Exploration of Drug Science

Table 2

Health benefits of psoralidin and key molecular targets

Biological effect	Psoralidin source	In vitro/in vivo	Study model	Drug concentration	Test/Assay	Molecular targets	References
Anti-bacterial	Seed extract	In vivo	Shigella sonnei, Shigella flexneri	200 µg/disc	Disc diffusion method	NA	[69]
Anti-bacterial	Hexane extract from seeds	In vivo	Escherichia coli, Staphylococcus aureus	90–150 µg/mL	Inhibition assay	NA	[76]
Anti-diabetic	Ethanolic extract from seeds	In vitro	NA	10 µM	PTP1B, VHR, PPase1	↓Tyrosine phosphatase 1B	[70]
Anti-inflammatory	Methanolic extract from seeds	In vitro	RBL-2H3	30–100 µM	β-hexosaminidase bioassay	↓Hexosaminidase release	[77]
	Methanolic extract from seeds	In vitro	Mice peritoneal exudate cells	29 µM	NO production Assay	↓NO	[78]
	Commercial	In vitro, In vivo	HFL-1, MRC-5, BALB/c mice	50–100 µM	Luciferase reporter gene assay, ITc assay	↓COX-2, PGE2 ↓PI3K/Akt, NF-кB ↓LTB4 ↑TNF-α, TGF-β, IL-6, IL-1α/β	[79]
	Methanolic extract from seeds	In vitro	RAW 264.7	1–30 µM	-	↓PI3K/Akt ↓iNOS	[80]
	Commercial	In vivo	Osteoarthritic chondrocytic pellet cultures	1–50 µM	Biochemical, Immunological, Histological analysis	↑Cartilaginous matrix ↑GAG/DNA ratio ↓MMP13, MMP1, MMP3	[81]
	Ethanolic extract from roots	In vitro	RAW 264.7	20 µM	NO production assay, α-glucosidase inhibitor assay	↓α-glucosidase	[82]
Anti-depressant	Seed	In vivo	ICR mice	20–60 mg/kg	Forced Swimming Test, Open Field Test	↑Swimming behaviour ↑5-HIAA, DA ↓CRF, ACTH, corticosterone	[83]
Anti-depressant	Seed	In vitro	N2A	160 µM	CRF promoter activity assay	↓CRF promoter acitivity ↓ CRF transcription	[84]
SARS-CoV	Ethanolic extract from seeds	In vivo	E. coli	NA	PLpro inhibition assay	↓PLpro	[85]
SARS-CoV	NA	In silico	NA	NA	Molecular Docking	↓Furin	[86]
Anti-protozoal	Methanolic extract from fruits	In vivo	Ichthyophthirius multifiliis	1 mg/L	Efficacy assay	↓Theronts number	[87]
Neuroprotective	Ethanolic extract from seeds	In vitro	BV-2, HT22	1.25–5 µM	CCK assay	↓NO	[88]
Neuroprotective	Commercial	In vivo	Cerebral cortices and hippocampi from ICR mice	1–20 µM	PSD 95/VGLUT1-positive clusters quantification	↑Arc, Egr1, c-fos ↑p-ERK1/2 ↑PSD 95/VGLUT1-cluster	[89]
Vasodilatory	Ethanolic extract from seeds	In vivo	Sprague Dawley rats, HEK293	NA	Electrophysiology	Aortic ring relaxation ↓hTRPC3 current	[90]
Osteoprotective	Commercial	In vitro	Rat calvarial osteoblasts	1 µM	ALP and TRAP activity	↑Osterix, Runx-2, IGF-1, β-catenin OPG ↓RANKL ↓TRAP	[91]
	Commercial	In vitro, In vivo	Bone marrow macrophages, ICR mice	1–50 µM 5–50 mg/Kg	TRAP assay, Bone absorption assay, F-actin labelling	↓TRAP-positive cells ↓F-actin ring formation ↓p-P38, p-JNK, p-ERK1/2, RANKL	[92]
	Ethyl-acetate extract from seeds	In vitro, In vivo	BMSCs, Sprague Dawley rats	10 mg/kg	DEXA, MicroCT, TRAP, ORO staining	↓TRAP ↑p-PI3K, p-Akt ↑HO-1	[93]
	Commercial	In vitro	Rat chondrocytes	1–20 µM	Caspase-3 and Caspase-9 activity assay, NO assay	↑Bcl-2 ↓Bax ↓NF-кB nuclear localization	[94]
	Commercial	In vitro	BMSCs, MC3T3-E1, 3T3-L1	0.001–20 µM	ALP, ORO staining	↑ALP ↑BSP, OCN ↓PPAR δ, CEBPα, LPL, Fabp4	[95]
	Commercial	In vitro, In vivo	BMSCs, C57BL/6J mice	1–10 µM 10 mg/kg	ARS, ALP, and ORO staining, MicroCT	↑Runx-2, Osterix, OCN ↓PPAR γ, Fabp4, LPL	[96]
Anti-vitiligo	Ethanolic extract from whole plant	In vitro	NA	NA	HPLC, tyrosinase activity	↑Tyrosinase	[64]
Psoriasis	Ethanolic extract from seeds	In vivo	Pigs and mice	NA	H&E staining	No effect	[97]
Cardioprotective	Commercial	In vivo, In vitro	BALB/c mice, HL-1	25 mg/kg 20–100 µM	Echocardiography evaluation, LDH release assessment	↓CK, AST, BUN ↑ALB ↓ROS, LDH	[98]
Anti-fungal	Hexane extract from seeds	In vivo	Candida albicans, Trichophyton rubrum	160–180 µg/mL	Inhibition assay	NA	[76]
Anti-septic	Ethanolic extract	In vivo	CLP-injured mice	50 mg/kg	Sepsis score analysis	↓Sepsis score ↓LDH, AST, BUN, CK ↑ALB ↑WBC, LYM, MID, GRA, PLT	[99]

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ACTH: adrenocorticotropic hormone; ALB: albumin; ALP: alkaline phosphatase; Arc: activity-dependent cytoskeleton associated protein; AST: aspartate aminotransferase; Bax: B-cell leukemia/lymphoma 2 protein associated X protein; Bcl-2: B-cell leukemia/lymphoma 2 protein; BMSCs: bone marrow mesenchymal stem cells; BSP: bone sialoprotein; BUN: blood urea nitrogen; CCK: cholecystokinin; CEBPα: CAAT/enhancer binding protein alpha; c-fos: fos proto-oncogene; CK: creatine kinase; CLP: cecal ligation and puncture; COX-2: cyclooxygenase-2; CRF: corticotropin releasing factor; DA: dopamine; Egr1: early growth response protein 1; Fabp4: fatty acid-binding protein 4; GRA: glucocorticoid receptor agonists; HEK: human embryonic kidney; 5-HIAA: 5-hydroxy indoleacetic acid; HO-1: heme oxygenase-1; IGF-1: insulin-like growth factor 1; iNOS: inducible nitric oxide synthase; p-JNK: phosphorylated c-Jun N-terminal kinase; LDH: lactate dehydrogenase; LPL: lipoprotein lipase; LYM: lymphocyte; NO: nitric oxide; OCN: osteocalcin; OPG: osteoprotegerin; p-Akt: phosphorylated protein kinase B; p-ERK1/2: phosphorylated extracellular signal-regulated kinase 1/2; p-PI3K: phosphorylated-phosphatidylinositol 3-kinase; PLpro: papain-like protease; PLT: platelet count; PPAR δ: peroxisome proliferator activated receptor delta; PSD 95: post-synaptic density 95; PTP1B: protein tyrosine phosphatase 1B; RANKL: receptor activator of nuclear factor kappa-B ligand; ROS: reactive oxygen species; Runx-2: runt-related transcription factor 2; SARS-CoV: severe acute respiratory syndrome coronavirus; TNF-α: tumor necrosis factor alpha; TRAP: tartrate-resistant acid phosphatase; VGLUT1: vesicular glutamate transporter 1; WBC: white blood cell; NA: not available