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2-methyl-5-hydroxy-1,4-naphthoquinone, 5-hydroxy-2-methyl-1,4-naphthoquinone, plumbagin

No.	Title	Href
1	Plumbagin Enhances the Anticancer Efficacy of Cisplatin by Increasing Intracellular ROS in Human Tongue Squamous Cell Carcinoma. Oxid Med Cell Longev. 2020 Mar 25;2020:5649174. doi: 10.1155/2020/5649174.	`Click`
2	Synergistic suppression of human breast cancer cells by combination of plumbagin and zoledronic acid In vitro. Acta Pharmacol Sin. 2015 Sep;36(9):1085-98. doi: 10.1038/aps.2015.42. Epub 2015 Aug 3. Erratum in: Acta Pharmacol Sin. 2019 Aug;40(8):1127-1128.	`Click`
3	Synergistic inhibitory effects of Celecoxib and Plumbagin on melanoma tumor growth. Cancer Lett. 2017 Jan 28;385:243-250. doi: 10.1016/j.canlet.2016.10.016.	`Click`
4	Plumbagin enhances TRAIL-induced apoptosis of human leukemic Kasumi‑1 cells through upregulation of TRAIL death receptor expression, activation of caspase-8 and inhibition of cFLIP. Oncol Rep. 2017;37(6):3423-3432. doi:10.3892/or.2017.5627	`Click`

No.

Title

Href

Plumbagin Enhances the Anticancer Efficacy of Cisplatin by Increasing Intracellular ROS in Human Tongue Squamous Cell Carcinoma. Oxid Med Cell Longev. 2020 Mar 25;2020:5649174. doi: 10.1155/2020/5649174.

Click

Synergistic suppression of human breast cancer cells by combination of plumbagin and zoledronic acid In vitro. Acta Pharmacol Sin. 2015 Sep;36(9):1085-98. doi: 10.1038/aps.2015.42. Epub 2015 Aug 3. Erratum in: Acta Pharmacol Sin. 2019 Aug;40(8):1127-1128.

Click

Synergistic inhibitory effects of Celecoxib and Plumbagin on melanoma tumor growth. Cancer Lett. 2017 Jan 28;385:243-250. doi: 10.1016/j.canlet.2016.10.016.

Click

Plumbagin enhances TRAIL-induced apoptosis of human leukemic Kasumi‑1 cells through upregulation of TRAIL death receptor expression, activation of caspase-8 and inhibition of cFLIP. Oncol Rep. 2017;37(6):3423-3432. doi:10.3892/or.2017.5627

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Name	Plumbagin
PubChem CID	10205
Molecular Weight	188.18g/mol
Synonyms	2-methyl-5-hydroxy-1,4-naphthoquinone, 5-hydroxy-2-methyl-1,4-naphthoquinone, plumbagin
Formula	C₁₁H₈O₃
SMILES	CC1=CC(=O)C2=C(C1=O)C=CC=C2O
InChI	1S/C11H8O3/c1-6-5-9(13)10-7(11(6)14)3-2-4-8(10)12/h2-5,12H,1H3
InChIKey	VCMMXZQDRFWYSE-UHFFFAOYSA-N
CAS Number	481-42-5
ChEMBL ID	CHEMBL295316
ChEBI ID	CHEBI:8273
Herb ID	HBIN040266
Drug Bank ID	DB17048
KEGG ID	C10387
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	BaiHuaDan
Use Part	Whole Grass, Root
Habitat	FuJian, TaiWan, GuangDong, GuangXi
Flavor	Pungent, Bitter

Chineses Pinyin	ZiJinLian
Use Part	Root
Habitat	GanSu, HeBei, ShanXi, JiangSu, ZheJiang, HeNan
Flavor	Pungent, Sweet
Meridian Tropism	Liver
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Caryophyllales 　　　　-->Family: Plumbaginaceae 　　　　　-->Genus: Ceratostigma 　　　　　　-->Species: Ceratostigma willmottianum

Chineses Pinyin	MaoGaoCai
Use Part	Whole Herb
Habitat	SiChuan, GuiZhou, YunNan, XiZang, JiangSu, ZheJiang, AnHui, FuJian, JiangXi, HuBei, HuNan, GuangDong, GuangXi, HaiNan, TaiWan
Flavor	Sweet, Pungent
Meridian Tropism	Spleen
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Caryophyllales 　　　　-->Family: Droseraceae 　　　　　-->Genus: Drosera 　　　　　　-->Species: Drosera peltata

Pair Name	Plumbagin, Cisplatin
Partner Name	Cisplatin
Disease Info	[ICD-11: 2B62.0]	Tongue squamous cell carcinoma		Investigative
Biological Phenomena	Induction-->ROS accumulation
Gene Regulation	Down-regulation	Expression	AKT1	hsa207
	Up-regulation	Activity	MAPK8	hsa5599
	Down-regulation	Expression	MTOR	hsa2475
	Up-regulation	Expression	ROS1	hsa6098
In Vitro Model	CAL-27	Tongue adenosquamous carcinoma	Homo sapiens (Human)	CVCL_1107
In Vivo Model	Each mouse was injected with 0.15 mL of cell suspension containing 1×10⁶ CAL27/CDDP cells into the right flanks.
Result	PLB combined with cisplatin is a potential therapeutic strategy against therapy TSCC cisplatin resistance.

Pair Name	Plumbagin, Zoledronic acid
Partner Name	Zoledronic acid
Disease Info	[ICD-11: 2C60]	Breast cancer		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	BCL2	hsa596
Gene Regulation	Up-regulation	Expression	NOTCH1	hsa4851
In Vitro Model	MDA-MB-231	Breast adenocarcinoma	Homo sapiens (Human)	CVCL_0062
Result	Combination of ZA and PL synergistically suppresses human breast cancer MDA-MB-231SArfp cells in vitro. PL can inhibit ZA-induced activation of the Notch-1 signaling pathway and subsequently reduce the expression of Bcl-2, thus potentiating cancer cell apoptosis.

Pair Name	Plumbagin, Celecoxib
Partner Name	Celecoxib
Disease Info	[ICD-11: 2C30]	Melanoma		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	COX2	hsa4513
Gene Regulation	Down-regulation	Expression	STAT3	hsa6774
In Vitro Model	UACC-903	Cutaneous melanoma	Homo sapiens (Human)	CVCL_4052
	Mel JuSo	Cutaneous melanoma	Homo sapiens (Human)	CVCL_1403
	A375-M	Amelanotic melanoma	Homo sapiens (Human)	CVCL_B222
	1205Lu	Cutaneous melanoma	Homo sapiens (Human)	CVCL_5239
In Vivo Model	Subcutaneous injection of 1.0×10⁶ UACC 903 or 1205 Lu melanoma cells were injected above both the left and right rib cages of 4-5 week-old female Athymic-Foxn1nu nude mice
Result	Combination of Celecoxib and Plumbagin decreased melanoma cell proliferation and retarded vascular development of tumors mediated by inhibition of COX-2 and STAT3 leading to decreased levels of key cyclins key on which melanoma cell were dependent for survival.

Pair Name	Plumbagin, rsTRAIL
Partner Name	rsTRAIL
Disease Info	[ICD-11: 2B33.4]	Leukemia		Investigative
Biological Phenomena	Induction-->ROS generation
Gene Regulation	Up-regulation	Expression	BAX	hsa581
	Down-regulation	Expression	BID	hsa637
	Up-regulation	Expression	CASP8	hsa841
	Down-regulation	Expression	CFLAR	hsa8837
	Up-regulation	Expression	TNFRSF10B	hsa8795
In Vitro Model	Kasumi-1	Childhood acute myeloid leukemia with maturation	Homo sapiens (Human)	CVCL_0589
In Vivo Model	Kasumi-1 cells were injected s.c. into the flanks of the mice (2.5×10⁶ in 2 ml) and tumors were allowed to develop for 18–30 days until they reached 50–100 mm3, then treatment was initiated.
Result	Our results suggest that both plumbagin and rsTRAIL could be used as a single agent or synergistical agents to induce apoptosis of leukemic Kasumi‑1 cells in vitro and in vivo.