Table 3.

Major Phytochemicals in Cassia obtusifolia and their pharmacological activities.

Compounds	Biological Activity	In Vivo/ In Vitro	Model	Administration (In Vivo)	Dose Range	Active Concentration	Reference
Anthraquinones
Emodin	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 9.17µg/mL (b) IC50 = 157 µg/mL (c) IC50 = 4.48 µg/mL	[10]
	Antimicrobial activity	In vitro	Antibacterial activity against (a) Staphylococcus aureus 209P (b) Escherichia coli NIHJ	-	0–1 mg/mL	MIC (a) 4.5 µg/mL (b) 25 µg/mL	[46]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity (c) Stimulation of glucose uptake in HepG2 cells	-	(a) 0–100 µg/mL (b) 0–400 µg/mL (c) 3.12–12.5 µM	(a) IC50 = 3.51 µg/mL (b) IC50 = 1.02 µg/mL (c) glucose uptake	[9]
	Platelet anti-aggregatory activity	In vitro	(a) Adenosine 5′-diphosphate inhibitory activity (b) Arachidonic-acid inhibitory activity (c) Collagen inhibitory activity	-	0–1 mg/mL	1 mg/mL	[47]
	Larvicidal activity	In vitro	Larvicidal activity against (a) Culex pipiens pallens (b), Aedes aegypti (c) Aedes togoi	-	1–20 mg/L	(a) LC50 = 1.4 mg/L (b) LC50 = 1.9 mg/L (c) LC50 = 2.2 mg/L	[44]
	Hepatoprotective activity	In vitro	Protection against t-BHP-induced hepatotoxicity in HepG2 cells	-	25 µM	protect cells damage	[37]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	25 µM	(a) IC50 = 23 µM (b) IC50 = 54 µM	[19]
Alaternin	Neuroprotective activity	In vivo	Prevented nitrotyrosine and lipid peroxidation, as well as BCCAO induced-iNOS expression and significantly reduced microglial activation	Orally	1, 10 mg/kg	10 mg/kg	[48]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity (c) Stimulation of glucose uptake in HepG2 cells	-	(a) 0–100 µg/mL (b) 0–400 µg/mL (c) 12.5–50 µM	(a) IC50 = 1.22 µg/mL (b) IC50 = 0.99 µg/mL (c) glucose uptake	[9]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 6.29 µg/mL (b) IC50 = 113 µg/mL (c) IC50 = 0.94 µg/mL	[10]
	Hepatoprotective activity	In vitro	Protection against t-BHP-induced hepatotoxicity in HepG2 cells	-	50, 100 µM	(a) protect cells damage (b) increased GSH level and reduce ROS level	[37]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	10 µM	(a) IC50 = 5.35 µM (b) IC50 = 4.55 µM	[19]
Obtusifolin	Neuroprotective activity	In vivo	Significantly reversed scopolamine-induced cognitive impairments in the passive avoidance test, improved escape latencies, swimming times in the target quadrant, and crossing numbers in the zone in Morris water maze test	Orally	0.25–2 mg/kg	0.5 mg/kg	[49]
	Hyperlipidemia and antioxidant activity	In vivo	Reduced body weight, TC, TG, LDL-C and increased HDL-C levels, as well as increased SOD and NO, and reduced MDA levels in hyperlipidemic rats.	Orally	5 and 20 mg/kg	20 mg/kg	[50]
	Neuropathic and anti-inflammatory activity	In vivo	Inhibition of TNF-α, IL-1β, IL-6 and NF-kB up-regulation in the spinal cord in mice and rat models	Intraperitoneal injection	0.25–2 mg/kg	1 and 2 mg/kg	[51]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 18.5 µg/mL (b) IC50 = 284 µg/mL (c) IC50 = 64.8 µg/mL	[10]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 35.2 µg/mL (b) IC50 = 142 µg/mL	[9]
	Hepatoprotective activity	In vitro	Protection against tacrine-induced hepatotoxicity in HepG2 cells	-	160 µM	Protection ratio value 41.2% at 160 µM	[36]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity; (b) MAO-B inhibitory activity	-	100 µM	(a) IC50 = 31 µM (b) IC50 ≥ 400 µM	[19]
Gluco-obtusifolin	Neuropathic and anti-inflammatory activity	In vivo	Inhibition of TNF-α, IL-1β, IL-6 and NF-kB up-regulation in the spinal cord in mice and rat models	Intraperitoneal injection	0.25–2 mg/kg	1 and 2 mg/kg	[51]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–400 µg/mL	(a) IC50 = 37.2 µg/mL (b) IC50 = 172 µg/mL (c) IC50 = 41.1 µg/mL	[10]
	Neuroprotective activity	In vivo	Significantly reversed scopolamine-induced cognitive impairments in the passive avoidance test, improved escape latencies, swimming times in the target quadrant, and crossing numbers in the zone in the Morris water maze test	Orally	0.25–2 mg/kg	0.5 mg/kg	[49]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 53.35 µg/mL (b) IC50 = 23.77 µg/mL	[9]
	Platelet anti-aggregatory activity	In vitro	(a) Adenosine 5′-diphosphate inhibitory activity (b) Arachidonic-acid inhibitory activity (c) Collagen inhibitory activity	-	0–1 mg/mL	(a) IC50 = 0.25 µg/mL (b) IC50 = 0.05 µg/mL (c) IC50 = 0.1 µg/mL	[5]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	500 µM	(a) IC50 ≥ 400 µM (b) IC50 ≥ 400 µM	[19]
Aurantio-obtusin	Hepatoprotective activity	In vitro	Protection against tacrine-induced hepatotoxicity in HepG2 cells	-	160 µM	Protection ratio value 55.3% at 160 µM	[36]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 92.1 µg/mL (b) IC50 = 314 µg/mL (c) IC50 = 67.9 µg/mL	[10]
	Platelet anti-aggregatory activity	In vitro	(a) Adenosine 5′-diphosphate inhibitory activity (b) Arachidonic-acid inhibitory activity (c) Collagen inhibitory activity	-	0–1 mg/mL	1 mg/mL	[48]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 27.19 µg/mL (b) IC50 = 41.20 µg/mL	[9]
	Anti-cancer activity	In vitro	Cytotoxicity against (a) HCT-116, (b) A549, (c) SGC7901 and (d) LO2 cell lines	-	0.4–50 µg/mL	(a) IC50 = 18.9 µg/mL (b) IC50 = 20.1 µg/mL (c) IC50 = 22.0 µg/mL (d) IC50 = 23.1 µg/mL	[52]
	Prevention of bone disease	In vitro	Stimulates osteoblast migration, differentiation, and mineralization in a dose-dependent manner in MC3T3-E1 osteoblast cells	-	0.1–100 µM	10 µM	[53]
	Anti-inflammatory activity	In vitro	(a) Significantly decreased the production of NO, PGE2, and inhibited the iNOS, COX-2, TNF-α and IL-6. (b) Reduced the LPS-induced activation of nuclear factor-κB in RAW264.7 cells.	-	6.12–100 µM	6.12–100 µM	[54]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	200 µM	(a) IC50 = 27.23 µM (b) IC50 = 174.40 µM	[19]
Obtusin	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 6.44 µg/mL (b) IC50 = 20.92 µg/mL	[9]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 82 µg/mL (b) IC50 = 287 µg/mL (c) IC50 = 61.9 µg/mL	[10]
	Anti-cancer activity	In vitro	Cytotoxicity against (a) HCT-116, (b) A549, and (c) SGC7901 cell lines	-	0.4–50 µg/mL	(a) IC50 = 13.1 µg/mL (b) IC50 = 29.2 µg/mL (c) IC50 = 15.2 µg/mL	[52]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	400 µM	(a) IC50 = 11.12 µM (b) IC50 ≥ 400 µM	[19]
Chryso-obtusin	Anti-cancer activity	In vitro	Cytotoxicity against (a) HCT-116, (b) A549, (c) SGC7901 and (d) LO2 cell lines	-	0.4–50 µg/mL	(a) IC50 = 10.5 µg/mL (b) IC50 = 14.6 µg/mL (c) IC50 = 12.0 µg/mL (d) IC50 = 15.8 µg/mL	[52]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 68.6 µg/mL (b) IC50 = 287 µg/mL (c) IC50 = 49.9 µg/mL	[10]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 14.88 µg/mL (b) IC50 = 36.1 µg/mL	[9]
	Platelet anti-aggregatory activity	In vitro	(a) Adenosine 5′-diphosphate inhibitory activity (b) Arachidonic-acid inhibitory activity (c) Collagen inhibitory activity	-	0–1 mg/mL	1 mg/mL	[47]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	400 µM	(a) IC50 = 327.67 µM (b) IC50 ≥ 400 µM	[19]
Questin	Antimicrobial activity	In vitro	Antibacterial activity against (a) Staphylococcus aureus 209P and (b) Escherichia coli NIHJ	-	0–100 µg/mL	MIC (a) 25 µg/mL (b) 50 µg/mL	[48]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 34.0 µg/mL (b) IC50 = 138 µg/mL (c) IC50 = 32.8 µg/mL	[10]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 5.69 µg/mL (b) IC50 = 136.1 µg/mL	[9]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	20 µM	(a) IC50 = 0.17 µM (b) IC50 = 10.58 µM	[19]
Gluco-aurantio-obtusin	Platelet anti-aggregatory activity	In vitro	(a) Adenosine 5′-diphosphate inhibitory activity (b) Arachidonic-acid inhibitory activity (c) Collagen inhibitory activity	-	0–1 mg/mL	(a) IC50 = 0.25 µg/mL (b) IC50 = 0.05 µg/mL (c) IC50 = 0.1 µg/mL	[5]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 109 µg/mL (b) IC50 = 50.9 µg/mL	[10]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 31.3 µg/mL (b) IC50 = 142.1 µg/mL	[9]
	Hepatoprotective activity	In vitro	Hepatoprotective efficacy against t-BHP-induced cell death in HepG2 cells	-	20 µM	Protection ratio value 49.7% at 20 µM	[12]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	400 µM	(a) IC50 = 39.55 µM (b) IC50 = 180.76 µM	[19]
Chrysophanol; Aloe-emodin; Physcion; Chrysophanol tri, Tetraglucoside; 2-hydroxyemodin-1methylether; Chryso-obtusin-2-O-β-d-glucoside	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 5~103 µg/mL (b) IC50 = 5~228 µg/mL	[9]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–400 µg/mL	(a) IC50 = 14~71 µg/mL (b) IC50 ≥ 100 µg/mL (c) IC50 = 13~59 µg/mL	[10]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	400 µM	(a) IC50 = 2.47~400 µM (b) IC50 ≥ 400 µM	[19]
Dihydroxyanthraquinone	Bacterial growth promoting and inhibiting activity	In vitro	(a) Growth promoting activity against Bifidobacterium bifidum (b) Growth inhibiting activity against Clostridium perfringens and Escherichia coli	-	(a) 0.05–0.5 mg/d (b) 0.1–5 mg/d	(a) GIR > 2.0 at 0.5 mg/disk (b) Inhibitory zone diameter > 30 mm	[7]
Naphthopyrone
Cassiaside	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 18.1 µg/mL (b) IC50 = 177 µg/mL (c) IC50 = 1.85 µg/mL	[10]
	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 48.55 µg/mL (b) IC50 = 129.2 µg/mL	[9]
	Hepatoprotective activity	In vitro	Hepatoprotective efficacy against t-BHP-induced cell death in HepG2 cells		25 µM	(a) protect cells damage (b) increased GSH level and reduce ROS level	[37]
	Parkinson’s disease activity	In vitro	(a) MAO-A inhibitory activity (b) MAO-B inhibitory activity	-	400 µM	(a) IC50 = 11.26 µM (b) IC50 ≥ 400 µM	[19]
Isotoralactone; Toralactone	Antimicrobial activity	In vitro	Antibacterial activity against (a) Staphylococcus aureus 209P and (b) Escherichia coli NIHJ	-	0–100 µg/mL	MIC (a) 2–3 µg/Ml (b) 5.5–12 µg/mL	[46]
Cassiaside B2, Cassiaside C2	Antiallergic activity	In vitro	Inhibition of histamine release in rat peritoneal mast cells	-	100 µM	Cassiaside B2 inhibit 17.2%; Cassiaside C2 Inhibit 53.9%	[6]
Toralactone Gentiobioside	Antidiabetic activity	In vitro	(a) PTP 1B inhibitory activity (b) α-glucosidase inhibitory activity	-	(a) 0–100 µg/mL (b) 0–400 µg/mL	(a) IC50 = 81.1µg/mL (b) IC50 = 37.60 µg/mL	[9]
	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) Butyrylcholinesterase inhibitory activity (c) β-secretase inhibitory activity	-	0–100 µg/mL	(a) IC50 = 91.3 µg/mL (b) IC50 = 117 µg/mL (c) IC50 = 69.0 µg/mL	[10]
	Hepatoprotective activity	In vitro	Hepatoprotective efficacy against t-BHP-induced cell death in HepG2 cells	-	20 µM	Increased in Nrf2/ARE-luciferase activity, and upregulated NQO1, GLC, HO-1 levels	[12]
rubrofusarin, Rubrofusarin 6-O-β-d-glucopyranoside, Rubrofusarin 6-O-β-d-gentiobioside, Nor-rubrofusarin 6-O-β-d-glucoside	Anti-Alzheimer’s activity	In vitro	(a) Acetylcholinesterase inhibitory activity (b) β-secretase inhibitory activity	-	(a) 0–100 µM (b) 0–750 µM	(a)15.95–148 µM (b) 14.0–190 µM	[55]