Citrullus colocynthis (L.) Schrad (Bitter Apple): An Overview of its Traditional Uses, Phytochemistry and Pharmacological Potential

Chemical Class	Isolated Compounds	Plant	Part Reference
Glycosides, flavonoids and phenolic acids	2-O-β-D-glucopyranosyl-Cucurbitacin I	Fruit	12
	2-O-β-D-glucopyranosyl-CucurbitacinL	Fruit	12
	Isosaponarin	Fruit, seeds	12, 13
	Isoorientin 3-o-methylether	Fruit, seeds	12, 13
	Isovitexin	Fruit, seeds	12, 13
	Quercetin	Fruits	14, 15
	Catechin	Fruit pulp	15
	Myricetin	Fruit pulp	15
	Gallic acid	Fruit pulp	15
	Kaempferol	Fruit pulp	15
	p-Hydroxybenzoicacid	Fruit pulp	15
	Caffeic acid	Fruit pulp	15
	Chlorogenic acid	Fruit pulp	15
	Vanillic acid	Fruit pulp	15
	Ferulic acid	Fruit pulp	15
	Sinapic acid	Fruit pulp	15
	p-Coumeric acid	Fruit pulp	15
Alkaloids	Choline	Whole fruit, pulp	10, 16, 17
Alkaloids	Choline	Fruit pulp	18
Cucurbitacins	Curcubitacin A	Fruit	19, 20
	Curcubitacin B	Whole fruit	17, 21
	Curcubitacin C	Fruit	19
	Curcubitacin D	Fruit	19
	Curcubitacin E	Whole fruit	17, 21, 22
	Curcubitacin I	Whole fruit	17, 20
	Curcubitacin J	Fruit	20
	Curcubitacin K	Fruit	20
	Curcubitacin L	Fruit	20
	Colocynthosides A	Fruit	20
	Colocynthosides B	Fruit	20
Fatty acids	Palmitic acid, stearic acid, linoleic acid, oleic acids	Seed oils	23,24,25
Fatty acids	Myristic, palmitic, stearic, oleic, linoleic and linolenic acids	Seeds	13
Tocopherols and Carotenes	α-tocopherol, γ-tocopherol, β-carotene	Seed oil	26

Table 2.

Chemical Structures of some chemical Compounds present in Citruluss Colosynthis.

Table 3.

Pharmacological Activities of different parts of Citruluss Colocynthis plant

Pharmacological activity	Part/Activity	Extract/ compound	Dose/conc.	Results	References
Antimicrobial activity	Fruit/ in vitro	Water extract	5 mg/mL	inhibition against Staphylococcus aureus	10
	Fruit/ in vitro	Ethanol extract	500 mg/mL	Inhibition against Staphylococcus aureus,	17
	Fruit/ in vitro	Ethanol extract	500 mg/mL	Inhibition against Bacillus cereus	17
	Fruit/ in vitro	Ethanol extract	500 mg/ml	Inhibition against Klebsiella pneumonia	17
	Fruit/ in vitro	Cucurbitacin B	500 mg/ml	Inhibition against Staphylococcus aureus	17
	Fruit/ in vitro	Cucurbitacin B	500 mg/ml	Inhibition against Bacillus cereus	17
	Fruit/ in vitro	Cucurbitacin B	500 mg/ml	Inhibition against Klebsiella pneumonia	17
	Fruit/ in vitro	Cucurbitacin E	500 mg/ml	Inhibition against Staphylococcus aureus	17
	Fruit/ in vitro	Cucurbitacin E	500 mg/ml	Inhibition against Bacillus cereus	17
	Fruit/ in vitro	Cucurbitacin E	500 mg/ml	Inhibition against Klebsiella pneumonia	17
	Fruit/ in vitro	Cucurbitacin I	500 mg/ml	Inhibition against Staphylococcus aureus	17
	Fruit/ in vitro	Cucurbitacin I	500 mg/ml	Inhibition against Bacillus cereus	17
	Fruit/ in vitro	Cucurbitacin I	500 mg/ml	Inhibition against Klebsiella pneumonia	17
Anti-inflammatory Activity	Fruit/ in vivo	Water extract	4 mg/kg	97.29% reduction in edema after 6 hour in Carrageenan-induced paw edema model in rats	46
Anti-inflammatory Activity	Fruit/ in vitro	Aqueous ethanol extract gel	2 g of gel/3%	45% reduction in edema in Carrageenan-induced paw edema model in rats	52
Hypolipidemic Activity	Seed/in vivo	Powder	300 mg/Day	Decrease in the level of triglyceride and cholesterol concentration in non-diabetic hyperlipidemic patients	37
Hypolipidemic Activity	Fruit/ in vivo	Aqueous ethanol extract	1.2 g/kg/day	Reduction in Serum cholesterol levels in Hyperlipidaemic Rabbits	45
Antidiabetic Activity	Fruit/ in vivo	Petroleum ether extract	300 mg/kg	reduction in blood glucose levels in STZ induced diabetic rats	9
	Fruit/ in vivo	Hydro-ethanol extract	300 mg/kg	Reduction in total cholesterol, triglycerides, phospholipids and free fatty acids levels in diabetic rats	53
	Fruit/ in vivo	Aqueous extract	300mg/kg	Decrease of blood glucose in normoglycaemic rabbits	54
	Seed/ in vivo	Aqueous extract	300mg/kg	Reduction in the plasma level of AST and LDH in Streptozotocin induced diabetic rats	55
	Fruit/ in vivo	Alkaloid rich fraction	50 mg/kg	Decrease of blood glucose from 132 to 120 mg/100 mL after 6 h of normoglycaemic rabbits	54
	Fruit/ in vivo	Glycoside rich fraction	50 mg/kg	Decrease of blood glucose from 132 to 89 mg/100 mL after 6 h of normoglycaemic rabbits	54
	Fruit/ in vivo	Saponin rich fraction	50 mg/kg	Decrease of blood glucose from 132 to 84mg/100 mL after 6 h of normoglycaemic rabbits	54
Antioxidant Activity	Fruit/ in vivo	Hydro-ethanol extract	300 g/kg	Increase in the enzymatic and non-enzymatic components of the oxidative system in the liver of Alloxan induced diabetic rats	53
	Seed/in vitro	Aqueous extract	IC5=0.021mg/mL	DPPH radical scavenging activity in term of IC50 of aqueous extract of Citrullus colocynthis seeds was tested	46
	Fruit/ in vitro	Methanol extract	2500 μg/mL	88% DPPH radical scavenging activity was found against ascorbic acid	56
	Fruit/ in vitro	Methanol extract	2500 μg/mL	61.4% Nitric oxide scavenging activity was found against ascorbic acid	56
	Fruit/ in vitro	Cucurbitacin glycosides	IC 50 145 μM	ABTS radical scavenging properties	57
Antiallergic Activity	Fruit/ in vivo	Methanol extract	200 mg/kg	72.5% inhibition in ear passive cutaneous anaphylaxis (PCA) reaction in mice	20
Antiallergic Activity	Fruit/ in vivo	Cucurbitacin E2-O-β-D-glucopyranoside	200 mg/kg	49.7% inhibition in ear passive cutaneous anaphylaxis (PCA) reaction in mice	20
Anticancer Activity	Fruit/ in vitro	Cucurbitacin B, Cucurbitacin E (1:1)	20 μM	inhibited the growth of ER+MCF-7 and ER-MDA-MB-231 breast cancer cell lines	21
	Fruit/ in vitro	Alkaloid rich fraction	IC50 3.30 μg/mL	Alkaloid rich fraction demonstrated strong cytotoxicity towards Artemia salina naupli	16
	Fruit/ in vitro	Cucurbitacin B	1–100 μM	Inhibited cellular proliferation of human laryngeal cancer cell line (Hep-2)	58
	Fruit/ in vitro	Cucurbitacin B	LD50 = 0.1 μM	Cucurbitacin B inhibited 50% growth at 0.1 μM of human GBM celllines in liquid culture	59
Insecticidal activity	Fruit/ in vitro	Ethanol extract	LC50 11,003ppm	Against Aphis craccivora	60
	Fruit/ in vitro	Chloroform extract	LC50 17,328ppm	Against Aphis craccivora	60
	Fruit/ in vitro	Methylenechloride extract	LC50 19,497ppm	Against Aphis craccivora	60
	Fruit/ in vitro	n-hexane extract	LC50 23,065ppm	Against Aphis craccivora	60

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DOI: https://doi.org/10.2478/sjecr-2021-0073 | Journal eISSN: 2956-2090 (formerly 2335-075X, 2956-0454) | Journal ISSN: 2956-0454 (formerly 1820-8665)

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Language: English

Page range: 3 - 14

Submitted on: Sep 1, 2020

Accepted on: Jan 27, 2021

Published on: Dec 12, 2022

Published by: University of Kragujevac, Faculty of Medical Sciences

In partnership with: Paradigm Publishing Services

Keywords:

Citrullus colocynthis,

Related subjects:

Clinical medicine, other

© 2022 Anil Kamboj, Randhir Singh Dahiya, published by University of Kragujevac, Faculty of Medical Sciences
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Volume 26 (2025): Issue 1 (March 2025)