Radix Bupleuri: A Review of Traditional Uses, Botany, Phytochemistry, Pharmacology, and Toxicology

Table 3

Pharmacological effects of Radix Bupleuri.

Pharmacological effects	Cell lines/model	Detail/mechanism(s) of action	Preparations/extracts/compounds	Application	Reference
Anti-inflammatory effect	LPS-induced mouse acute lung injury	Increases levels of MPO and TNF-α; Inhibits the No level	Crude polysaccharides	In vivo	[66]
	Formalin-induced mice paw edema	Regulates the nicotinate and nicotinamide metabolism and arachidonic acid metabolism	Saikosaponins	In vivo	[5]
	LPS-stimulated RAW 264.7 cells	Regulates MAPK and NF-κB signals pathways	Saikosaponin a	In vitro	[68]
	LPS-stimulated human umbilical endothelial cells	Activates the LXRα-ABCA1 signaling pathway	Saikosaponin a	In vitro	[69]
	Septic rats model	Inhibits the nucleotide-binding oligomerization domain 2 (NOD2)/NF-κB signaling pathway	Saikosaponin a	In vivo	[70]
	LPS-induced apoptosis in human umbilical vein endothelial cells	Inhibits the caspase-3 activation and caspase-3-mediated-FAK degradation	Saikosaponin c	In vitro	[71]
	C6 rat glioma cells	Inhibits PGE2 production and elevates intracellular free Ca^2+ concentration	Saikosaponin d	In vitro	[72]
	Monoclonal antibody induced nephritis	Suppresses proteinuria, proliferation of mesangial cells, and expansion of the mesangial matrix	Saikosaponin d	In vivo	[73]
	Chronic pancreatitis rats model	Inhibits the expression of NF-κB and TNF-α mRNA	Chai-hu-shu-gan powder	In vivo	[74]
	LPS-stimulated rat aorta and Raw 264.7 macrophages	Inhibits the NO production and iNOS protein expression	RCM-101	In vivo/in vitro	[76]
Anticancer effect	A549 human lung cancer cells	Suppresses telomerase activity and activates ERK 1/2 and caspase-3/9	Acetone extracts	In vitro	[77–79]
	Human non-small-cell lung cancer A549 cells	Regulates Fas-dependent apoptotic pathway	Saponins	In vitro	[80]
	HepG2 hepatoma cells	Induces cell arrest at the late G1/early S phase	Water extracts	In vitro	[6]
	HepG2 cell line	Activates caspase-3 and caspase-7	Saikosaponin d	In vitro	[81]
	SMMC-7721 cell line	Regulates the HIF-1α/COX-2 pathway	Saikosaponin d	In vitro	[82]
	HeLa and MCF-7 cancer cells	Inhibits the SERCA; Activates the CaMKKβ-AMP-AMPK-mTOR signaling cascade, ER stress and UPR	Saikosaponin d	In vitro	[43]
Antiviral effect	H1N1-infected A549 cells	Anti-H1N1 virus	Acetone extracts	In vitro	[10]
	HBV-transfected human hepatoma cells	Inhibits DNA expression of HBsAg, HBeAg, and HBV	Saikosaponin c	In vitro	[81]
	HBV-transfected human hepatoma cells	Inhibits the production of HBV and the expression of HBeAg	Crude saponins	In vitro	[87]
	HBV-transfected human hepatoma cells	Inhibits DNA replication of HBV	MeOH extracts	In vitro	[88]
	Human coronavirus-229E	Interferes with the early stage of viral replication	Saikosaponins	In vitro	[89]
Antipyretic effect	Dry yeast-induced high fever rats	Adjusts the synthesis and exudation of cAMP and AVP	Water extracts	In vivo	[90]
	Turpentine-induced fever rabbits	Decreases body temperature	The essential oil	In vivo	[91]
	Turpentine-induced fever rabbits and rats	Decreases body temperature	The essential oil	In vivo	[92]
Antibacterial effect	Helicobacter pylori strain	Anti-Helicobacter pylori	Ethanol extracts	In vitro	[93]
	Staphylococcus aureus strain	Anti-Staphylococcus aureus	Chaihu injection	In vitro	[95]
	Pseudomonas aeruginosa, Listeria monocytogenes strains	Anti-Pseudomonas aeruginosa, Anti-Listeria monocytogenes	Saikosaponins	In vitro	[94]
Hepatoprotective effect	CCl4 induced hepatic damage in rats	Hepatoprotective effects	Methanol extracts	In vivo	[96]
	D-galactosamine-induced hepatic injury in rats	Decreases the activity of glucose-6-phosphatase and NADPH-cytochrome C reductase; increases 5′-nucleotidase activity	Saikosaponins	In vivo	[97]
	D-galactosamine-induced cytotoxicity in rat hepatocytes	Hepatoprotective effects	Bupleurosides III, VI, IX, and XIII; saikosaponin b3	In vitro	[98]
	BEL-7402 cells	Regulates intracellular calcium levels	Saikosaponins	In vitro	[99]
	CCl4 induced acute hepatic injury in rats	Hepatoprotective effects	Saikosaponin d	In vivo	[100]
	CR-1548 cell; liver fibrosis in rats	Reduces lipid peroxidation	Saikosaponin d	In vitro/in vivo	[101]
Immunomodulatory effect	Rats fed with Radix Bupleuri	Increases the amplitude of spontaneous activity of lymphatic vessels	Water extracts	In vivo	[102]
	Human peripheral blood T cells	Inhibits CD28-costimulated activation	MeOH extracts	In vitro	[62]
	BALB/c, C3H/He and CDF1 mice	Stimulates T and B cells	Saikosaponin d	In vivo	[103]
	Thymocytes and spleen cells; C57BL/6 mice	Regulates receptor-bypassed pathway	Saikosaponin d	In vitro/in vivo	[41, 104, 105]
Others	Male SD rats	Exhibits strong induction activity on the CYP2E1, CYP2D6, and CYP3A4	Ethanol extracts	In vivo	[107]
	PTZ-induced epilepsy rats model	Inhibits mTOR signaling pathway	Saikosaponin a	In vivo	[109]
	THP-1 Cells	Inhibits PI3K/Akt/NF-κB/NLRP3 signaling pathway	Saikosaponin a	In vitro	[110]
	Human umbilical vein endothelial cells	Activates MMP-2, VEGF, and the p42/p44 mitogen-activated protein kinase	Saikosaponin c	In vitro	[111]
	SH-SY5Y and SK-N-SH cell lines	Suppresses the secretion of Aβ peptides	Saikosaponin c	In vitro	[112]
	Male Wistar rats	Increases the level of 5-HT and NE	Polyacetylenes	In vivo	[56]
	Dactylogyrus spp. infecting goldfish	Anthelmintic activity	Saikosaponins a and d	In vivo	[113]