A Contrastive Phytopharmacological Analysis of Gala and Fuji Apple

 

Shoaib Ahmad, Tarique Mahmood, Ranjan Kumar, Paramdeep Bagga, Farogh Ahsan, Arshiya Shamim, Abdullah Ansari, Mohammad Shariq, Saba Parveen

Faculty of Pharmacy, Integral University, Lucknow

 

ABSTRACT:

Plants have been utilized for wellbeing and therapeutic purposes for a few a huge numbers of years. The quantity of higher plant species on earth is around 250000. It is assessed that 35000 to 70000 species have, at some time, been utilized in certain societies for therapeutic purposes. A dominant part of the total populace in developing nations still depends on natural prescriptions to meet its wellbeing needs. Natural prescriptions are regularly used to give first-line and fundamental wellbeing need, both to individuals living in remote zones where it is the main accessible wellbeing administration, and to individuals living in poor regions where it offers the main reasonable cure. Indeed, even in territories where present day medication is accessible, the enthusiasm on herb grown prescriptions and their usage have been expanding quickly as of late. Phytochemicals including phenolics, flavonoids and carotenoids from foods grown from the ground may assume a job in lessening interminable sickness chance. Apples (Malus domestica) (Family - Rosaceae) are generally devoured, rich wellspring of phytochemicals, and the plant has been considered for its different pharmacological exercises like antioxidant, anti-proliferative, anti-depressant, against microbial, restraint of lipid oxidation and Cholesterol-lowering agent. Malus domestica has an incredible viewpoint for the treatment of infections like acid neutralizer, hostile to diarrheal, delicate purgative, diuretic and depurative, hearing misfortune etc. Further studies and examinations can be performed on the plant for its different pharmacological potential. This present review gives a detail information regarding describe active constituents, therapeutic uses and pharmacological activities of both species of Malus domestica i.e Gala and fuji apple.

 

 

INTRODUCTION:

The diverse flora and fauna of the planet earth have offered the treatment of various diseases in human beings since ancient history. Among these herbs are the prominent sources of medicines across the globe. Traditionally they have been used to cure, prevent or treat diseases¹. Traditional systems of medicine continue to be widely practiced in both rural and urban areas. Population rise, inadequate supply of drugs, prohibitive cost of treatments, side effects of several allopathic drugs and development of resistance to currently used drugs for infectious diseases have led to increased emphasis on the use of plant materials as a source of medicines for a wide variety of human ailments².

 

Apple belongs to the Rosaceae family, subfamily of Maloideae and genus Malus. The common cultivated apple, Malu domestica, is believed to be generated in central Asia and to be an interspecific new generation complex of European apple Malus sylvestris and Asian species Malus dasyphyllus and Malus praecox³.

 

It is one of the most widely cultivated tree fruits, and the most widely known of the many members of genus Malus that are used by humans. Apples grow on small, deciduous trees. The tree originated in Central Asia, where its wild ancestor, Malus sieversii, is still found today. Apples can be consumed fresh, but they are also a valuable raw material for processing into apple juice, concentrates, canned, frozen, dried, and stewed fruits, jellies, purée and cider⁴.

 

Apples (Malus sp., Rosaceae) are a rich source of nutrient as well as non-nutrient components and contain high levels of polyphenols and other phytochemicals. Main structural classes of apple constituents include hydroxycinnamic acids, dihydrochalcones, flavonols (quercetin glycosides), catechins and oligomericprocyanidins, as well as triterpenoids in apple peel and anthocyanins in red apples⁵.

 

Apples contain many flavonoids and phenolic acids. Apples constitute one of the basic sources of antioxidants. Epidemiological studies have linked the consumption of apples with reduced risk of some major diseases such as cancers, cardiovascular disease, asthma, and diabetes coronary atherosclerosis, obesity^6,7. Traditional fruits (especially apples) and vegetables have many healthy properties. The positive influence of these natural products is attributed to their bioactive compounds: dietary fiber and antioxidants, mainly phenolic compounds, flavonoids, phenolic acids⁸.

 

As it has been shown, diets rich in dietary fiber and other bioactive substances have decreased the risk of civilization diseases⁷. Others compared with apple flesh; apple peel shows more potent antioxidant activity and antiproliferative activity⁸. It is well known that phenolic compounds possess antioxidant properties and prevent the oxidation of low density lipoprotein cholesterol (LDL-C)⁹. Apples and apple juice contain nutrient as well as non-nutrient components, including dietary fiber, minerals, and vitamins, as summarized in Table 1 with exception of protein levels, fiber, and natural vitamin C contents, the average nutrient composition of apples and apple juice¹⁰.

 

This review was prepared by searching the various databases like pubmed, science direct and google scholar and visited various relevant websites. The aim of this review is to compile all the phytochemical and pharmacological information regarding Malus domesticus and its various species.  

 

Table: 1 Distribution of Nutrients (fresh fruit)

Nutrients: Content per 100 g
Energy 229 kJ (54 kcal)	Vitamins	Tyr 5 mg
Water 85.3 g	Carotene 45 µg	Val 12 mg
Protein 0.3 g	Vitamin E 490 µg
Lipids 0.4 g	Vitamin K 0-5 µg	Carbohydrates
Carbohydrate 11.8 g	Vitamin B1 35 µg	Glucose 2210 mg
Carbohydrate 11.8 g	Vitamin B2 30 µg	Fructose 6040 mg
Fiber 2.3 g	Nicotinamide 300 µg	Sucrose 2470 mg
Minerals 0.3 g	Pantothenic acid 100 µg	Starch 600 mg
	Vitamin B6 45 µg	Sorbit 510 mg
Minerals	Biotin 1-8 µg
Sodium 3 mg	Folic acid 7 µg	Lipids
Potassium 145 mg	Vitamin C 12 mg	Palmitic acid 50 mg
Magnesium 6 mg		Stearic acid 10 mg
Calcium 7 mg	Amino Acids	Oleic acid 20 mg
Manganese 65 µg	Arg 8 mg	Linolic acid 100 mg
Iron 480 µg	His 6 mg	Linoleic acid 20 mg
Copper 100 µg	Ile 10 mg
Zinc 120 µg	Leu 16 mg	Other
Phosphorus 12 mg	Lys 15 mg	Malic acid 550 mg
Chloride 2 mg	Met 3 mg	Citric acid 16 mg
Fluoride 7 µg	Phe 9 mg	Oxalic acid 500 µg
Iodine 2 µg	Thr 8 mg	Salicylic acid 310 µg
Selenium 1-6 µg	Trp 2 mg	Purines 3 mg

 

Apples are popular because of the many ways that they can be consumed and because of their convenience and durability. Apples may be eaten off the tree or stored for up to a full year. Apples can be processed into sauce, slices, or juice and are favored for pastries, cakes, tarts, and pies¹¹. The pulp has been processed into candies (fruit leathers) and used as a source of pectin. The juice can be consumed fresh, either natural or filtered, fermented into alcoholic beverages such as cider or wine, distilled into brandy, or transformed into vinegar. Apples have become the symbol of wholesomeness: “An apple a day keeps the doctor away” is a favorite aphorism, and apple pie has become a symbol of goodness along with motherhood. Finally, crabapples, grown for their attractive flowers, foliage, and fruit, are among the most popular of ornamental trees (Figure 1). The use of apple in treatment of various ailments in traditional system of medicine has been implemented since centuries Table 2.

 

Table 2: Traditional uses of Malus domestica

S.no.	Parts	Activity	Reference
1.	JUICE	Anti- Alzheimer and haemorrhoids	12
2.	FRUITS	Anti-parkisons, anti-daibetes and weight loss, gallstones.	13, 14, 15
3.	PEEL	Anti-cancer (pancreatic, colon, breasts )	16, 17
4.	FIBER	Anti-diarrhoea and constipation, irritable bowel syndrome, immune system, cataracts, liver disease	18, 19

 

Common apple varieties grown in India include:

Red delicious:

A mid-season apple grown in Himachal Pradesh. This variant, along with Royal Delicious, are the most widely grown types in India.

Golden delicious: A late-season cultivar gown in Jammu and Kashmir, and Himachal Pradesh.

McIntosh: A reddish pink apple with a golden blush grown in Uttar Pradesh and Himachal Pradesh.

ChaubattiaAnupam: A red and yellow-striped apple grown in Uttar Pradesh

LalAmbri: A reddish yellow apple grown in Jammu and Kashmir. Some exotic (often imported) varieties are as follows:

Fuji                                                                                           

Royal Gala (from New Zealand)

Washington Red: American variety

Granny Smith: American variety

Chilean

These are but a handful of the 700 varieties grown in the country, which too is but a small number: one could eat an apple every day for the next 55 years before sampling all of the varieties available in the world. Scientific classification of Malus domestica has been mentioned in Table 3.

 

Table 3: Scientific classification Malus domestica
Kingdom	Plantae
Subphylum	Euphyllophytina
Infraphylum	Radiatopses
Order	Rosales
Superorder	Rosanae
Subclass	Magnoliidae
Family	Rosaceae
Tribe	Pyreae
Genus	Malus
Species	M. domestica

 

Vernacular name:

English-Apple

Gujarati-Safarjan

Hindi, Oriya-Sev

Kannada-Sebu

Kashmiri-Tsoonth

Marathi-Safar Chad

Malayalam-Epal

 

Characteristics:

Plant: Small and deciduous, reaching 3 to 12 meters (9.8 to 39 ft) tall, with a spreading canopy. Size and shape of the plant mainly depends on rootstock and training system.

 

Leaves:

Color: Dark green

Size: 5-12 cm long and 3-6 cm broad.

Shape: simple oval, arranged alternatively elliptical with serrate margin with an acute tip.

Blossoms:Blossoms are produced in spring simultaneously with the budding of the leaves.

Flower

Color: White in color with pink tinge that gradually fades and five petals.

Size: 2.5-3.5 cm in diameter.

Fruit:

Size: Typically ranges from 5-9 cm in diameter.

Color: Different in color, it depends on various species. The center of the fruit contains five carpels arranged in a five point star, each carpels containing 1-3 seeds²⁰.

 

Figure 1. Diagram of Malus domestica, flower, plant and fruits and seed and leaves

 

Types:

Gala Apple: The Gala, being one of the relatively recent introductions, sometimes is called a "gourmet apple”. One of the most widely grown apple varieties in the world, because it is available year round from northern and southern hemisphere suppliers. One of the unique features of Gala is that it can be grown with good quality results in both temperate and warm apple-growing regions, and it is generally regarded as a low-chill variety, Perhaps the flavor does not quite live up to that promise, but this is still a high quality apple with the potential to deliver really good flavor, particularly when home grown (Figure 2a) (Table 4).

 

Fuji Apple: Fuji apples are a relatively new variety. They were first bred in Japan in the late 1930s, but were only brought to the world market in 1962. They’re the result of a successful cross between two American varieties, Red Delicious and Virginia Ralls Janet. They are known for their sweetness, Fuji apples have one of the highest sugar contents of apples on the market at about 14g of sugar per 100g. Apple peel is a good source of pectin, a form of soluble fiber. Pectin can help lower cholesterol and blood sugar levels. Crisp fresh Fuji apples are at their sweet juicy peak between April and October. One large Fuji can give you 15 per cent of your daily vitamin C (Figure 2b) (Table 4).

                               Gala Apple                      Fuji Apple

 

 

 

Figure 2 (a) image of Gala Apple (b) Fuji Apple

 

 

Table 4: Common chemical constituents of Gala and Fuji apple

Name of constituents	Category	Gala	Fuji
Gentisic acid	Insoluble-bound phenolic acids	0.050 ± 0.01	0.026 ± 0.02
Protocatechuic acid	Free phenolic acids	0.634 ± 0.09	1.723 ± 0.01
	Insoluble-bound phenolic acids	0.055 ± 0.01	0.051 ± 0.00
Gallic acid	Free phenolic acids	0.065 ± 0.01	0.0804 ± 0.08
	Esterified phenolic acids	0.175 ± 0.04	0.061 ± 0.10
Caffeic acid	Esterified phenolic acids	0.062 ± 0.04	0.046 ± 0.00
	Insoluble-bound phenolic acids	0.033 ± 0.00	0.025 ± 0.00
Sinaptic acid	Free phenolic acids	0.009 ± 0.08	0.633 ± 0.01
	Esterified phenolic acids	0.140 ± 0.10	0.115 ± 0.03
	Insoluble-bound phenolic acids	0.021 ± 0.01	0.026 ± 0.00
Ellagic acid	Esterified phenolic acids	0.055 ± 0.01	0.059 ± 0.01
Total phenolics	Free phenolic acids	29.11	16.03
	Esterified phenolic acids	53.75	48.29
	Insoluble phenolic acid	11.08	4.06

 

Phytochemistry:

Apples contain a variety of phytochemicals, including quercetin, catechin, phloridzin and chlorogenic acid, all of which are strong antioxidants. The phytochemical composition of apples varies greatly between different varieties of apples, and there are small changes in phytochemicals during the maturation and ripening of the fruit. Storage has little to no effect on apple phytochemicals, but processing can greatly affect apple phytochemicals⁵. The compounds most commonly found in apple peels consist of the procyanidins, catechin, epicatechin, chlorogenic acid, phloridzin, and the quercetin conjugates. In the apple flesh, there is some catechin, procyanidin, epicatechin, and phloridzin, but these compounds are found in much lower concentrations than in the peels. Chlorogenic acid tends to be higher in the flesh than in the peel²¹. The main constituents that contribute to the apples vast usefulness and great taste are hard to narrow down. Over 20 have been documented in the unpeeled fruit alone to contribute a vast amount of biological activities. Those with known biological activities located in either the fruit or peel or both are: Alpha-Linolenic-Acid, Asparagine, D-Categin, Isoqurctrin, Hyperoside, Ferulic-acid, Farnesene, Neoxathin, Phosphatidyl-Choline, Reynoutrin, Sinapic-acid, Caffeic-Acid, Chlorogenic-acid, P-Hydroxy-benzoic-acid, P-Coumaric-acid, Avicularin, Lutein, Quercitin, Rutin, Ursolic-acid, Protocatechuic-acid, and Silver. In addition to these phytochemicals, the whole fruit contains many more for which the biological activity is not yet known. Many of the benefits of the apple come from enzymes and flavonoids⁵. Polyphenol molecule concentrations range in seed, peel and peel + flesh. Data

 

 

Figure 3: Shows location of active constituents in various part of apple fruit

 

In one medium apple weighing about five ounces the following constituents of vitamins and minerals are found: Vitamin A, B1, B2, and B6, Niacin, Pantothenic acid, Folic acid, Vitamin C and Vitamin E, Calcium, Copper, Iron, Magnesium, Manganese, Phosphorus, Potassium, Selenium, Sodium, and Zinc. The fats in the apple contain no cholesterol. Instead they are a blend of lipids, saturated, unsaturated and monounsaturated fats. In addition to fats, the apple contains the other macronutrients of proteins, and carbohydrates. Other phytochemicals include; Tryptophan, Threonine, Isoleucine, Leucine, Lycine, Methionine, Cystine, Phenylalanine, Tyrosine, Valine, Argenine, Histidine, Alanine, Aspartic Acid, Glutamic Acid, Glycine, Proline, and Serine, and trace amounts of Boron and Cobalt. There are four to five grams of soluble and insoluble fiber per apple. This fiber is from cellulose, pectin and lignin. The sugars of fructose and sucrose make up about 9-12% of the fruit and give it its sweet taste, while the tartness comes from the malic, tartaric, and citric acids (Figure 3). The tannins, making up 0.2%, give it an astringent cooling and thirst-quenching effect. Amygdaline, naturally occurring cyanide is found in the seeds⁵. An individual chemical constituent of Gala and Fuji apple has been summarized in Table 5.

Table 5: Individual chemical constituents of Gala and Fuji apple

Chemical constituents	Category	Gala	Fuji
Vanillic acid	Esterified phenolic acids	0.044 ± 0.02	-
O-coumaric acid	Esterified phenolic acids	0.028 ± 0.02	-
Quinic acid	Free phenolic acids	0.032 ± 0.01	-
Ellagic acid	Esterified phenolic acids	0.055 ± 0.01	-
Chlorogenic acid	free phenolic acids	-	0.655 ± 0.90
Chlorogenic acid	free phenolic acids	-	1.147 ± 0.40 were re- elaborated from22, 23

 

Table 6: Structure of chief chemical constituents Malus domestica

Chemical constituents	Chemical formula	Chemical structure	Reference
α-Linolen-Acid	C18H30O2		24
Asparagine	C4H8N2O3		24
Isoqurctrin	C21H20O12		24
Ferulic-Acid	C10H10O4		24
Farnesene	C15H24		24
Neoxathin	C40H56O4		24
Sinapic-Acid	C11H12O5		24
Caffeic-Acid	C9H8O4		24
Chlorogenic-Acid	C16H18O9		25
P-Coumaric-Acid	C9H8O3		24
Lutein	C40H56O2		24
Quercetin	C15H10O7		26
Rutin	C27H30O16		27
Ursolic-Acid	C30H48O3		25
Protocatechuic-Acid	C7H6O4		24
Catechin	C15H14O6		25
Gallic acid	C7H6O5		24
Phloretin	C15H14O5		26

 

The results demonstrate that the consumption of the fresh and dried apple exerts a beneficial effect to human health. Different molecular mechanisms can be suggested to explain the protective effect exerted by apple components. The beneficial effects of whole apples on plasma lipid levels are probably related to synergistic interactions between apple components. Contrasting results have been reported in obese and hypercholesterolemic patients. Additional human studies are needed to confirm the hypothesized antioxidant, antiinflammatory, and vascular protective effects of apples and derivatives in normal and pathological conditions. Various chemical structures of active constituents are mentioned in Table 6.

 

Health benefits of Malus domestica:

Apples are also full of a fiber known as pectin – a medium-sized apple offers about four grams of fiber. Pectin is defined as a soluble, fermentable and viscous fiber, a combination that gives apples a huge list of health benefits. Nutritional value (100g) has been summarized in table 7

 

Table 7: Nutritional values per (100 g )

Energy	218 kJ (52 kcal)
Carbohydrates	13.81 g
Dietary fiber	2.4 g
Sugars	10.39
Beta-carotene	27 μg (0%)
Calcium	6 mg (1%)
Fat	0.17 g
Fluoride	3.3 μg
Folate (B9)	3 μg (1%)
Iron	0.12 mg (1%)
Lutein zeaxanthin	29 μg
Magnesium	5 mg (1%)
Manganese	0.035 mg (2%)
Niacin (B3)	0.091 mg (1%)
Pantothenic acid (B5)	0.061 mg (1%)
Phosphorus	11 mg (2%)
Potassium	107 mg (2%)
Protein	0.26 g
Riboflavin	0.026 mg (2%)
Sodium	1 mg (0%)
Thiamine (B1)	0.017 mg (1%)
Vitamin A	3 μg (0%)
Vitamin B6	0.041 mg (3%)
Vitamin C	4.6 mg (6%)
Vitamin E	0.18 mg (1%)
Vitamin K	2.2 μg (2%)

 

Dental benefits:

Biting and chewing an apple stimulates the production of saliva in mouth, reducing tooth decay by lowering the levels of bacteria²⁸.

 

Neuroprotective effect:

The benefits of apples shows that drinking apple juice could keep Alzheimer’s away and fight the effects of aging on the brain. The mice in the study that were fed an apple-enhanced diet showed higher levels of the neurotransmitter acetylcholine and did better in maze tests than those on a regular diet¹². Research has shown that people who eat fruits and other high-fiber foods may be protected against Parkinson’s disease, a condition characterized by a breakdown of the brain’s dopamine-producing nerve cells. Scientists have linked this to the free radical-fighting power of the antioxidants contained therein¹³.

 

Reduces the risk of cancer:

Scientists from the American Association for Cancer Research, among others, agree that the consumption of flavonol-rich apples could help reduce your risk of developing pancreatic cancer by up to 23 per cent. Researchers at Cornell University have identified several compounds – triterpenoids – in apple peel that have potent anti-growth activities against cancer cells in the liver, colon and breast. Their earlier research found that extracts from whole apples can reduce the number and size of mammary tumors in rats. Meanwhile, the National Cancer Institute in the U.S. has recommended a high fiber intake to reduce the risk of colorectal cancer^16,17.

 

Hypoglycemic effect:

One who eat apples at least one a day are 28 per cent less likely to develop type 2 diabetes than those who don’t eat apples. The health benefits of apples are because this fruit is loaded with soluble fiber, the key to blunting blood sugar swings^14,15.

Triglyceride lowering effect:

The soluble fiber found in apples binds with fats in the intestine, which translates into lower cholesterol levels and a healthier you.²⁹.

 

Cardioprotective effect:

An extensive body of research has linked high soluble fiber intake with a slower buildup of cholesterol-rich in plaque arteries. The phenolic compound found in apple skins also prevents the cholesterol that gets into system from solidifying on artery walls. When plaque builds inside arteries, it reduces blood flow to your heart, leading to coronary artery disease¹⁹.

 

Reduces gallstones:

Gallstones form when there’s too much cholesterol in your bile for it to remain as a liquid, so it solidifies. They are particularly prevalent in the obese. To prevent gallstones, doctors recommend a diet high in fiber to control weight and cholesterol levels^30,31.

 

Prevents diarrhea and constipation:

Fiber can either pull water out of colon or absorb excess water from stool to slow bowels down¹⁸.

 

Neutralizes irritable bowel syndrome:

Irritable bowel syndrome is characterized by constipation, diarrhea, and abdominal pain and bloating. To control these symptoms doctors advised to take high-fiber diet like apples.¹⁸

 

Prevents hemorrhoids:

Hemorrhoids are a swollen vein in the anal canal and while not life threatening, these veins can be very painful. They are caused by too much pressure in the pelvic and rectal areas. Fiber can prevent from straining too much and thereby help in preventing hemorrhoids³².

 

Prevents obesity:

Many health problems are associated with being overweight, among them heart disease, stroke, high blood pressure, type 2 diabetes and sleep apnea. To manage weight and improve overall health, doctors recommend a diet rich in fiber. Foods high in fiber like apples¹⁵.

 

Hepatoprotective effect:

Liver is responsible for clearing toxins out of body. They have the potential to do more harm than good. Luckily, one of the best and easiest things to help to detoxify liver is fruits such as apples¹⁸.

 

Boosts and energizes immune system:

Red apples contain an antioxidant called Quercetin. Recent studies have found that Quercetin can help boost and fortify immune system¹⁸.

 

Prevent cataracts;

Though past studies have been divided on the issue, recent long-term studies suggest that people who have a diet rich in fruits that contain antioxidants like apples are 10 to 15 percent less likely to develop cataracts¹⁸.

 

Pharmacological of Malus domestica:

Analgesic Activity:

Malus domestica (Apple) a traditional plant widely used since Iron Age and has multiple benefits. In the present study extracted and isolated pectin (MDP) from pulp and extracted Quercetin (MDQ) was evaluated for analgesic action by using various animal models.

 

The extracts of apple MDP and MDQ on isolation of biologically active constituents like pectin and Quercetin respectively were assessed for their potential analgesic activities. In vivo studies performed confirmed with analgesic activity of MDP and MDQ extracts of Malus domestica (Apple), which may due to the presence of isolated active constituents like pectin and Quercetin. An intensive study on molecular pathways, mediators and the enzymes is required for the potential use of MDP and MDQ extracts of Malus domestica (Apple) as analgesic drugs³³.

 

Antipyretic activity:

The antipyretic activity of apple juice was estimated by subcutaneously injecting 20% w/v brewer's yeast suspension (10ml/kg) into the animal's dorsum region .The rectal temperature of each rat was measured using a thermometer before injection of the yeast. The apple juice and paracetamol (100mg/kg) was administered orally and the temperature was measured at 0, 1, 2, 3 and 4 h after administration. Apple is effective as antipyretic. However, describing the active constituent which is responsible for antipyretic effect and its mechanisms of action are required³⁴.

 

Cardiovascular activity:

Epidemiological evidence supports the concept that diets rich in fruits and vegetables promote health and attenuate or delay the onset of cardiovascular disease (CVD). In particular, a reduced risk of CVD has been associated with apple consumption, probably due to the cholesterol lowering effect of the main bioactive compounds, namely fiber and polyphenols. This study describes for the first time the effect of three different apple varieties, namely Bravo de Esmolfe, Malápio da Serra and Golden, containing different amounts of bioactive compounds, on two relevant biomarkers of cardiovascular diseases in an animal model. The results show that both cholesterol- and LDL- lowering effects may be directly correlated with the phenolic contents, namely catechin, epicatechin and procyanidin B1, antioxidant activity and -carotene concentration of apples³⁵.

 

Antibacterial activities

Synthetic antimicrobials are losing ground to their natural counterparts and therefore, the food industry has motivated to seek other natural alternatives. Apple pomace, a by-product in the processing of apples, is rich in polyphenols, and plant polyphenols have been used as food additives owing to their strong antimicrobial properties. The study was conducted to screen the individual polyphenols with antimicrobial activities from the extracts (methanol, ethanol, acetone, ethyl acetate, and chloroform) of Golden Delicious pomace. Ethyl acetate was the best solvent of choice to extract natural products to obtain the maximum antibacterial benefits. Phloridzin and phloretin have the potential to be used as natural alternatives to antimicrobials³⁶.

 

Hyperlipidemic activities

A healthy life style and a balanced diet, associated with a high fruit and vegetable intake, are linked to good health and the prevention of diseases. Apples contain bioactive compounds that help in the prevention and control of hyperlipidemia. One of the Public Health concerns in Brazil is to reduce cardiovascular diseases. Therefore, a research has been done to analyze the chemical composition of Gala apples and to study the effect of their consumption on weight gain, food intake, and serum levels of total cholesterol, HDL-C, LDL-C, triglycerides, hepatic cholesterol and fecal cholesterol in male albino Wistar rats fed a hypercholesterolemic diet. The 15 and 25% apple diets showed significant reductions in the serum levels of total cholesterol and LDL-C and an increase in the level of fecal cholesterol in relation to the control group. The 25% apple diet provided a significant reduction in the hepatic cholesterol levels compared to the control group. After 60 days, the serum levels of total cholesterol, LDL-C, HDL-C and triglycerides in rats fed with 5, 15 and 25% apple diets were similar to the control group. This probably happened due to a reversion of the process. These results show the importance of Gala apples in the control of hyperlipidemia in rats. A diet rich in vegetables and fruits, including apples, associated to a healthy life style, over time, could prevent or reduce the risk of heart disease³⁷.

 

Anti-inflammatory:

The dietary consumption of fruit and vegetable is associated with a lower incidence of degenerative diseases such as cardiovascular disease. Most recent interest has focused on the bioactive phenolic compounds in vegetable products. All varieties of apple contain several antioxidants and polyphenols that possess many biological activities, such as antioxidant and anti-inflammation properties. The review describes the nutritional properties of apples and their derivatives, with a particular attention to polyphenol compounds. Moreover, the health benefits of apples and the potential molecular mechanisms against cardiovascular disease are reviewed. The beneficial effects of whole apples on plasma lipid levels are probably related to synergistic interactions between apple components. Contrasting results have been reported in obese and hypercholesterolemic patients. Additional human studies are needed to confirm the hypothesized antioxidant, antiinflammatory, and vascular protective effects of apples and derivatives in normal and pathological conditions³⁸.

 

Table 8: Potential disease-preventive mechanisms of apple and their active constituents as identified in human dietary studies

Potential disease-preventive mechanisms	Key active components
Antioxidant activity (ROS and RNS)	Flavonoids, Ascorbic acid, Pronthocyanidins
Blood pressure reduction	Flavonoids
Modifications of plasma lipids and lipoprotein levels	Fibers (Pectin), Polyphenols
Modulation of endothelial cells	Flavonoids
Anti-inflammatory properties	Flavonoids, Proanthocyanidins

 

Antihypertensive activities:

Apples or otherwise botanically known as Malus domestica is said to have originated in the mountains of Central and west Asia. It is one of the earliest and most commonly grown trees. In humans it is consumed in various forms and varieties; also it is eaten as a raw fruit. The study has highlighted the antihypertensive property of an apple peel along with numerous health benefits of an apple. It is concluded from this article that the flavonoids such as Quercitin, Proanthocyanidin present in the peel of an apple along with pectin can help in reducing the blood pressure among which inhibition of Angiotensin converting enzyme is one of the important mechanism. It can be concluded that an apple peel is a rich source of flavonoids. These flavonoids such as Quercetin, proanthocynadins, anthocynanins and pectin content of an apple directly or indirectly benefit the cardiovascular system and helps in lowering of blood pressure. Most of these flavonoids exhibits there action by inhibition of angiotensin converting enzyme , improving endothelial function of blood vessels, preventing oxidation of low density lipoprotein and improving high density lipoprotein in circulation, prevent atherosclerosis and are strong antioxidants³⁹.

 

Antioxidant activities:

Evidence suggests that increasing consumption of fruit and vegetables contributes to improved health and well-being by providing protection from diseases including various cancers and cardiovascular disease. Although there is uncertainty about which components generate this effect, an attractive hypothesis is that the antioxidants are at least partly responsible. A research showed that the concentration of polyphenolics content varied among the apple cultivars, with Pacific Queen containing 2.7 times the amount of polyphenolics found in Cox’s Orange. Furthermore, there were significant differences in polyphenolic concentrations in fruit from different regions for some cultivars but not for others. The researcher also measured the polyphenolic concentrations in apple skin and flesh and found that on average 46% of the polyphenolics in whole apples were in the skin. Essentially all of the flavonols (quercetin derivatives) were present in the skin. To maximize the intake of apple polyphenols, it is necessary to consume apples of cultivars with high polyphenolic concentrations such as Pacific Queen and include the skin. The results also showed that there is potential for promoting apple fruit from specific geographical regions because they contained elevated concentrations of antioxidant polyphenolic compounds⁴⁰.

 

Anticancer activities:

Apples (Malus sp., Rosaceae) are a rich source of nutrient as well as non-nutrient components and contain high levels of polyphenols and other phytochemicals. Main structural classes of apple constituents include hydroxycinnamic acids, dihydrochalcones, flavonols (quercetin glycosides), catechins and oligomericprocyanidins, as well as triterpenoids in apple peel and anthocyanins in red apples. In brief, apple extracts and components, especially oligomeric procyanidins, have been shown to influence multiple mechanisms relevant for cancer prevention in in vitro studies. These include antimutagenic activity, modulation of carcinogen metabolism, antioxidant activity, anti-inflammatory mechanisms, modulation of signal transduction pathways, antiproliferative and apoptosis-inducing activity, as well as novel mechanisms on epigenetic events and innate immunity. Apple products have been shown to prevent skin, mammary and colon carcinogenesis in animal models. Epidemiological observations indicate that regular consumption of one or more apples a day may reduce the risk for lung and colon cancer. This review emphasizes the importance of apples and apple products for cancer prevention. Apples and apple juice are an integral part of the human diet and are consumed by a majority of the population, including children. Almost all studies summarized here suggest that apples, natural cloudy apple juice, and apple extracts should be further investigated as part of a prevention strategy for cancer, especially of hereditary and sporadic colorectal cancer and lung cancer²⁵.

 

Antiproliferative activity:

Apples have been shown to have potent antiiproliferative activity in several studies. When Caco-2 colon cancer cells were treated with apple extracts, cell proliferation was inhibited in a dose-dependent manner reaching a maximum inhibition of 43% at a dose of 50 mg/mL. The same trend was seen in HepG2 liver cancer cells with maximal inhibition reaching 57% at a dose of 50 mg/mL. Due to its unique combination of phytochemicals in the apples that are responsible for inhibiting the growth of tumor cells. Apples had the third highest antiproliferative activity when compared to eleven other commonly consumed fruits Apples without peels were significantly less effective in inhibiting HepG2 cell proliferation when compared to apples with the peel, suggesting that apple peels possess significant anti-proliferative activity. It was concluded that apple peels alone inhibited HepG2 cell proliferation significantly more than whole apples⁴¹.

 

Hepatoprotective activity:

Natural remedies from medicinal plants are considered to be effective and safe alternative treatment for liver toxicity. Hepatoprotective effect of alcoholic and water extract of apple has been used estimated, and result suggests that alcoholic extract has more hepatoprotective effect as compared to water extract⁴².

 

Gastro esophageal Reflux Disease:

This randomized, placebo-controlled, double-blind, cross-over research study tested the efficacy of the organic apple cider vinegar, with mother, on alleviation of the heartburn symptom related to Gastro-esophageal reflux disease (GERD) and result suggest that apple extract is effective in reducing the GERD⁴³.

 

Antimicrobial activity:

A study was done to evaluate for potential antimicrobial activity of false fruit apple extracts. Separately cashew apple were extracted with aqueous and ethanol solvents and their antimicrobial activity was compared against few selected gram positive [Bacillus cereus (ATCC11778)] and gram negative bacteria Klebsiella pneumoniae (ATCC11298)] by disc diffusion technique .The study revealed the potential antimicrobial activity of different false fruit extract of apple. The Preliminary phytochemical analysis indicated the presence of various phytoconstituents in all the tested extracts⁴⁴.

 

Hypoglycemic activity:

Type 2 diabetes is the most common metabolic disorder worldwide and its prevalence is growing at an alarming rate in both developed and developing countries. It is characterized by abnormalities in carbohydrate, lipid and lipoprotein metabolism, which lead to hyperglycemia and many complications such as hyperlipidemia, hyperinsulinemia, hypertension and atherosclerosis. In order to prevent diabetes, in addition to oral hypoglycemic drugs, the dietary component such as Apple cider vinegar seems to be promising for glycemic control in patients with type 2 diabetes as well as for diabetes related medical conditions. Apple cider vinegar is fermented juice from crushed apples. Acetic acid in vinegar seems to suppress disaccharides activity and increase glucose-6-phosphate levels in skeletal muscle. Thus an attempt is made in the present study to find out the impact of apple cider vinegar in patients with type 2 diabetes. The result suggests that it has potent hypoglycaemic activity⁴⁵. Potential mechanism of action of apple in treating various diseases has been compiled in table 8.

 

CONCLUSION:

The above compiled information regarding the use of Malus domesticus in world is matched with available literature. Recent year, traditional and ethno-botanical use of natural origin drugs, most importantly plants received more attention as it’s a general belief that they are safe to human⁴⁶. The herbal products today symbolize safety in contrast to the synthetics that are regarded as unsafe to human and environment⁴⁷.

 

The strategic favour of the medicinal virtues of plants requires systematic and scientific approach in exploration of the chemical constituents of plants⁴⁸. Apple possesses various phytoconstituent which have well established antioxidant potential and is used in treatment of various ailments. Apart from its various pharmacological activities it has very rich nutritional value. The toxicity study and safety pharmacology has yet to be established for malus species.

 

ACKNOWLEDGMENT:

Author sincerely pays his heartfelt respect and gratitude toward Prof. Syed Waseem Akhtar, Hon. Chancellor and Prof. Aqil Ahmad, Hon. Vice Chancellor (Acting), Integral University for providing an excellent research environment. The university has provided a manuscript communication number for further communication (IU/RandD/2019-MCN000626).

 

CONFLICTS OF INTEREST:

The authors declare no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.

 

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Accepted on 21.11.2019                                 © RJPT All right reserved

Research J. Pharm. and Tech 2020; 13(3):1527-1537.