl PBS containing 50% Matrigel per mouse.
Result	Our findings provide strong evidence that Ori may be highly promising in enhancing the efficacy of Dox and decreasing its adverse cardiotoxic effects, thus suggesting that Ori may serve as a potential adjunct therapy during Dox-based chemotherapy.