Pharmacognosy, Phytochemistry and Pharmacology of Annona squamosa Linn -          A Review

 

Satish Kumar B.N.*, Gobinda Mohan Behera, Malay Baidya

Gautham College of Pharmacy, Sulthanpalya, R.T .Nagar, Bangalore-32, Karnataka

 

ABSTRACT:

This review gives an account of the current knowledge on the pharmacognosy, phytochemistry, and pharmacological aspects of Annona squamosa Linn. (Annonaceae

), Sugar apple. A wide range of Phyto constituents mainly alkaloids, terpenoids and phenolics, kaurane type diterpenes, quercitin and many more compounds and whose activities are been proved. Different parts of the plant have been used in traditional medicine, roots as Purgative, useful in mental depression; fruits as Haematinic, Cooling, sedative, vomiting, cough, malignant tumor and strengthening muscles; seeds as abortifacient, useful in destroying lice in the hair; bark as atonics; leaves- crushed leaves are applied on ulcers and wounds and a leaf decoction is taken in cases of dysentery. Phytoconstituents  like (-)-ent-kaur-16-en-19-oic acid and 16α,17-dihydroxy-ent-kauran-19-oic acid known to posses Anticancer activity, Cyclic peptide, Cyclosquamosin B, has Vasorelaxant activity, Annonaine possess Antifungal activity, which are consistent with the reported uses of the plant extracts in the indigenous system of medicine. Hence the present article includes the detailed exploration of morphology, phytochemistry, and pharmacological aspects of entire plant of Annona squamosa L. in an attempt to provide a direction for further research.

 

Key Words: Annona squamosa, pharmacognosy, phytochemistry, pharmacological activity.

 

INTRODUCTION:

Annona includes approximately 100 species of evergreen or semi deciduous shrubs and tree1. Archaeobotanical studies have dated exploitation and cultivation in the Yautepe river region of Mexico to approximately 1000 BC. The first botanical references to the Annona genus appeared in the 16th century and described morphologically different species2. Annona squamosa commonly known as custard apple, is a native of West Indies and is now cultivated throughout India, mainly for its edible fruits. The generic name derives from anon, a Hispaniola Taino word for the fruit3. Many of the species are used in traditional medicines for the treatment of a variety of diseases. The genus Annona is the most important source of edible fruits in Annonaceae. The name is derived from the Latin “annual harvest”. The most common Annona species dealt with Annona cherimola, Annona muricata, Annona squamosa, Annona reticulata, Annona glabra, Annona montana, Annona chrysophylla.

 

 


These species have several common names, and they need to be used with caution because some names may be applied to two or more species in different countries, or even in different regions of the same country4. Therefore the botanical descriptions, pharmacognostical and phytochemical parameter are essential to distinguish among them. Like many other tropical fruit trees and shrubs, such as mango, coconut and tamarind, the Annona are multi use plants with acceptable nutritional value as food products. They also serve as sources of medicinal and industrial products. So to explore use of the Annona genus, a review is made on one species of Annona, Annona squamosa in respect of its Pharmacognostical, Phytochemical studies and Pharmacological activities carried out on the plant.

 

Plant description:

Annona squamosa

Synonym(s) - Annona biflora Moc & Sesse, Annona cinerea Dunhal, Annona forskahlii DC 5.

Family- Annonaceae 6

The image of fruit, seed and entire plant of Annona squamosa Linn.  in Fig 1, 2, 3 respectively

 

Fig.1. Fruit of Annona squamosa

 

Fig. 2.  Seeds of Annona squamosa

 

Fig. 3. Entire plant of Annona squamosa

 

Vernacular names:

Sanskrit-Shubha, Suda, Ganda, Gutea, Gandhagatra; English- Custard Apple tree, Sweet sop of America; Hindi- Sharifah, Sitaphal; Bengali- Ata; Gujurati- Anusa; Kannada Sitaphala; Telugu- Seetapandu; Tamil-Sitaphalam; Malayam- Sirpha; Assami-Ata, Katal ;Myanmar-Amesa ; France- Attier; Germany-Zue-Kerapfel 6.

 

Scientific Classification:

Kingdom          Plantae

Division-               Angiospermis

Sub class-             Magnolids

Order-                  Magnoliales

Family-                 Annonaceae

Genus-                  Annona

Species-                 A. squamosa 7.

 

Varieties:

There are two varieties of custard apple are “Ramphal” and “Sitaphal”. The fruit with creamy colored channels on the surface and with pulp of the same color is considered superior to that with white channels and white pulp” 6.

 

Distribution:

Annonaceae is a large family consisting of aromatic trees, shrubs and lianas. In India, it is represented by 26 genera and 129 species, which are mostly distributed in the states of Andhra Pradesh, Assam, West Bengal, Tamilnadu, Uttar Pradesh and Madhya Pradesh. Annona squamosa and Annona reticulate are exclusively cultivated in India for their edible fruits. About 60% of Indian species are endemic8.

 

Parts used: Roots, leaves, fruits, seeds9.

 

Ayurvedic Medicinal Property:

Rasa: Sweet; Virya: Cold; It alleviates Pitta, aggravates Vata and kapha, is nourishing strength, giving aphrodisiac and cardiac tonic, and is useful in thirst, vomiting, nausea, burning and bleeding from internal organs 10.

 

Properties and uses: Roots- Purgative, useful in mental depression and spinal disorders

 

Fruits- Haematinic, Cooling, sedative, stimulant, expectorant and tonic. They are useful in anemia, burning sensation, vitiated conditions of pitta, vomiting, cough, malignant tumor and strengthening muscles.

 

Seeds- Abortifacient, useful in destroying lice in the hair9.

 

Bark- Used as a tonic 6.

 

Leaves- Crushed leaves are sniffed to overcome hysteria and fainting spells; they are also applied on ulcers and wounds and a leaf decoction is taken in cases of dysentery. Throughout tropical America, a decoction of the leaves alone or with those of other plants is imbibed either as an emmenagogue, febrifuge, tonic, cold remedy, digestive, or to clarify the urine. The leaf decoction is also employed in baths to alleviate rheumatic pain8.  It is used as insecticide, antiovulatory, haematinic, sedative, stimulant, expectorant and abortifacient 11.

 

PHARMACOGNOSTICAL STUDIES:

Leaf of Annona squamosa:

Microscopy

Transverse section of Folia Annona shows a dorsiventral nature. The section is broadly divided into the lamina and the midrib. The lamina of the leaf shows three distinct regions such as upper epidermis, lower epidermis and the mesophyll.

 

The upper epidermis is single layered with straight walled cells which are more or less rectangular in shape. It is continuous and coated by a waxy cuticular thickening with simple or stellate hairs. The lower epidermis is continuous and wavy cell wall interrupted by presence of stomata frequently. Simple or stellate hairs are also found on the lower epidermis. However the cuticle thickening is not very well represented. Some of the cells of the epidermis both on the upper and lower surface contain single stellate, prismatic, square or clustered crystals. The mesophyll tissue consists of palisade and spongy parenchyma. The upper palisade is made up of two layers of vertically arranged compact tabular palisade cells containing chloroplastids. Few starch grains are also seen in the palisade cells.

 

The lower bulk of the mesophyll tissue is made up of spongy tissue, which is comprised of oval and circular spongy parenchyma cells, enclosing intercellular spaces filled with air. In the spongy region there are scattered groups of sclerides with thick cell walls, which provide mechanical stability to the leaf. The spongy parenchyma cells also contain chloroplast and starch grains. Present are vascular strands with closed collateral bundles which get distributed in a reticulate fashion in the lamina. These specialized structures conduct water and food to the leaf.

 In the midrib, which is prominent, below the upper epidermis there are one or two layer of the collenchymas cells, which constitute the hypodermis. Below the upper collenchymas and above the lower collenchymas there are cells of medulla, which are parenchymatous enclosing lysigenous secretory cavities which help in the storage of mucilaginous content. There are group of sclerides in the upper part of the medulla. The vascular bundles are distributed in the form of an arc open towards the upper epidermis. The number of vascular bundles varies from 8-12. The phloem is towards the lower epidermis. Below the phloem there are sclerenchymatous fiber strands capping each vascular bundle, which enclosed by parenchyma, which has starch grains in plenty. The vascular bundles are radially traversed by interfasicular or intervascular parenchyma connecting the central part of the medulla to the outer part of the midrib.

 

Powder microscopy:

The leaf powder is grayish green or dull green in color with an unpleasant odour and mucilaginous taste. On microscopical examination the powder showed numerous sickle shaped unicellular and multicellular warty and covering trichomes which are lignified, sometimes stellate, broken and rarely collapsed. Paracytic or rubiaceous type of stomata with irregularly shaped epidermal cells are seen. Palisade cells are seen in association with mucilage ducts and veins. Prismatic and cluster calcium oxalate crystals present in sheath of cells around the fibers. A number of stone cells, which are lignified are seen isolated or in groups. Concentric starch grains are also seen. Apart from these characters, oil sacs are seen at intervals. There are also few lignified xylem vessels and non-lignified phloem cells12. The physico- chemical parameters are explained in Table No; 1,2,3,4

 

Table No. 01: Ash value and extractive value of the leaf powder of Annona squamos

Parameters

Values %W/W              

Total ash                      

8.78                      

Acid insoluble ash          

0.52

Water soluble ash          

2.03

Sulphated ash               

9.08

Carbonated ash             

6.88

Nitrated ash                

6.10

Hot extraction                           

17.92

Cold maceration

 

Water soluble extractive value                

18.62

Ethanol soluble extractive value            

08.75

Non volatile ether soluble extractive value   

3.28

 

 

Table No. 02:   Leaf constants of leaf of Annona squamosa

Parameters

Values

Vein islet number                    

16

Vein termination number             

28

Palisade ratio 

8.5

Stomata index   

14.2                                                

 

 

Table No. 03:  Physicochemical constants of leaf of Annona squamosa

Parameters 

Values

Bitterness Value                    

nil

Foaming index           

less than 100

Swelling index                

18.0

Mucilage content             

15.26%w/w

 

 

Table No. 04: Physical characteristic and percent yield of crude methanol extract of fruit and leaf of Annona squamosa 13.

 

Extract

Sharifa fruit

Sharifa leaves

Botanical name        

Annona squamosa

Annona squamosa

Nature

Sticky

Oily solid

Color

Yellowish brown

Green

Odour

Peculiar

Aromatic

% Yield

33.40

21.50

 

PHYTOCHEMISTRY:

1.      Twelve compounds were isolated from Annona squamosa. Their structures were identified as liriodenine, moupinamide, -(-)-kauran-16 alpha-ol-19-oic acid , 16 beta, 17-dihydroxy-(-)-kauran-19-oic acid, anonaine, 16 alpha, 17-dihydroxy-(-)-kauran-19-oic acid, (-)-isokaur-15(16)-en-17,19-dioicacid, squamosamide, 16 alpha-methoxy-(-)-kauran-19-oic acid, sachanoic acid, (-)-kauran-19-al-17-oic acid, daucosterol14.

2.      The qualitative phytochemical fingerprint of the methanolic extract leaf revealed the presence of alkaloids, terpenoids and phenolics, fats and waxes15.

3.      The bioactive two kaurane-type diterpenes, (-)-ent-kaur-16-en-19-oic acid and 16α, 17-dihydroxy-ent-kauran-19-oic acid from the pericarp of the fruit known to posses anticancer activity16.

4.      Phytochemical analyses including HPLC revealed the presence of quercetin in the seed extract and the results on the effects of quercetin suggested the involvement in the mediation of antithyroidal activity of Annona squamosa seed extract17.

5.      Cyclic peptide, cyclosquamosin B, from seeds of Annona squamosa has vasorelaxant activity18

6.      Eleven compounds were isolated and identified as annonaceous acetogenins: squamocenin, annotemoyin-2, reticulatain-2, squamocin-I, squamocin-B, squamocin, motrilin, squamostatin-D, squamostatin-E, cherimolin-1, cherimolin-2 from the seed of ethyl alcohol extract of A. squamosa 19.

7.      The chemical composition of the fruit pulp of Annona squamosa were found to have high (58% of dry mass), the triglyceride concentration was found to be very low. The presence of the diterpenoid compound kaur-16-en-18-oic acid in a considerable amount (0.25% of dry mass) was detected in the lipid fraction. The essential oil of the fruit pulp was obtained and its volatile constituents were identified by GC-MS. The major compounds were α -pinene (25.3%), sabinene (22.7%) and limonene (10.1%) 20.

8.      Squamocin-G and its isomer squamocin-H (asimicin) were reported to have cytotoxic activity against P-388 mouse leukemia, PC-6, lung human cancer and NUGC-3 human cancer cell lines21.

9.      Asimicin/squamocin-H, motrlin/squamocin-C Annonin III and a related compound trilobin which possess an adjacent bis tetrahydrofuran moiety also showed highly potent insecticidal activity against the yellow fever mosquito Aedes aegyptii22.

10.    The seeds of Annona squamosa also yielded monotetrahydrofuran derivatives annonacin , annonacin A 23  and annonastatin 24  and they were found to be toxic to the nematode Caenohabditis elegans and the insect Phaedon cochleariae.

11.    Squamostene-A 25, reticulacin-126 isolated from the seeds of Annona squamosa also possess a single tetrahydrofuran ring.

12.    The isolation of three compounds having one tetrahydrofuran ring exhibiting selective cytotoxic activity against certain specific human tumor cells from the bark of Annona squamosa27.A compound possessing the same molecular weight and fragmentation pattern in its mass spectrum resembling squamocin was found to be an acaricide against tropical cattle to ticks28.

13.    Cyclopeptide derivatives were also isolated from the seeds of Annona squamosa29.

14.    A saponin stigmasta-5, 24 (28)-diene-3β-ol-α-L rhamnoside was also isolated from the seeds of Annona squamosa 30.

15.    Investigation of the stem bark of Annona squamosa yielded bullatacin, bullatacinone and squamone  having an adjacent bis tetrahydrofuran moiety31 and the monotetra-hydrofuran derivatives 2,4-(cis and trans)-mosinone-A , mosin-B , mosin-C  and annoreticulone  possessing selective cytotoxic activities against some human tumor cell lines 27.

16.    The ethanolic extract of leaves and stem of Annona squamosa was found to possess anticancer activity32. Chemical investigation of the leaves resulted in the isolation of a mixture of aliphatic alcohols, a mixture of β-sitosterol, stigmasterol camposterol, 16-hentria contanone sitosterol and stigmasterol showing antibacterial activity and the flavonoids quercentin-3-0-rutinoside and quercentin-3-B-galactoside 33.

17.    The branches of Annona squamosa gave the alkaloids squamosamide, liriodenine moupinamide, annonaine, sachanoic acid and diterpenoids belonging to the kaurane group 34.

18.     Alkaloids isolated from Annona squamosa were also found to possess larvicidal and insect growth regulating and chemosterilant activities against the mosquito Anopheles stephensi at 50–200 ppm. Mortality in the larvae, pupae and adults was 52–92% 35.

19.    Phytochemical analysis of fruit of Annona squamosa also resulted in the isolation of alkaloids and several diterpenoids of  kaurane group of  which 16β, 17- dihydroxy-ent-kauran-19-oic acid showed significant activity against HIV replication in H9 lymphocyte cells36.

20.    Chemical structure of Annonaceous acetogenins from Annona squamosa seeds is in Fig. 4. Chemical structure of constituents found in Annona squamosa Linn.   fruit and seeds in Fig. 5.

 

Fig .4:  Chemical structure of annonaceous acetogenins from Annona squamosa seeds 37.

 

Fig. 5: Chemical structure of constituents found in  Annona squamosa Linn.  fruit and seeds 38-46.

 

Bis-tetrahidrofuran

 

Higenamin hydrochloride

 

PHARMACOLOGICAL ACTIVITY:

1.      Antidepressant, Analgesic activity, and Anti-inflammatory activity:

The Antidepressant, Analgesic activity, and Anti-inflammatory activity of polyherbal formulation of methanol extract of leaves of Annona squamosa, Azadiracta indica is studied on the rats, mice. Polyhedral formulation possesses potent anti-inflammatory activity and analgesic activity, as it inhibits maximum edema at 5 hrs, which was comparable to that of standard Indomethacin. Since, serotonin, histamine and prostaglandins are the major mediators of inflammation, anti inflammatory effect of polyherbal formulation could be due to inhibition of either their synthesis or release possibly due to inhibition of the enzyme cycloxygenase leading to inhibition of prostaglandin synthesis at third stage of inflammation. Based on the results of the present study, it can be concluded that polyherbal formulation showed significant anti-inflammatory activity and analgesic activity, but not significant Anti depressant activity 47.

 

2.      Anti carcinogen:

The present study was examined modifying effects of aqueous and ethanol extract of bark of Annona squamosa on glycoconjugates levels in 7,12-dimethyl benz(a)anthracene (DMBA) induced hamster buccal pouch carcinogenesis. Oral squamosa cell carcinomas were induced in buccal pouches of male golden syrian hamsters, the tumor volume and burden was also significantly increased in hamsters painted with DMBA alone as compared to control hamsters. The levels of glycol conjugates were significantly increased in plasma and buccal mucosa whereas decreased in erythrocyte membranes of tumor bearing hamsters as compared to control hamsters. Oral administration of A. squamosa bark extracts significantly prevented the tumor formation as well as reduced the incidence of pre-cancerous lesions such as keratosis, hyperplasia and dysplasia, tumor volume and burden in DMBA painted hamsters, which indicates their potent chemo preventive efficacy in experimental oral carcinogenesis. Although both aqueous and ethanolic extracts of A. squamosa bark exert chemo preventive efficacy in experimental oral carcinogenesis, the ethanolic extract was found to be more potent than that of aqueous bark extract 48.

 

3.      Hepatoprotective activity:

The ethanol extract of leaf of Annona squamosa is evaluated for Hepatoprotective effect on the mice. The levels of GOT (Glutamyl oxaloacetate transaminase), GPT (Glutamyl pyruvate transaminase), ALP (Alkaline phosphatase), ACP (Acid phosphatase), AFP (Alpha fetoprotein), Total and direct bilirubin in serum and tissue and also histopathological studies in liver are carried out in control and experimental mice. The results of bio chemical analysis and histopathological studies reveals, the plant Annona squamosa is strongly recommended in the herbal treatment of hepatic problem for effective remedy 49.

 

4.      Insecticidal/antifeedant activity:

In the present study pure acetogenins like Squamocin , Squamocin-D and a mixture of acetogenins from the seeds and pure alkaloids like (+)- O-Methyl armepavine 1 and (-) Xylopine from the leaves were isolated of Annona Squamosa. The acetogenins and alkaloids are the active principles for the insecticidal antifeedant activity. Insect antifeedant activity and the insecticidal activity of all the pure compounds isolated from Annona were assessed on Spodoptera litura (Tobacco Caterpillar) in the laboratory. The pure compounds exhibiting considerable antifeedant and insecticidal activity 50.

 

5.      Antihyperglycemic activity:

The present study investigated the possible therapeutic effects of Annona squamosa (A. squamosa) extract on certain biochemical markers in streptozotocin (STZ) –induced diabetes mellitus in rats. The effects of an aqueous extract of A. squamosa leaves on blood glucose, insulin, C-peptide, albumin, albumin/globulin ratio, urea, uric acid and creatinine and the activities of diagnostic marker enzymes aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and gamma-glutamyl transpeptidase were examined in the plasma, liver and kidney tissues .Oral administration of A. squamosa (300 mg/kg) aqueous extract to diabetic rats for 30 days significantly reduced blood glucose, urea, uric acid and creatinine, but increased the activities of insulin, C-peptide, albumin, albumin/globulin ratio and restored all marker enzymes to near control levels. Thus present results shown that A.squamosa extract has an antihyperglycaemic effect and consequently may alleviate liver and renal damage associated with STZ-induced diabetes mellitus in rats 51.

 

6.      Anti diabetic and Anti Oxidant activity:

The antioxidant effect of oral administration of aqueous extract of Annona squamosa (A. squamosa) leaf on blood glucose, haemoglobin, glycosylated haemoglobin, plasma insulin, antioxidant enzymes and lipid peroxidation in liver and kidney to streptozotocin (STZ)-induced diabetic rats is been analyzed. The A. squamosa aqueous extract supplementation is useful in controlling the blood glucose level, improves the plasma insulin, lipid metabolism and is beneficial in preventing diabetic complications from lipid peroxidation and antioxidant systems in experimental diabetic rats 52.

Antidiabetic activity of aqueous leaf extract of Annona squamosa is evaluated in type 2 diabetic rats.  Diabetes mellitus was induced with streptozotocin–nicotinamide and graded doses of the aqueous leaf extracts were then administered in drinking water to normal and experimental diabetic rats for 12 days. Fasting plasma glucose levels, serum insulin levels, serum lipid profiles and changes in body weight were evaluated in normal rats while liver glycogen levels and pancreatic TBARS levels were evaluated additionally in diabetic rats. The diabetic groups treated with the aqueous leaf extract were compared with standard glibenclamide. The findings of the study support the antidiabetic claims of Annona squamosa 53.

 

7.      Antihead lice activity:

The separation and identification of the active compounds against head lice from the hexane extract of Annona squamosa L seed. Chromatographic and spectroscopic techniques revealed that two major compounds of the hexane seed extract were oleic acid and triglyceride with one oleate ester. The compounds were tested in vitro against head lice, comparing to the crude hexane extract of the seed. The triglyceride with one oleate ester and the crude hexane extract diluted with coconut oil 1:1. These compounds were found to kill all tested head lice in 49, 11 and 30 minutes, respectively. The triglyceride with one oleate ester was the most active compound against head lice. The triglyceride ester can be used as a marker for quantitative analysis of the active compound for quality control of the raw material A. squamosa seed and its extract54. Antihead lice activity of ethyl acetate of Annona squamosa L seed is been evaluated 55.

 

8.      Hypoglycemic and Antidiabetic activity:

The aim of study was to demonstrate the hypoglycemic and antidiabetic activity of the water extract of leaves of Annona squamosa in alloxan (80 mg/kg bw)-induced diabetic rabbits and streptozotocin (STZ) (50 mg/kg bw)-induced diabetic rats. The water extract of leaves of A. squamosa at a dose 350 mg/kg showed antidiabetic activity in two species of animals, namely rabbits and rats with induced diabetes. In the case of alloxan-induced diabetes in rabbits, a significant reduction in FBG and improvement in glucose tolerance, fall in blood glucose at 1 h and 2 h during GTT was observed. In STZ diabetic rats also, there was decrease in FBG, and reduction in blood glucose during GTT. It brought about fall in the levels of total cholesterol with increase of high density lipoprotein (HDL) cholesterol and fall in low density lipoprotein (LDL) cholesterol, including decrease in triglyceride (TG) levels. The glycosylated haemoglobin level (HbA1c) was reduced by with a increase of total haemoglobin. Extract enhanced the serum insulin level in diabetic animals during GTT and insulin release from isolated pancreatic islets. Thus present study reveals that A. squamosa has both hypoglycemic and antidiabetic activity 56.

 

9.      Histological alteration in liver:

The present study was aimed to evaluate the effect of aqueous leaves extract of Thai  Annona  squamosa L. at different doses to the histological  alteration of the livers in normal and STZ-induced diabetic rats. The histological study implies that Annona  squamosa L. leaves extract is not toxic to normal liver tissue, meanwhile promotes recovery of diabetic liver tissue in dose-dependent manner. The improvement of histological morphology of liver in diabetic rat received aqueous leaves extract of Annona  squamosa L. is probably explained by its hypoglycemic effect caused from anti-oxidant activities of its flavonoids, thus decreasing the number of beta-cell injury and reducing hyperglycemic condition. The mucilage obtained from the extract may absorb the blood glucose and unknown active ingredients stimulate either the pancreatic insulin secretion from the existing beta-cells or its release from the bound form. In addition to the liver histological improvement caused by hypoglycemic effect, the anti-oxidant properties of the extract itself may also directly improve the histological features of the liver by free radical scavenging ability. This study indicates that the aqueous leave extract of A. squamosa could improve the histological morphology of the livers of diabetic rats 57.

 

10.       Larvicidal and chemosterilant activity:

Alkaloids isolated from Annona squamosa have shown larvicidal growth-regulating and chemosterilant activities against Anopheles stephensi at concentrations of 50 to 200 ppm. Adults exposed as larvae to different treatments showed reduced fecundity and fertility in females. Mortality in the larvae, pupae and adults produced about a 52-92% decrease in the laboratory experiment. The total developmental period was slightly reduced from the control. Treatment with the alkaloids had a significant effect on the mortality, emergence and reproductive physiology of Anopheles stephensi 35.

 

11.    Anti cancer:

Various solvent extracts of Annona squamosa fruit pericarp is tested for cytotoxic activity using in vitro cultures of Dalton’s lymphoma cells as well as HeLa cells. Cytotoxicity was detected by the Trypan blue exclusion test and induction of apoptosis was evaluated by [3-(4,5-Dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide] assay (MTS assay) and DNA ladder assay. The chloroform extract of Annona squamosa pericarp was found to be cytotoxic to the different cell lines tested. The inhibitory concentration required for 50% cytotoxicity (IC50) was also determined. This study suggests the potential of Annona squamosa fruit pericarp for the development of modern medicine for the treatment of cancer 16.

 

12.    Hyperthyroidism and lipid-peroxidation:

The seed extract of Annona squamosa was evaluated for its possible ameliorative effect in the regulation of hyperthyroidism in mouse model. Serum triiodothyronine ([T.sub.3]), thyroxine ([T.sbu.4]) concentrations, hepatic glucose-6-phospatase (G-6-Pase) and 5'-mono-deiodinase (5'DI) activity were considered as the end parameters of thyroid function. Simultaneously hepatic lipid peroxidation (LPO), superoxide dismutase (SOD) and catalase (CAT) activities were investigated to observe its hepatotoxic effect-[T.sub.4] administration (0.5 mg/kg/d for 12 days, i.p.) increased the levels of serum [T.sub.3] and [T.sub.4], activity of hepatic G-6-Pase, 5'DI and LPO with a parallel decrease in SOD and CAT activities. However, simultaneous administration of the Annona seed extract (200 mg/kg) or quercetin (10mg/kg) to [T.sub.4]-induced hyperthyroid animals for 10 days, reversed all these effects indicating their potential in the regulation of hyperthyroidism. Further, the seed extract did not increase, but decreased the hepatic LPO suggesting its safe and antiperoxidative nature. Quercetin also decreased hepatic LPO. When relative efficacy was compared with that of propyl thiouracil (PTU), a standard antithyroidic drug, experimental seed extract appeared to be more effective17.

 

13.      Mosquitocidal activity:

Methanolic extract of leaves of A. squamosa was tested for Mosquitocidal effect against Culex quinquefasciatus. A liquid mosquito insecticide formulation was prepared with the extract (1, 3 and 5 %w/w) using deodorized kerosene as solvent and investigated for its knock-down and 24 hr mortality. The extract formulation produced dose dependent activity, exhibited significantly shorter knock down KD50 and KD90 values and produced significant mortality. The results suggest the potential Mosquitocidal effect of A. squamosa on Culex quinquefasciatus 58.

 

14.    Larvicidal activity:

Acetogenins isolated from the seeds of Annona squamosa shows a number of biological activities. In the present study acetogenins have shown larvicidal and growth regulating activities against Anopheles stephensi at concentrations of 1 to 2 mg. Fall in population as a result of mortality of larvae, pupae and adults ranged from 79-86% as compared to control. The average larval, pupal and developmental periods increase with the increase in the concentration of acetogenins. Further studies are needed to recommend the acetogenins of A. squamosa for mosquito control and to establish the cause of mortality 59.

 

15.    Antiabortifacient activity:

The purpose of present study was to investigate A. squamosa seed aqueous extract, in doses higher than that popularly used to provoke abortion, interferes with reproductive performance, and to correlate the ingestion of this extract with possible alterations in rat embryonic implantation. Doses of 300 and 600 mg/kg body wt. were administered by gavage, during days 1 to 5 of pregnancy (Pre implantation period). Treatment of dams during the pre implantation period showed no signs of toxicity, and no alteration in the corpora lutea, implantations and embryo in terms of development numbers. Thus, that treatment with the aqueous extract of A. squamosa seeds at the different doses tested, resulted neither in morphological changes of the endometrium, reflected in the viable embryonic implantation, nor in interference with the reproductive performance of pregnant rats 60.

 

CONCLUSION:

In this review, authors presented information about the botanical description, traditional uses of Annona squamosa L., pharmacognostical studies of leaf, phytochemistry and pharmacology studies of various parts of Annona squamosa (Annonaceae), a medicinal plant found in central and southern Europe, western Asia and the very frequently in southern Mexico, Bahamas and Bermuda, and occasionally in southern Florida and also found in India. A variety of phytochemical such as terpenoids, flavonoids, quinones, volatile oil, and others have been reported to be present in this plant. It exhibits several pharmacological activities Anti-cancer, Anti-inflammatory, Hepatoprotective, Antidiabetic and Antihyperglycemic, Antioxidants, Analgesic and other Pharmacological activity. It is potentially an important medicinal plant for mankind.

 

ACKNOWLEDGEMENT:

The authors wish to thank Management, Gautham college of Pharmacy, Bangalore for encouraging and providing facilities to collect the information on this plant.

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4.       Hui YH, Chen F, Nollet MLM, Raquel PFG and Fernando LP Pessoa. Ph. Handbook of Fruit and Vegetable Flavors. John Wiley & sons Inc, Canada. 2010; pp. 232- 233.

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Received on 05.01.2011

Accepted on 06.03.2011     

© A&V Publication all right reserved

Research Journal of Pharmacognosy and Phytochemistry. 3(3): May- June 2011, 93-102