Citrus aurantium

scientific name:

Citrus aurantium L.

synonym:

Aurantium acre Mill.

Botanical family:

RUTACEAE

Botanical description

Tree, up to 10 m tall with slender thorns. Leaf blade 7-20 cm x 7 cm; widely winged petiole; flowers axillary, white 4 cm; fruit, globose, 7-8 cm in diameter, somewhat flat at the top, peel thick, rough and strongly aromatic, pulp acidic and bitter, seeds numerous.

Voucher(s)

Jiménez,1507,JBSD

Medina,2,CICY

Benedetti,3,MAPR

Fuentes,946,ROIG

Ríos,409,CECALLI

Longuefosse&Nossin,13,HAVPM

flatulence:

fruit peel, infusion, orally⁵

fever:

peel or leaf, decoction or infusion, orally^3-4

conjunctivitis:

fruit, juice, instillation^2-3

diarrhoea:

fruit, juice, orally^2-3

flu:

fruit, juice, orally^3-4

colics:

leaf, decoction or infusion, orally¹

headhache:

leaf, decoction or infusion, orally^3-4

flu:

leaf, decoction or infusion, orally^3-4

intestinal parasites:

leaf, decoction, orally⁶

cough:

fruit, juice, orally^2-3,39

The fruit and the juice of Citrus aurantium are widely used for human consumption and the peel as an industrial source of essential oil.

For colic, headache, fever, flu:

Prepare a decoction or infusion with 10-15 grams (3-5 tender leaves) in 1/2 liter (2 cups) of water. For decoction, boil for at least 10 minutes in a covered pot; for infusion, add boiling water to 3-5 tender leaves, cover and leave to cool down. Drink lukewarm, 1 cup 3 times a day¹.

For fever:

Prepare a decoction with 1-2 teaspoonfuls (5-10 grams) of fruit peel in 250 mL (1 cup) of water, boil for at least 10 minutes in a covered pot. Filter, cool down and drink 1 cup 3 times a day³³.

For flatulence:

Prepare an infusion, adding 1 liter (4 cups) of boiling water to the peel of half a fruit. Cover the pot, let it settle for 5-10 minutes and filter. Drink 1 cup as needed⁵.

For intestinal parasites:

Prepare a decoction with 8-18 tender leaves in 1/2 liter (2 cups) of water. Boil for at least 10 minutes in a covered pot. Leave it to cool down, sweeten with honey and drink lukewarm, 1 cup twice a day¹.

For conjunctivitis, diarrhea, flu, cough (juice):

There is no available information establishing a means of preparation and dosage other than that referred to by traditional use.

According to published and other information:

Use for colic, conjunctivitis, headache, fever, flu, intestinal parasites and cough is classified as REC, based on the significant traditional use (OMS/WHO)⁴ documented in the TRAMIL surveys.

In every application in the eyes, strict hygiene measures should be observed in order to avoid contamination or additional infection. Additionally, contact with any substances that may be irritating to the conjunctiva should be avoided. There exists the risk of increasing irritation due to the application of Citrus spp juice.

Should there be a notable worsening of the patient’s condition, or should fever last more than 2 days, or should conjunctivitis or headache last more than 3 days, seek medical attention.

Use for diarrhea and flatulence is classified as REC, based on the significant traditional use documented in the TRAMIL surveys, and on available published scientific information.

In the case of diarrhea, the use of this resource can be considered complementary to oral re-hydration therapy. Should there be a notable worsening of the patient’s condition, or should diarrhea last more than 3 days in adult, or 2 days in children, seek medical attention.

Due to the risk of interaction with cyclosporin, ingestion of the fruit decoction should be avoided by anyone taking this medicine.

The essential oil of the plant can cause reactions of hypersensitivity.

TRAMIL Research³⁴

Decoctions at 30% of fresh fruit (yield 1.15 mg/mL) administered to rats as a single oral dose (maximum volume of 2 mL/100 g body weight, equivalent to 6 g plant material/kg or 230 mg of total solids/kg) in conformance with the normal acute toxicity test, did not cause death nor evidence signs of intoxication during the first 24 hours nor during the following 14 days of observation, nor were any histopathological alterations seen.

TRAMIL Research³⁵

The juice of the fresh fruit (yield: 12.29 mg/mL) administered to rats as a single oral dose (maximum volume of 2 mL/100 g body weight, equivalent to 2458 mg of total solids/kg or 20 mg plant juice/kg) in conformance with the normal acute toxicity test, did not cause death nor evidence signs of intoxication during the first 24 hours nor during the following 14 days of observation, nor were any histopathological alterations seen.

TRAMIL Research³¹

The lyophilized aqueous decoction of the fresh leaf was administered orally at a dose of 1 g/kg/day during 5 successive days per week for two weeks (ten administrations) to 10 Swiss male mice (21.33 + 0.64 g). The control group of 10 mice, of the same strain and characteristics, received distilled water (0.3 mL). The groups were observed for another 7 days after the treatment period. No mortality or signs of toxicity were observed in the observed parameters. Autopsy did not reveal any internal alterations.

TRAMIL Research³⁸(will be translatedin 3rd Edition)

El jugo fresco del fruto, vía tópica (100 µL) en el saco conjuntival del ojo derecho de 3 conejos en el modelo de irritación ocular. Se observa por 72 horas. No se observó ninguna alteración ni irritación durante el periodo de observación.

The decoction of fruit administered orally to pig (1 L/day) jointly with cyclosporin (10 mg/kg) increased the maximum concentration by 64% and its bioavailability; in 20% of the animals there were signs of acute toxicity by cyclosporin²⁹.

The aqueous extract from the fruit (500 µg/mL) was cytotoxicin vitro but there was no evidence of embryotoxicity³⁰.

The aqueous and methanolic extracts from the unripe fruit (50 mg dry weight/disc) did not show mutagenic activity, with and without metabolic activation, in agar plate cultures of Salmonella typhimurium strains TA98 and TA100³¹.

The aqueous and methanolic extracts from the unripe fruit (100 mg/mL) on agar plates did not exhibit mutagenic activity in Bacillus subtillis H17 and Salmonella typhimurium TA98 and TA100 with and without metabolic activation³².

There is no available information documenting the safety of medicinal use in children or in women during pregnancy or breast feeding.

The leaf contains essential oils: linalool (11%), linalool acetate⁸; flavonoids: neodiosmin, neohesperidin, naringin and rhoifolin⁹.

The seed contains various terpenes¹⁰; the fruit contains triterpene limonoid bitter principles: limonin, nomilin and nomilic acid^-12 and an isoquinoline alkaloid: synephrine¹³.

The fruit pulp contains large amounts of organic acids (mainly citric and malic) and of vitamin C; while the pericarp contains pectin¹⁴.

The flower contains essential oil ("neroli") 0.05-0.5%: limonene, linalool, nerol and methyl anthranilate⁸.

The pericarp has been extensively studied and contains, among other components, flavonoids: naringenin, hesperidin, neohesperidin¹⁵; essential oil ("curaçao") 2%: limonene (90%)⁸.

Proximate analysis of 100 g of fruit¹⁶: calories: 44; water: 87.5%; proteins: 0.7%; fat: 0.1%; carbohydrates: 11.2%; fiber: 2%; ash: 0.5%; calcium: 42 mg; phosphorus: 20 mg; iron: 0.4 mg; carotene: 70 mg; thiamine: 0.07 mg; riboflavin: 0.03 mg; niacin: 0.3 mg; ascorbic acid: 43 mg.

Trabajo TRAMIL³⁷(will be translatedin 3rd Edition)

La decocción 30% de hoja fresca, vía oral (dosis 0.5, 1 y 5 g de material vegetal/kg), modelos de contorciones inducidas por ácido acético (0.75%, 0.1 mL/10 g) intraperitoneal y retirada de la cola provocada por inmersión en agua caliente (55^oC), ratones OF-1 machos (20-25 g), 10 animales/grupo. La decocción (1 y 5 g/kg) mostró actividad analgésica significativa en el modelo de contorciones y no inhibió significativamente la respuesta en el de retirada de la cola.

The aqueous extract from the dried fruit (20 mg/disc) showed in vitro activity against Candida albicans¹⁷.

The tincture of the dried fruit (10 g of dried vegetal material/100 mL of ethanol) on agar plate (30 µL/disc) showed antibacterial activity in vitro against Staphylococcus aureus¹⁸.

The decoction of the fruit (0.05 mg/mL) in vitro was active against rotavirus; the active principles were the flavanone glycosides hesperidin and neohesperidin with median inhibiting concentrations (MIC) of 10 and 25 micromoles, respectively¹⁹.

The aqueous extract from ripe fruit in estrogenized uterus of rat showed unspecific antispasmodic effects in vitro, with an ID₅₀ of 1.8 µg/mL. The aqueous extracts from ripe and unripe fruit peel showed the same effects in this experimental model with an ID₅₀ = 0.16 and 0.27 µg/mL, respectively²⁰.

The decoctions of dried unripe (1.7 and 10 µg/mL)²¹ and ripe (1.8 µg/mL) fruit²⁰in vitro had a relaxing effect on the estrogenized uterus of rat.

The hydroalcoholic extract (95%) from the dried fruit peel (2.5 mL/L) had an antispasmodic effect on guinea pig ileum²².

The aqueous extract from the dried fruit (2 g/kg) administered orally to mouse had anti-diarrheal effects in vivo in 5-hydroxytryptophan-induced diarrhea²³.

The aqueous extract from the dried fruit (19.3 mg/kg) administered orally to mouse showed immunomodulating activity in vivo²⁴.

The decoction of the dried fruit (100 and 250 mg/kg) administered orally to rats, both male and female, evidenced anti-ulcer activity in gastric injuries induced by ethanol, hydrochloric acid and aspirin²⁵.

The decoction of the dried fruit peel (1%) applied topically in human adults was active against skin pigmentation induced by ultraviolet light²⁶.

In a pharmaco-kinetic study, the ingestion of fresh fruit juice (1250 mL) by human adults reported absorption of naringin and hesperidin (flavonoids)²⁷.

Vitamin C has anti-infectious¹⁴ and anti-scorbutic properties, it is an enzymatic cofactor, it is involved in the synthesis of collagen and carnitine, the transformation of folic acid into folinic acid, the microsomic metabolism of drugs, the synthesis of noradrenaline and peptidic hormones, the reduction of ferric to ferrous iron at gastric level, and the formation of suprarenal hormones²⁸.

Pharmacopoeia:

Ed.2

References:

1 MENDEZ M, MEDINA ML, DURAN R, 1996 Encuesta TRAMIL. Unidad de recursos naturales, Centro de Investigación Científica de Yucatán CICY, Mérida, México.

2 WENIGER B, ROUZIER M, 1986 Enquête TRAMIL. Service Oecuménique d'Entraide SOE, Port au Prince, Haïti.

3 WENIGER B, 1987-88 Encuesta TRAMIL. enda-caribe, Santo Domingo, Rep. Dominicana.

4 GERMOSEN-ROBINEAU L, GERONIMO M, AMPARO C, 1984 Encuesta TRAMIL. enda-caribe, Santo Domingo, Rep. Dominicana.

5 MARCELLE G, 1996 TRAMIL survey. Produce chemist laboratory, Ministry of Agriculture, St George's, Grenada.

6 BENEDETTI MD, 1994 Encuesta TRAMIL. Universidad de Puerto Rico, Mayagüez, Puerto Rico.

7 OMS/WHO, 1991 Pautas para la evaluación de medicamentos herbarios WHO/TRM/91.4 (original inglés). Programa de Medicina Tradicional, OMS, Ginebra, Suiza.

8 LIN Z, HUA Y, GU Y, 1986 The chemical constituents of the essential oil from the flowers, leaves and peels of Citrus aurantium. Chih Wu Hsueh Pao 28(6):635-640.

9 RIO JAD, BENAVENTE O, CASTILLO J, BORREGO F, 1992 Neodiosmin, a flavone glycoside of Citrus aurantium. Phytochemistry 31(2):723-724.

10 BENNETT RD, MIYAKE M, OZAKI Y, HASEGAWA S, 1991 Limonoid glucosides in Citrus aurantium.Phytochemistry 30(11):3803-3805.

11 WIDMER WW, 1991 Improvements in the quantitation of limonin in Citrus juice by reversed-phase high-performance liquid chromatography. J Agric Food Chem 39(8):1472-1476.

12 HERMAN Z, FONG CH, OU P, HASEGAWA S, 1990 Limonoid glucosides in orange juices by HPLC. J Agric Food Chem 38(9):1860-1861.

13 HOSODA K, NOGUCHI M, KANAYA T, HIGUCHI M,1990 Studies on the preparation and evaluation of Kijitsu, the immature citrus fruits. III. Relation between diameter of Kijitsu and synephrine content. Yakugaku Zasshi 110(1):82-84.

14 BEZANGER-BEAUQUESNE L, PINKAS M, TORCK M, 1986 Les plantes dans la thérapeutique moderne. 2 éd. Paris, France: Ed. Maloine.

15 WAGNER H, BLADT S, MUNZING-VASITIAN K, 1975 Thin-layer chromatography of bitter principle drugs. Pharm-Ztg 120:1262.

16 DUKE JA, ATCHLEY AA, 1986 Handbook of proximate analysis tables of higher plants. Boca Raton, USA: CRC Press, p45.

17 AVIRUTANT W, PONGPAL A, 1983 The antimicrobial activity of some Thai flowers and plants. Mahidol Univ J Pharm Sci 10(3):81-86.

18 CACERES A, GIRON LM, ALVARADO SR, TORRES MF, 1987 Screening of antimicrobial activity of plants popularly used in Guatemala for the treatment of dermatomucosal diseases. J Ethnopharmacol 20(3):223-237.

19 KIM DH, SONG MJ, BAE EA, HAN MJ, 2000 Inhibitory effect of herbal medicines on rotavirus infectivity. Biol Pharm Bull 23(3):356-358.

20 SANKAWA U, 1980 Screening of bioactive compounds in oriental medicinal drugs. Korean J Pharmacog 11:125-132.

21 KINOSHITA T, SAMESHIMA M, SANKAWA U, 1979 Isolation of a sympathomimetic substance from Chinese medicinal drugs originated from Citrus sp. Shoyakugaku Zassmi 33:146-149.

22 FORSTER HB, NIKLAS H, LUTZ S, 1980 Antispasmodic effects of some medicinal plants. Planta Med 40(4):309-319.

23 YOO JS, JUNG JS, LEE TH, SON KH, SUH HW, SONG DK, KIM YH, 1995 Inhibitory effects of extracts from traditional herbal drugs on 5-hydroxytryptophan-induced diarrhea in mice. Korean J Pharmacog 26(4):355-359.

24 IWAMA H, AMAGAYA S, OGIHARA Y, 1986 Effects of five kampohozais on the mitogenic activity of lipopolysaccharide, concanavalin A, phorbol myristate acetate and phytohemagglutinin in vivo. J Ethnopharmacol 18(2):193-204.

25 HIRANO H, TAKASE H, YAMAMOTO K, YANASE T, ABE K, SAITO Y, 1997 The anti-ulcer effects of Aurantii Fructus Immaturus, Aurantii Fructus and the principles in Aurantii Fructus Immaturus. Nat Med 51(3):190-193.

26 AZUMA S, YADA Y, IMOKAWA G, TAZAKI S, SHINHO T, 1996 Skin-lightening cosmetics containing plant extracts and ascorbic acid or placenta extracts. Patent-Japan Kokai Tokyo Koho-08 208,451.

27 AMEER B, WEINTRAUB RA, JOHNSON JV, YOST RA, ROUSEFF RL, 1996 Flavonone absorption after naringin, hesperidin, and Citrus administration. Clin Pharmacol Ther 60(1):34-40.

28HARTMAN JG, LIMBIRD ILE, Eds., 1996 Goodman & Gilman las bases farmacológicas de la Terapéutica, 9^a edición. México, México: McGraw-Hill Editorial. p1670-1671.

29 HOU YC, HSIU SL, TSAO CW, WANG YH, CHAO PD, 2000 Acute intoxication of cyclosporin caused by coadministration of decoctions of the fruits of Citrus aurantium and the pericarps of Citrus grandis.Planta Med 66(7):653-655.

30 SATO A, 1989 Studies on anti-tumor activity of crude drugs. I. The effects of aqueous extracts of some crude drugs in short term screening test. Yakugaku Zasshi 109(6):407-423.

31 YAMAMOTO H, MIZUTANI T, NOMURA H, 1982 Studies on the mutagenicity of crude drug extracts. I. Yakugaku Zasshi 102(6):596-601.

32 MORIMOTO I, WATANABE F, OSAWA T, OKITSU T, KADA T, 1982 Mutagenicity screening of crude drugs with Bacillus subtilis REC-assay and Salmonella microsome reversion assay. Mutat Res 97(2):81-102.

33 CANIGUERAL S, VILA R, RISCO E, PEREZ F, PORTILLO A, FREIXA B, MILO B, VANACLOCHA B, RIOS JL, MORALES MA, ALONSO JR, BACHILLER LI, PERIS JB, STUBING G, 2002 Citrus aurantium. Vademecum de Fitoterapia, Editorial Masson, Barcelona, España, Jul.20,2002. URL: http://www.masson.es/book/fitoterapia.html

34 MARTINEZ MJ, MOREJON Z, LOPEZ M, BOUCOURT E, FUENTES V, MORON F, 2005 Clases tóxicas agudas (CTA) de una infusión de corteza de fruto fresco de Citrus aurantium L.Informe TRAMIL. Laboratorio Central de Farmacología, Facultad de Ciencias Médicas “Dr. Salvador Allende”, La Habana, Cuba.

35 MARTINEZ MJ, MOREJON Z, LOPEZ M, BOUCOURT E, FUENTES V, MORON F, 2005 Clases tóxicas agudas (CTA) de zumo de fruto fresco de Citrus aurantium L.Informe TRAMIL. Laboratorio Central de Farmacología, Facultad de Ciencias Médicas “Dr. Salvador Allende”, La Habana, Cuba.

36 GarcIa-GONZALEZ M, fallas LV, 2005 Toxicidad aguda dosis repetida, en ratones, del extracto acuoso (decocción) de las hojas frescas de Citrus aurantium . Informe TRAMIL.PRONAPLAMED. Depto de Fisiología, Escuela de Medicina, Universidad de Costa Rica, San Pedro, Costa Rica.

37 MORON FJ, MOREJON Z, GARCIA AI, LOPEZ M, BOUCOURT E, BACALLAO Y, FUENTES V, 2008 Acción analgésica de la decocción 30% de hojas frescas de Citrus aurantium L. (naranja agria) en ratones. Informe TRAMIL. Laboratorio Central de Farmacología, Facultad de Ciencias Médicas “Dr. Salvador Allende”, Ciudad de La Habana, Cuba.

38 PAZOS L, COTO T, CAIZA F, 2009

Irritación ocular, en conejos, del jugo fresco del fruto de Citrus aurantium. Informe TRAMIL. Laboratorio de Ensayos Biológicos, LEBi, Universidad de Costa Rica, San Pedro, Costa Rica.

39 LONGUEFOSSE JL, NOSSIN E, 1990-95 Enquête TRAMIL. Association pour la valorisation des plantes médicinales de la Caraïbe AVPMC, Fort de France, Martinique.

40 MOREJON Z, LOPEZ M, GARCIA MJ, BOUCOURT E, VICTORIA M, FUENTES V, MORON F, BOULOGNE I, ROBINEAU L, 2009 Encuesta TRAMIL preliminar a grupos de vecinos en los municipios 10 de Octubre, Lisa, Marianao, Habana del Este (Cojímar) en la Ciudad de la Habana. Laboratorio Central de Farmacología, Universidad de Ciencias Médicas de La Habana, Ciudad de La Habana, Cuba.

DISCLAIMER

The information provided is for educational purposes only for the benefit of the general public and health professionals. It is not intended to take the place of either the written law or regulations. Since some parts of plants could be toxic, might induce side effects, or might have interactions with certain drugs, anyone intending to use them or their products must first consult with a physician or another qualified health care professional. TRAMIL has no responsibility whatsoever towards the user for any decision, action or omission made in relation to the information contained in this Pharmacopoeia.

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