P-glycoprotein (ABCB1) and Oxidative Stress: Focus on Alzheimer’s Disease

Table 1

Summary of (a) in vitro and (b) in vivo studies and (c) clinical trials on neuroprotective activity of compounds that targeted Aβ transport across the blood-brain barrier mediated by ABCB1.

(a) In vitro

Treatment	Dose	Duration	Cell line	Species	Reference
Sulforaphane (SFN)	0.01–5 μM	0–200 min	Brain capillaries	Nrf2^−/− mouse	[108]
				p53^−/− mouse
Oleocanthal (Oleo)	0.5–50 μM	72 h	bEnd3	Mouse	[141]
1α,25-Dihydroxyvitamin D3 (1,25(OH)2D3)	1–100 nM	4 h or 24 h	Brain capillaries	Rat	[145]
		1–3 days	RBE4	Rat
			hCMEC/D3	Human
Fascalpsyn	1–100 μM	24–48 h	LS-180	Human	[147]
			hGF

(b) In vivo

Treatment	Dose	Duration	Model	Species	Reference
SFN	1–10 mg/kg intraperitoneal (i.p.)	2 days	Sprague-Dawley	Rat	[108]
Verapamil	2–5 mg/kg i.p.	21 days	Streptozocin-induced sporadic dementia	Rat	[136]
Berberine	25–100 mg/kg per oral (p.o.)	21 days
α-Tocopherol	36 mg/kg p.o.	Lifespan	Ttpa^−/− APPsw	Mouse	[138]
Pregnenolone-16α-carbonitrile	25 mg/kg i.p.	7 days	APPsw/Tg2576	Mouse	[114]
Oleo	10 mg/kg/12 h i.p.	2 weeks	C57BL/6	Mouse	[141]
Oleo	5 mg/kg/die i.p.	4 weeks	TgSwDI	Mouse	[142]
St. John’s wort	1250 mg/kg/die p.o.	60–120 days	APP/PS^+/−	Mouse	[143]
1,25(OH)2D3	2.5 μg/kg/die i.p.	8 days	Fxr^−/−	Mouse	[144]
1,25(OH)2D3	2.5 μg/kg/48 h i.p.	8 days	Tg2576	Mouse	[146]
			TgCRND8
Rivastigmine	0.3 mg/kg/day alzet pump	8 weeks	APP^+/mdr1	Mouse	[148]

(c) Clinical trials

Treatment	Dose	Duration	Diagnosis	Reference
Rifampin	300 mg/die p.o.	12 months	AD	[140]
Doxycyclin	200 mg/die p.o.