Natural Product Radiance, Vol. 8(1), 2009, pp.77-83 Review Paper

Hibiscus sabdariffa Linn.–An overview N Mahadevan*, Shivali and Pradeep Kamboj Department of Pharmacognosy ISF College of Pharmacy Moga-142001, Punjab, India *Correspondent author, E-mail: [email protected] Phone: 09417169055 (Mob) Received 10 September 2007; Accepted 24 December 2008 Abstract 8-12 slim, pointed bracts (or bracteole) sabdariffa Linn. is an annual herbaceous shrub, cultivated for its around the base, they begins to enlarge at although and seeds have also been used in traditional medicine. The calyces of the are the end of the day, 3.2-5.7cm long and used as a refrigerant in the form of , to make jellies and jams. The plant is reported to contain fully enclose the . The fruit is a velvety proteins, , , , acids, minerals and . The plant has been reported capsule, 1.25-2cm long, which is green to have antihypertensive, hepatoprotective, antihyperlipidemic, anticancer and antioxidant properties. The present paper is an overview on its phytochemical and pharmacological properties when immature, 5-valved, with each valve reported in the literature. containing 3-4 seeds. The capsule turns Keywords: Hibiscus sabdariffa, Lal-ambari, Patwa, Red , , Herbal brown and splits open when mature and medicine. dry. Seeds are kidney-shaped, light-brown, IPC code; Int. cl.8— A61K 36/00, A61P 3/06, A61P 9/12, A61P 39/06 3-5mm long and covered with minute, stout and stellate hairs3. Introduction languages it is called as Gongura, Lal- The species H. sabdariffa Hibiscus sabdariffa Linn. is ambari, Patwa (Hindi), Lal-mista, comprises a large number of cultivated a shrub belonging to the family— Chukar (Bengali), Lal-ambadi types which, on the basis of their growth . It is thought of native to Asia (Marathi), Yerra gogu (Telugu), habit or end use, are classified broadly (India to Malaysia) or Tropical . The Pulichchai kerai (Tamil), Pulachakiri, under two varieties, H. sabdariffa var. plant is widely grown in tropics like Pundibija (), Polechi, sabdariffa and H. sabdariffa var. Caribbean, Central America, India, Africa, Pulichchai () and Chukiar altissima Wester. Former is generally Brazil, , Hawaii, Florida and (Assam)1. bushy and pigmented and cultivated for Philippines as a home garden crop. In The plant is about 3.5m tall and the edible calyces; the latter includes tall- , it is a major crop of export has a deep penetrating taproot. It has a growing, unbranched types bearing especially in western part where it smooth or nearly smooth, cylindrical, inedible calyces and mainly cultivated for occupies second place area wise after pearl typically dark green to red stems. Leaves the stem fibre, roselle1. Sorrel is cultivated millet followed by Sesamum1-2. are alternate, 7.5-12.5cm long, green with in various parts of Punjab, Uttar Pradesh, In addition to Roselle, in English- reddish veins and long or short petioles. Andhra Pradesh, Assam, , Madhya speaking regions it is called as Rozelle, Leaves of young seedlings and upper leaves Pradesh, , Orissa and West Sorrel, Red sorrel, sorrel, Indian of older are simple; lower leaves Bengal during April to November. The sorrel, Guinea sorrel, Sour-sour, are deeply 3 to 5 or even 7-lobed and the propagation is done by seeds or by rooting Queensland jelly plant, Jelly okra, Lemon margins are toothed. Flowers, borne singly shoot cuttings. The edible fleshy calyces bush and Florida cranberry. In North Africa in the axils are up to 12.5cm wide, are collected after 15-20 days of flowering. and the Near East, Roselle is called yellow or buff with a rose or maroon eye Rest of the crop is left in the field until karkade or carcadé and it is known by and turn pink as they wither at the end of seeds are ready for threshing. The calyces these names in the pharmaceutical and the day. The typically red calyx, consist of can be dried and stored in air-tight food-flavoring trades in Europe3. In Indian 5 large with a collar (epicalyx) of containers1.

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H. sabdariffa is a hardy herbaceous shrub, grows well in most soils that are well drained. The flowers are hermaphrodite and are pollinated by insects4. It requires a monthly rainfall ranging from 130 to 260 mm in the first 3 to 4 months of growth. Rain and high Dried calyces humidity during harvest and drying can demulcent, digestive, diuretic, emollient, downgrade the quality of calyces and purgative, refrigerant, sedative, stomachic reduce the yield5. Roselle is usually and tonic6-9. On the basis of traditional propagated by seed but grows readily from uses several phytochemical and cuttings. The latter method results in pharmacological studies on the whole shorter plants preferred in India for plant, calyces and seeds have been interplanting with tree crops but the yield conducted by researchers. An overview of of calyces is relatively low3. The plants may these reports are presented here to be cut off 6 weeks after transplanting, facilitate further investigations and leaving only 7.5-10cm of stem in the field. preparation of useful herbal drugs. A second cutting is made 4 weeks later and a third after another 4 weeks. Then Phytochemistry Freshly harvested calyces plants are thinned out and the remaining The leaf is reported to contain plants left to grow and develop fruit as a protein, , , fibre, ash, presence of crude protein and minerals second product. The are harvested calcium, phosphorus, iron, thiamine, such as iron, phosphorus, calcium, when full-grown. The fruits of roselle β-carotene, riboflavin, niacin and manganese, aluminium, magnesium, ripen progressively from the lowest to the ascorbic acid10-16. The yields a sodium and potassium. Mucilage, calcium highest. Harvesting of seeds takes place yellow dye; the major pigment identified citrate, ascorbic acid, gossypetin and when the lower and middle tiers of the is daphniphylline. The plant contains hibiscin chlorideare also present in last of the fruits are allowed to mature, at flavonoids such as hibiscitrin and calyces1. this time the plants are cut down, stacked hibiscetin1 and dried calyces contain the The seeds contain protein for a few days, then threshed between flavonoids gossypetine, hibiscetine and (18.8-22.3%), fat (19.1-22.8%) and canvas sheets. The common pests of the sabdaretine. It also contains alkaloids, dietary fibre (39.5-42.6%) content were plant are root-knot nematode and beetles β-sitosterol, , citric acid, found to be high. The seeds were found such as Nisotra breweri, Lagris cyanea cyanidin-3-rutinose, delphinidin, to be a good source of minerals like 3 and Rhyparida discopunctulata . galactose, pectin, protocatechuic acid, phosphorus, magnesium, calcium, lysine In Egypt and Sudan, the deep red , stearic acid and wax17. Small and tryptophan contents. Seed oil is rich tea from the calyces, called Karkade, is amounts of delphinidin 3-monoglucoside, in unsaturated fatty acids (70%), of which 2 popular as a refrigerant . It is commonly cyanidin 3-monoglucoside (chrysanthenin) linoleic acid constituted 44%. Seeds used to make jellies, jams and beverages. and delphinidin are also present3. Three contain nitrogen, fatty oil, cellulose, In Ayurvedic literature of India, different water soluble polysaccharides have been pentosans and starch19. Steroids and parts of this plant have been recommended isolated from flower buds; neutral tocopherols have been reported in the seed for various ailments like hypertension, polysaccarides composed of arabinans and oil19-21. -3-O-rutinoside, pyrexia and liver disorders. It is arabinogalactans18. kaempferol-3-O-glucopyranoside, traditionally used as antiseptic, The calyces are rich in acid and quercetin, 3-O-rutinoside, citrusin C, 2,3- aphrodisiac, astringent, cholagogue, pectin. Analysis of calyces has shown the dihydro-2-(4’-hydroxy-3’-methoxyphenyl)-

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Table 1: Physicochemical constituents of the fresh calyces and 3-β-D-glucopyranosylmethyl-7-hydroxy-5- leaves of H. sabdariffa benzofuranpropanol, corchoionoside C and trans-carveol-6-O-β-glucopyranoside Constituents Calyces (fresh) Leaves (fresh) were isolated from 70% aqueous ethanol extract of leaves22. The physicochemical Moisture 9.2g 86.2 % Protein 1.145g 1.7-3.2 % analysis of the fresh calyces and leaves are Fat 2.61g 1.1 % given in Table 1 and phytochemicals Fibre 12.0g 10 % present in the various parts of the plant Ash 6.90g 1 % are presented in Table 2. Calcium 12.63mg 0.18 % Phosphorus 273.2mg 0.04 % Iron 8.98mg 0.0054 % Pharmacology Carotene 0.029mg — Antihypertensive Thiamine 0.117mg — Aqueous extract of petals Riboflavin 0.277mg — exhibited antihypertensive and Niacin 3.765mg — 23 Ascorbic Acid 6.7mg — cardioprotective effects in rats . Infusion is also found to lower both systolic and g and mg/100g diastolic pressure significantly in Table 2: Phytochemicals of H. sabdariffa spontaneously hypertensive and normotensive rats24. Part of the plant Chemical constituents Tea of calyces showed 11.2% reduction in the systolic blood pressure Flower Carbohydrates, arabinans, mannose, sucrose, thiamin, xylose, mucilage, niacin, pectin, and 10.7% decrease in diastolic pressure25. proteins, fat, arabinogalactans, rhamnogalacturans, riboflavin, β-carotene, Effectiveness and tolerability of a phytosterols, citric acid, ascorbic acid, fruit acids, maleic acid, malic acid, standardized extract was studied in hibiscic acid, oxalic acid, tartaric acid, (+)-allooxycitronic acid-lactone, allohydroxycitric-acid, glycolic acid, utalonic acid, protocatechuic acid, patients with mild to moderate cyanidin-3-glucoside, cyanidin-3-sambubioside, cyanidin-3-xyloglucoside, hypertension which revealed a reduction delphinidin, delphinidin-3-glucoside, delphinidin-3-sambubioside, in systolic and diastolic blood pressure delphinidin-3-xyloglucoside, delphinin, gossypetin, gossypetin-3-glucoside, by more than 10 per cent26. hibiscetin, hibiscin, hibiscitrin, sabdaretin, sabdaritrin, fibre (crude), resin, The aqueous extracts of the calyx fibre (dietery), minerals and ash. showed a dose-dependent decrease in β Seed Starch, cholesterol, cellulose, carbohydrates, campesterol, -sitosterol, mean arterial pressure of the rats27. The ergosterol, propionic acid, pentosans, pelargonic acid, palmitoleic acid, palmitic acid, oleic acid, myristic acid, methanol, malvalic acid, linoleic acid, extract has a vasodilator effect in the sterculic acid, caprylic acid, formic acid, stearic acid, cis-12,13-epoxy-cis-9- isolated aortic rings of hypertensive rats. octadecenoic acid, isopropyl alcohol, isoamyl alcohol, ethanol, 3-methyl-1- These effects are probably mediated butanol, fibre and minerals. through the endothelium-derived nitric Leaf α-Terpinyl acetate, anisaldehyde, β-carotene, β-sitosterol, β-D-galactoside, oxide-cGMP-relaxant pathway and β-sitosteryl benzoate, niacin, fat, isoamyl alcohol, iso-propyl alcohol, methanol, inhibition of calcium influx into vascular 3-methyl-1-butanol, benzyl alcohol, ethanol, malic acid, fibre and ash. smooth muscle cells28. Daily consumption Fruit α-Terpinyl acetate, pectin, anisaldehyde, ascorbic acid, calcium oxalate, of tea lowers blood pressure in pre and caprylic acid, citric acid, acetic acid, ethanol, formic acid, pelargonic acid, mildly hypertensive adults and may prove propionic acid, isopropyl alcohol, methanol, benzyl alcohol, 3-methyl-1- butanol, benzaldehyde and minerals. an effective component of the dietary changes recommended for people Root Tartaric acid and saponin. at risk of developing hypertension29. A

Vol 8(1) January-February 2009 79 Review Paper standardized extract has shown effective oxidation and anti-hyperlipidemia in COX-1 enzyme inhibition than COX-2 blood pressure lowering activity in fructose and cholesterol-fed rats was inhibition45. hypertensive humans. A recent double demonstrated38. It revealed that the extract blind, reference-controlled trial reduced the level of LDL and the ratio of Anticancer demonstrated significant reduction in LDL-cholesterol to HDL-cholesterol. can cause cancer blood pressure in the hibiscus group when Consumption of dried calyx ethanol cell apoptosis, especially in HL-60 cells46. compared with lisinopril30. extract reduces lipid profile in rats39. Anti-oxidative activity of anthocyanins was Hypocholesterolemic and antioxidant evaluated by their effects on LDL oxidation Hepatoprotective effects of aqueous extracts in in cell free system and anti-apoptotic Protective effects of dried flower hypercholesterolemic rats is also abilities in RAW264.7 cells47. The study extracts against oxidative stress in rat reported40. Antioxidant effects of the showed that anthocyanins of this plant primary hepatocytes were demonstrated31. aqueous extracts of dried calyx using rat may be used to inhibit LDL oxidation and Protocatechuic acid, a simple low density lipoprotein was investigated oxLDL-mediated macrophage apoptosis, phenolic compound isolated from and the study demonstrated protective serving as a chemopreventive agent. H. sabdariffa showed protective effects effect of roselle on LDL oxidation41. Inhibitory effect of protocatechuic acid on against cytotoxicity and genotoxicity of Biochemical dynamics and tumour promotion in mouse skin hepatocytes induced by t-BHP. One of hypocholesterolemic action of the plant demonstrated that protocatechuic acid mechanisms may be associated with its demonstrated that its administration possesses potential as a cancer property of scavenging free radicals32. induces significant decrease in the activity chemopreventive agent against tumour The extract of its petals protected of serum GOT, GPT, alkaline and acid promotion48. rats against cadmium induced liver, phosphatase as well as total serum protein. prostate and testis lipoperoxidation33. The These values nearly returned to the initial Other activities extract offers hepatoprotection by levels after 9 weeks of administration42. Delphinidin 3-sambubioside, a influencing the levels of lipid peroxidation Aqueous extracts of the petals of anthocyanin isolated from the dried products and liver marker enzymes in red and green plant decreases total plasma calyces of H. sabdariffa can induce a experimental hyperammonemia and this concentrations in rats indicating dose-dependent apoptosis in human could be due to the free radical scavenging cardiovascular protective effects43. leukemia cells (HL-60) as characterized property of natural antioxidants present by cell morphology, DNA fragmentation, in the plant34. Antioxidant activity activation of caspase 3, 8 and 9, and The protective effect of aqueous The antioxidant and free radical inactivation of poly(ADP) ribose extract and anthocyanins on paracetamol- scavenging effects of two fractions of the polymerase49. Ethanol and aqueous induced hepatoxicity in rats has also ethanol extract (chloroform soluble extracts of its calyces possess antipyretic been reported35. Aqueous-ethanol (1:1) fraction and ethyl acetate soluble fraction) activity in experimental animals50. extract of the calyx showed a significant obtained from its dried flowers were Ethanol extract of the plant decrease in the level of lipid peroxidation investigated44 and found that both the reduces the extent of cisplatin-induced in carbon tetrachloride induced liver fractions scavenge hydrogen peroxide sperm abnormality and enhanced sperm damage36. However, a study showed that (79-94%) at the dose of 500µg. Similarly, motility in rats51. Inhibition of intestinal prolonged usage of aqueous-methanol extract the extracts showed inhibitory (70-80%) motility by methanol extract in rats showed of the calyces could cause liver injury37. effects on superoxide anions radicals a significant dose dependent relaxant effect - (O2 ) at a dose of 1000µg. The antioxidant on rat ileal strip comparable to the effect Antihyperlipidemic activities of three varieties using liposome shown by nifedipin and papaverine as Inhibitory effects of the plant system have also been reported. Methanol reference compounds52. Investigation of extract on low-density lipoprotein and ethyl acetate extracts showed higher the antispasmodic potential revealed that

80 Natural Product Radiance Review Paper aqueous extract of calyces inhibited the crude hydroalcoholic extract showed an for his cooperation and for providing the tone of various isolated muscle appreciable enzyme-inhibiting activity required institutional facilities. preparations53. towards the angiotensin I converting Effect of zobo drink enzyme, attributable to flavones, but weak References (H. sabdariffa water extract) on the inhibiting activities towards elastase, 1. Gautam RD, Sorrel– A lesser-known source pharmacokinetics of acetaminophen in trypsin and alpha-chymotrypsin59. of medicinal soft drink and food in India, human volunteers was studied and the Antibacterial activity of Nat Prod Rad, 2004, 3(5), 338-342. results showed no statistically significant gossypetin isolated from H. sabdariffa 2. Leung AY and Foster S, Encyclopedia of changes in the absorption parameters was carried out and results revealed that Common Natural Ingredients used in Food, nd t1/2a, Ka, Tmax, Cmax and AUC0-alpha after the the activity may be due to polyphenolic Drugs and Cosmetics, 2 ed, John Wiley and administration of zobo54. nature of the gossypetin60. Sons, New York, 1996. Investigation of the anti- Investigation on nootropic acitivity of its inflammatory activity showed that its calyces in mice indicated that the extract 3. Julia F, Roselle, In: Fruits of warm climates, edited by Morton J, Miami, 1987, 281-286 extract had no effect on rat paw edema of calyces might prove to be useful (also available on http:// but had an inhibitory effect on yeast memory restorative agent in the treatment www.hort.purdue.edu/newcrop/morton/ induced pyrexia and a significant effect of dementia seen in elderly which may be roselle.html). on the hot plate reaction time55. due to its anti-acetylcholinesterase Polysaccharides from its flowers can property61. The haemostatic effect of the 4. Duke JA, Handbook of Energy Crops, 1983 (www.hort.purdue.edu/new crop). stimulate proliferation and differentiation leaves was evaluated to confirm its of Human Keratinocytes56. The study also traditional use to arrest bleeding. The 5. McCaleb S, Evelyn L and Krista M, The showed that raw polysaccharides and all extract enhanced coagulation of blood, Encyclopedia of popular , Prima acidic fractions cause a strong induction while causing precipitation of some blood Lifestyles, 2000. of proliferation of human keratinocytes material. The bleeding time was also 6. Cribb AB and Cribb JW, Wild Food in Australia, 62 while the neutral polymers were decreased . Fontana, 1976. ineffective. Neuropharmacological effects Tea made from dry roselle calyces of the aqueous extract of calyx in rodents was given to human and analysed for uric 7. Bown D, Encyclopedia of herbs and their uses, revealed that the extract produced a acid and other chemical composition Dorling Kindersley, London, 1995. remarkable dose dependent decrease in related to urinary stone risk factors. The 8. Chopra RN, Nayar SL and Chopra IC, Glossary spontaneous motor activity in mice and results suggest the urocosuric effect of the of Indian Medicinal Plants, Council of increased the duration of pentobarbital tea in human63. Scientific and Industrial Research, New Delhi, induced sleep in rats57. 1986. Anticlastogenic effects of aqueous Conclusion 9. Manandhar NP, Plants and People of Nepal, extract of fruits in bone marrow cells of The reported phytochemical and Timber Press, Oregon, 2002. 58 mice were studied . The results showed pharmacological studies support its that administration of a crude extract led traditional uses and may prove to be useful 10. Crane, JC, Roselle — a potentially important plant fiber, Econ Bot, 1949, 3, 89-103. to a significant reduction of micronuclei for clinical evaluation and development in polychromatic erythrocytes and of commercial drugs. Introduction and 11. Duke JA, The quest for tolerant germplasm, combination of H. sabdariffa and commercial cultivation of its varieties in In: ASA Special Symposium 32, Crop sodium arsenite reduced significantly the India is also recommended. tolerance to suboptimal land conditions, Am frequencies of micronucleated PCEs Soc Agron, Madison, 1978, 1-61. induced by sodium arsenite. Studies on Acknowledgements 12. Duke JA, Ecosystematic data on economic in vitro enzyme inhibitory and in vivo Authors are thankful to the plants, Quart J Crude Drug Res, 1979, cardioprotective activities revealed that a Chairman of the Institute, Mr. Parveen Garg 17(3-4), 91-110.

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13. Duke JA and Atchley AA, Proximate analysis, 2-Kidney, 1-Clip renovascular hypertension, hepatocytes, Food Chem Toxicol, 1997, In: Christie, BR (ed), The handbook of plant J Ethnopharmacol, 2003, 86(2-3), 35(12), 1159-1164. science in agriculture, CRC Press, Inc., Boca 181-185. Raton, 1984. 32. Tseng TH, Wang CJ, Kao ES and Chu HY, 24. Onyenekwe PC, Ajani EO, Ameh DA and Hibiscus protocatechuic acid protects 14. Morton JF, Is there a safer tea?, Morris Arb Gamaniel KS, The antihypertensive effect of against oxidative damage induced by tert- Bull, 1975, 26(2), 24-30. roselle (Hibiscus sabdariffa) calyx butylhydroperoxide in rat primary hepatocytes, infusion in spontaneously hypertensive rats Chem-Biol Inter, 1996, 101(2), 137-148. 15. Perry LM, Medicinal Plants of East and and a comparison of its toxicity with that in Southeast Asia, MIT Press, Cambridge, 1980. Wistar rats, Cell Biochem Funct, 1999, 33. Asagba SO, Adaikpoh MA, Kadiri H and Obi 17(3),199-206. FO, Influence of aqueous extract of Hibiscus 16. Watt JM and Breyer B, The medicinal and sabdariffa L. petal on cadmium toxicity in poisonous plants of southern and eastern 25. Faraji MH and Haji Tarkhani A, The effect of rats, Biol Trace Elem Res, 2007, 115(1), Africa, 2nd ed, E & S, Livingstone, Ltd., sour tea (Hibiscus sabdariffa) on essential 47-58. Edinburgh and London, 1962. hypertension, J Ethnopharmacol, 1999, 65(3), 231-236. 34. Musthafa ME, Perumal S, Ganapathy, 17. Vilasinee H, Anocha U, Noppawan PM, Tamilarasan M, Kadiyala BD, Ramar S, Nuntavan B, Hitoshi S, Angkana H and 26. Herrera-Arellano A, Flores-Romero S, Chavez- Selvaraju S and Govindarajaha V, Influence of Chuthamanee S, Antioxidant Effects of aqueous Soto MA and Tortoriello J, Effectiveness and Hibiscus sabdariffa on the levels of extracts from dried calyx of Hibiscus tolerability of a standardized extract from circulatory lipid peroxidation products and sabdariffa L. 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