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INVESTIGATION ON THE EFFECT OF METHANOL EXTRACT OF carica papaya ON THE ISOLATED RAT RECTUM
The crude methenol extract of Carica papaya leaf was prepared using the method of Coke and Rice (1965)
Studies carried out on isolated rectum muscle of albino rats (1978-250g) showed that the methanol extract of the Carica papaya leaf causes contradiction.
The contractile effects of Carica papaya extract on the rat rectum are investigated in the presence of mepyramine (antihistamine), propranolol (B-adrenoceptor blocker), phentolamine (alpha – adrenoceptor blocker), and atropine (Acetycholine myscurine receptor blocker).
Atropine (5×10 -6-5×10-5m) and phentolamine (5×10-7–10-4m) has no significant effect on the contratile responses, while propranold (5×10-7–10-4m) and Mepyramine (5x 10-7 -2.5×10-5m) inhibited these responses to papaya extract.
These results show that propranolol and mepyramme are the more potent antagonist of papaya extract than any other adrenergic or chlonergic blocker.
The effect of adrenaline on the rat rectum was effect of adrenaline on the rat rectum was also investigated, and it revealed that adrenaline relaxed the tissue and inhibited spontaneous activity.
1.1 Carica papaya
The Carica papaya is a member of the family caricaceae, a small dicot family of four genera and thirty-one species. This family consists of small trees with usually unbranched trunks, thin bark and soft wood. The leaves are only on the upper protion of the trunck and are simple and usually palmately lobed. Flowers are unisexual or bisexual palmately lobed. Flowers are unsexual or bisexual, radially symmetrical; sepals 5, petals 5. The fruit is a berry, large and melon – like. The flowers are of various types according tyo whether the palnt is staminate, pistillate or polygamous with bisexual and unisexual flowers on the same individual as follows:
Stamainate plants-flowers in long dangling recems; stamens 10, in 2 series and are sessile.
Pistillatye plants – A(type A) – flowers several in each leaf axil, fruit is globes to avoid or perashaped. (Type B) – flowers in comymbs; fruits elongated and cylindrical.
Polygamous plants – (type A_ – corolla tube is long, the 10 stamens ae sessile and attached in corolla throat. (type B) – corolla type is very short, the 5 statmens have long filaments.
The four genera and number of included species are namely the carica 22. The Jarilla 1, thye Jacaratia 6 and the cylicomorpha 2 (Lymen, 1979). The first three are indigenous in tropical America, the last in equatorial Africa (Bedillo, 1971).
The seeds and leaves of Carica papaya have been reported to contain many active ingredients. These include the following:-
Chloline – as the most abundant basic constituent in the leaves of Nigerian variety of papaya (organ, 1971) tang (1979), however, reported that the effects of the methanol papaya extract on guinea pig uterine tissue was probably due to the we4ll known stimulant action of acetyicholine on smooth muscles. As a drug, choline (CH)+3 NCH2CH2OH.OH– has an effect similar to that of parasympathetic stimulation.
Benzylglucosinolate – from the latex (Tang, 1979) and has a germicidal effect.
Ascorbic acid – is usually more abundant in the leaves than in the seeds of Carica papaya. Many workers have reported the effects of ascorbic acid on smooth muscles. These include stimulation of he guinea pig ileum (Basu et. al., 1940) potentiation of electrically induced conractions of guinea pig intestinal muscle (Friedman, 1941) and a complec stimulator effect on isolated longitudinal smooth muscle of the guinea pig ileum (Dawson, 1961; Joiner, 1973). Ascorbic acid is obtained from the leaves, seeds and fruits of Carica papaya (Wenkam and miller, 1965). Joiner (1973) found that sodium ascorbatye had a complex stimulatory action on the guinea pig isolated ilea longitudinal smooth muscle. He also observed that magnesium ion blocked this action. He showed that at least three stimulatory actions of ascorbic acid on ileal smooth muscle occur.
In its biochemical function, ascorbic acid, (Mw 176.14). a water –s soluble levorolatory vitamin clearly acts as a regulator in tissue respiration. Its physiological roles have been classified in direct and indirect effects (Lewin, 1976). Direct effects include, inter alia, association of phosphoidesterase (PDE) with ascorbate resulting in adverse effects on the hydrolysis of cyclic adenine monophesphrate (cyclic AMP) by HD PDE. Indirect effects are mediated through affecting the structure, or concentration levels, of another substance which in turn gives rise to particular physiological effects. Inhibition of increased PDE activity has been reported to enhance relaxation of smooth muscle activity.
Carica Xanthine – is also present in Carica papaya in varying but appreciable concentrations (cobley * steele, 1976; Samson, 1980) believed to be B-carotene (a carotene) in being an oxygenated carotenoid, though this does not explain its hydrophobicity evident in its solubility property (Table 5).
Papain – the latex of the papaya plant contains the proteolitic enzyme, papain, which strongly resembles pepsin in odour, taste and appearance (Arieve, 1975) this has the property of coagulating milk and softening flesh. It is thus used for tenderizing meat, and in exfoliate cytology for detecting stomach and intestinal ulcers (Becker, 1958) the leaves are used as a substitute for soap (Grieve, 1975) and for dressing foul wounds. In Ghana, red infusion of the dried leaves is drunk to cure stomach troubles (Irvine, 1930) while the dried older leaves are smoked like tobacco (Irvine, 1961)
Volatile components – these components are responsible for the fresh ripe odour of papaya fruit. Examples are esters, aldehydes, alcohols, ethers, and ketones (Robert et. al, 1977).
Alkaloids – More interestingly papaya contains several macrocyclic lactonic alkaloids of carparine family with Unique structures. Carpaine (C28H 50N 2 04) has been reported in all green parts and seeds of papaya. It is a secondary amide (Tang, 1979) with the properties of a lactone. The common belief that carpaine is the major alkaloid in papaya leaves has been questioned in recent study (Tang, 1979).
Tang, isolated two new carpaine analogues, dehydro carpaine I and dehydrocarpaine II from the alkaloidal extract of the dired leaves of Carica papaya. Carpaine appeared to be the last prominent alkaloid amongst the three. Carpaine (MW 478.72) is a dimer of carpamic acid (c14H27 No3), it is a macrocyuclic dilactone with two piperidine units incorporated into the 26-membered ring (Hill, 1970); Tang, 1979). First isolated in 1890 from papaya leaves by Greshoft, carpaine and several other macrocgiclic lactones now represent an increasingly important class of biologically active loleculrttes (Corey et. al., 1975). It depresses auricular contractions and ventricular contractions without interfering with conduction until the contraction is sufficient to stop the heart. This contraction sufficient to stop the heart. This cardiac depression is sufficient to determines a lowering of blood pressure (taffley and Williams, 1951). This cardivoscualar effect was confirmed at the University of Hawaii when it was found that carpaine has a dose-dependent effect on lowering the blood pressure and heart rate of the rat (Hornick et al,. 1978) in addition at amobiccial and antibacterial properties, it also possess activities which on the on hand can be compared to digitalis (burdick, 1971); Grieve, 1975) and on the other hand with emetine (webb, 1948; Burdick, 1971).
To and kru (1934) reported that carpaine was a potent amoebicide effective for amoebic dysentery. Ramsawamy and siri (1960) found that it inhibited mucobaterium tubere culosis at the low dilution of 10–m. Henry et. al; (1929) stated that it is a heart poison capable of lowering pulse frequency and depressing central nervous system. Carpaine hydrochloride has been used in cardiac disease in oral doses of 0.01-0.02 and at hypodermic doses of 0.006-0.01g daily. Watt et al; (1962) have also suggested carpaine in the treatment of hypertension, a dose of 20mg/day has an action like digitalis.
The stereoisomer of carpaine (Pseudocar paine, C28H 50N204)) was found in very small quantity by Govindachari et. al, (1965). It difers from Carpaine in melting point, rotation of planepolaized light, and solubility. The common belief that caarpaine is the major alkaloid in papaya leaf (rapoport, 1956) has been questioned, as was said above. The finding of two triangle, ( ) – piperideines, dehydro-carpaine I (C28H48N204) as the major papaya alkaloids (tang, 1976) raises the possibility that the two dehydrocarpaines are intermediary metabolites in the Carpaine biosynthesis pathway (Tang 1979). The medicinal uses of Carica papaya in different parts of the work was compiled by Tang (1979) and shown in the Table.
1.2 RECTUM OF RAT
The rectum of the rat is a narrow tube, which is a continuation from the colon or large intestine. The rectum is dilated at intervals by the pellet-like faeces. The rectum of rat has all the four coatism, namely; tunica mucosa, tunica sub mucosa, tunica muscularis and tunica externa.
The tunica mucosa has a single layer of colummar epithelium. The crypts of lieberkurn have more of argentaffin cells. There is more of lymphoid tissue in the maina propria of the tunica mucosa and muscularis mucosas is not well developed.
The turnica sub mucosa is the usual two layers of smooth muscle fibres.
The turnica externa is a serosa.
Unlike in man, the rat rectum is produced into leaf-like villi. The Crypts of lieberkugn are longer than those of the colon, but their cells are only of the goblet type. The rectum has longitudinal and circular folds on its inner lining.
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