KR20120008370A - Anti-cancer composition comprising extract from hylocereus undatus - Google Patents

Abstract

PURPOSE: An anticancer composition containing Hylocereus undatus extract is provided to suppress cancer cell proliferation and to ensure anticancer efficiency. CONSTITUTION: An anticancer composition contains Hylocereus undatus extract as an active ingredient. The Hylocereus undatus is isolated from peel or pulp of Hylocereus undatus using water, anhydrous or hydrous low alcohol of 1-4 carbon atoms, acetone, ethyl acetate, butyl acetate, or 1,3-butyelen glycol. The composition is a pharmaceutical composition for preventing or treating cancer or a food composition for relieving cancer. The daily dose of the pharmaceutical composition is 0.001-1000 mg/kg(body weight).

Description

Anti-cancer composition Comprising extract from Hylocereus undatus containing white pitaya extract as an active ingredient

The present invention relates to an anticancer composition comprising a white pitaya ( Hylocereus undatus ) extract as an active ingredient.

Consumers' concerns about synthetic antioxidants have increased the need for natural antioxidants (Shahidi 1997). Various studies have been reported on the antioxidant properties of fruit juices and pulp from edible fruits (Mokbel and Hashinaga 2006). Fruits have been noted for their antioxidant activity because they are rich in compounds that play an important role in free radical scavenging. Various studies on apples (Wolfe and others 2003), grape seeds (Chidambara-Murthy and others 2002), strawberries (Meyers and others 2003), common vegetables (Chu and others 2002), and raspberries (Liu and others 2002) These fruits and vegetables are reported to have antiproliferative effects. However, the antioxidant and antiproliferative activities of other plant-derived foods are not well studied, and the information available on the medicinal and nutritional values of subtropical fruits is very limited.

It is mentioned in the historical documents that Pitaya was a very popular fruit from the Aztec race. Native to Mexico, Central and South America, this fruit has long been consumed in the Western Hemisphere (Mizrahi and others 1997). It is also grown on Jeju Island in Korea, where the current climate is changing to suit the cultivation of pitaya. The skin of a pitaya is covered with a bract or scale and is called a dragon fruit. Based on their skin and pulp color, pitaya has been classified as white pitaya (Hylocereus undatus), red pitaya (H. costaricensis) and yellow pitaya (Selenicereus megalanthus) (Nerd and others 2002, Hoa and others 2006). Pitaya fruit attracts a lot of attention because of its health benefits in addition to its excellent color and economic value as a food (Chen and He 2007, Li and others 2003). For example, red pitaya has been reported to have a wide variety of efficacy, including anticancer efficacy, anti-inflammatory and anti-diabetic efficacy, and reduced mortality of cardiovascular disease, as well as antioxidant properties conferred by beta cyanine content (Cos and others 2004, Stintzing and others 2002; Wybranice and Mizrahi 2002). Fatty oils of white pitaya seeds are known to contain linoleic acid with cardio-protective, anti-diabetic and antibacterial properties (Das 2000, Szentmihtmlyi 2002). Recently, there have been reports of polyphenol and flavonoid content from the flesh extracts of red and white pitaya, and the DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging activity against HeLa cells The results of measuring antiproliferative activity have been reported (Asmah and others, 2008). In addition, red pitaya showed a cytotoxic effect at the stage of metastasis of human oral cancer cells induced by B16F10 melanoma cells (Menon and others 1995). In addition, chemical research efforts on betalain in pitaya are underway (Wybranice and Mizrahi 2002, Stintzing and others 2004). Attempts have been made to identify the health benefits of pitaya and the substances contributing these benefits, but little research has been done on pitaya's bark extracts.

Numerous papers and patent documents are referenced and cited throughout this specification. The disclosures of cited papers and patent documents are incorporated herein by reference in their entirety, and the level of the technical field to which the present invention belongs and the contents of the present invention are more clearly explained.

The present inventors analyzed the antioxidant and anticancer activity of extracts of the subtropical fruit, Pitaya, as part of research to develop antioxidant and antiproliferative substances from natural sources. As a result, the phytic extract and the flavonoid compound contained very rich in phytaya extract, excellent in antioxidant activity against various kinds of free radicals, and effectively inhibited the proliferation of cancer cell lines to complete the present invention.

Therefore, an object of the present invention is to provide an anticancer composition comprising a white pitaya ( Hylocereus undatus ) extract as an active ingredient.

The objects and advantages of the invention will become apparent from the following detailed description, claims and drawings.

According to one aspect of the invention, the present invention provides a composition for anticancer comprising a white pitaya ( Hylocereus undatus ) extract as an active ingredient.

According to a preferred embodiment of the present invention, the white pitaya extract is an extract from the skin or flesh of the white pitaya.

The white pitaya extract in the present invention can be separated according to conventional methods known in the art for extracting extracts from natural products, that is, using conventional solvents under the conditions of conventional temperature, pressure. As an extraction solvent for extracting the white pitaya extract of the present invention, a solvent that can be generally used in the extraction process may be used. For example, water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, acetone, ethyl acetate, Preference is given to using a solvent selected from the group consisting of butyl acetate and 1,3-butylene glycol.

According to a more preferred embodiment of the present invention, the white pitaya extract of the present invention is an extract using anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms as a solvent.

The active ingredient white pitaya ( Hylocereus undatus ) extract of the present invention contains a polyphenolic compound and a flavonoid compound, and has cancer cell proliferation inhibitory activity against various kinds of cancer cells.

According to a preferred embodiment of the present invention, the composition of the present invention may be prepared in the form of a pharmaceutical composition for the treatment or prophylaxis of cancer.

According to another preferred embodiment of the invention, the cancer to be treated in the present invention is not limited to a specific cancer, for example breast cancer, lung cancer, stomach cancer, liver cancer, blood cancer, bone cancer, pancreatic cancer, skin cancer, head or neck cancer (head or neck cancer), skin or eye melanoma, uterine sarcoma, ovarian cancer, rectal cancer, anal cancer, colon cancer, fallopian tube cancer, endometrial cancer, cervical cancer, small intestine cancer, endocrine cancer, thyroid cancer, parathyroid cancer, kidney cancer, soft tissue Tumors, urethral cancer, prostate cancer, bronchial cancer or bone marrow cancer, and more preferably gastric cancer, breast cancer or cervical cancer.

The pharmaceutical composition of the present invention includes a pharmaceutically acceptable carrier in addition to the white pitaya extract as an active ingredient.

Pharmaceutically acceptable carriers included in the pharmaceutical compositions of the present invention are those commonly used in the preparation, such as lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, calcium phosphate, alginate, gelatin, Calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, and the like It doesn't happen.

In addition to the above components, the pharmaceutical composition of the present invention may further include a lubricant, a humectant, a sweetener, a flavoring agent, an emulsifier, a suspending agent, a preservative, and the like. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington's Pharmaceutical Sciences (19th ed., 1995).

Suitable dosages of the pharmaceutical compositions of the present invention may vary depending on factors such as the formulation method, mode of administration, age, weight, sex, morbidity, condition of food, time of administration, route of administration, rate of excretion and response to response of the patient. Can be. On the other hand, the oral dosage of the pharmaceutical composition of the present invention is preferably 0.001-1000 mg / kg (body weight) per day.

The pharmaceutical composition of the present invention may be administered orally or parenterally, and when administered parenterally, may be administered topically to the skin, intravenous injection, subcutaneous injection, intramuscular injection, intraperitoneal injection, transdermal administration, and the like. .

The concentration of the white pitaya extract, which is an active ingredient included in the composition of the present invention, may be determined in consideration of the purpose of treatment, the condition of the patient, the period of time, etc., and is not limited to a specific range of concentration.

The pharmaceutical composition of the present invention may be formulated into a unit dose form by formulating it using a pharmaceutically acceptable carrier and / or excipient according to a method which can be easily carried out by a person having ordinary skill in the art to which the present invention belongs. Or by intrusion into a multi-dose container. The formulations may be in the form of solutions, suspensions or emulsions in oils or aqueous media, or in the form of excipients, powders, granules, tablets or capsules, and may additionally contain dispersing or stabilizing agents.

According to another preferred embodiment of the present invention, the composition of the present invention may be prepared in the form of a functional food composition for use in alleviating or ameliorating cancer.

Functional food compositions of the present invention include ingredients that are commonly added in the manufacture of food, and include, for example, proteins, carbohydrates, fats, nutrients and seasonings. For example, when prepared with a drink, it may be included as an additional ingredient a flavor or natural carbohydrate in addition to the white pitaya extract as an active ingredient. For example, natural carbohydrates include monosaccharides (eg, glucose, fructose, etc.); Disaccharides (eg maltose, sucrose, etc.); oligosaccharide; Polysaccharides (eg, dextrins, cyclodextrins, etc.); And sugar alcohols (eg, xylitol, sorbitol, erythritol, and the like). As the flavoring agent, natural flavoring agents (e.g., taumartin, stevia extract, etc.) and synthetic flavoring agents (e.g., saccharin, aspartame, etc.) can be used.

The features and advantages of the present invention are summarized as follows:

(i) The present invention relates to a novel anticancer use of white pitaya ( Hylocereus undatus ) extract.

(Ii) The white pitaya extract of the present invention ( Hylocereus undatus ) has the effect of inhibiting the proliferation of cancer cells.

(Iii) The white phytaya ( Hylocereus undatus ) extract of the present invention can be developed into a pharmaceutical composition or a functional food composition for use in the treatment, prevention or amelioration of cancer.

The present invention relates to a novel anticancer use of white pitaya ( Hylocereus undatus ) extract. White pitaya extract of the present invention ( Hylocereus undatus ) has an anticancer effect of inhibiting the proliferation of cancer cells. The white pitaya ( Hylocereus undatus ) extract of the present invention can be developed into a pharmaceutical composition or a functional food composition for use in the treatment, prevention or amelioration of cancer.

1A-1C show the results of the correlation between the polyphenol and flavonoid content and free radical scavenging activity of the pulp and bark extracts of white and red pitaya.
1A shows hydroxy radical scavenging activity (%) vs. The relationship with polyphenol and flavonoid content is shown.
Figure 1b shows alkyl radical scavenging activity (%) vs. The relationship with polyphenol and flavonoid content is shown.
Figure 1C shows DPPH radical scavenging activity (%) vs. The relationship with polyphenol and flavonoid content is shown.
Figure 2 shows the correlation between the cell viability of various cancer cell lines and DPPH radical scavenging activity of the white and red pitaya pulp and bark extract.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it will be apparent to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. .

Example

Materials and Methods

1. Compound

Folin-Ciocalteu Phenolic Reagent, Rutin, Gallic Acid, Hydrogen Peroxide, Ferrous Sulfate, DPPH, DMPO (5,5-dimethyl-1-pyrroline-N-oxide) , AAPH [[2,2'-azobis (2-amidinopropane) hydrochloride], and 4-POBN [α- (4-pyridyl-1-oxide) -Nt-butylnitrone] are described in Sigma Chemical Co. (St. Louis, MO, USA). Dimethyl sulfoxide (DMSO) and MTT [3- (4, 5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide] are available from Amresco Inc. (Solon, OH, USA). RPMI 1640 medium, DMEM (Dulbecco's modified Eagle's medium), trypsin / EDTA, fetal bovine serum (FBS), penicillin and streptomycin are described by Invitrogen Inc. (Grand Island, NY, USA). All other compounds and reagents were of analytical grade.

2. Fruit

White and red pitaya fruits were collected on farms near Hallim Park in Jeju Island. All fruits were washed and the skin was carefully removed. The pulp and shells were cut into small thin slices and stored at −70 ° C. until used in the assay.

3. Sample preparation

The pulp and skin samples were lyophilized under reduced pressure for 2 days and then powdered. Extraction in 80% methanol was performed at room temperature for 3 days with sonication. The resulting extract was Whatman No. It was filtered through 1 filter paper and concentrated using a 40 ° C. reduced pressure rotary evaporator and then lyophilized. They were dissolved in DMSO and diluted in PBS (phosphate-buffered saline, pH 7.4) to prepare to final use concentrations. Methanol extracts from each plant were measured for total phenolic compound content, DPPH radical scavenging activity and cytotoxicity.

4. Determination of Total Polyphenols and Flavonoid Levels

Total polyphenol and flavonoid levels were measured according to the Cheung method (Cheung and others 2003) with minor modifications. Sample aliquots (1.5 mL) were mixed with 0.5 mL of Folin-Ciocalteu phenolic reagent. After 5 minutes, 1 ml of 10% (w / v) Na ₂ CO ₃ was added to each reaction mixture. The reaction was carried out under dark conditions for 30 minutes, and the absorbance at 725 nm was recorded using a UV 1800 spectrometer (Shimadzu, Tokyo, Japan). Results are expressed as gallic acid equivalent (GAE) (mg GAE / g of dried sample). Flavonoid content was measured using known colorimetric assays (Zhishen and others 1999). Absorbance was measured at 510 nm for blank (PBS) and flavonoid content was expressed in rutin equivalents (RE) (mg RE / g of dried sample). All analyzes were performed at least three times.

5. DPPH Radical Scatters  ( DPPH radical scavenging )

DPPH radical scavenging activity was determined according to the methods previously described (Nanjo and others 1996). 30 μl aliquots (or PBS alone as controls) of each sample diluted in PBS were added to 30 μL DPPH (60 μM) in ethanol. The final concentration of each pitaya extract was 25 μg / ml. After vigorous mixing for 10 seconds, the solution was placed in 50 μL of Teflon capillary tube and inserted into a JES-FA electron spin resonance (ESR) spectrometer (JEOL, Tokyo, Japan). The spin adduct was then measured at 2 minutes. The measurement conditions were as follows: center field 3475 G, control frequency 100 kHz, control amplitude 2G, microwave power 5 mW, gain 6.3 X 10 ⁵ and temperature 297 K. The radical scavenging ability of the pitaya extract was Calculated according to: scavenging rate = (h ₀ -h _x ) / h ₀ X 100%, where h ₀ and h _x are the ESR signal strengths of the sample with or without the extract, respectively to be.

6. hydroxyl radical scavenging ability

The hydroxyl radical was produced by the Fenton reaction and reacted rapidly with the nitrone spin trap DMPO. The resulting DMPO-OH reaction adduct was measured by ESR (Rosen and Rauckman 1984). ESR spectra were measured in 2.5 minutes after mixing with 20 μL of 0.3 M DMPO, 20 μL of 10 mM FeSO ₄ and 20 μL of 10 mM H ₂ O ₂ in phosphate buffer (pH 7.4) under the following conditions: : Center field 3475 G, adjustable frequency 100 kHz, adjustable amplitude 2 G, microwave power 1 mW, gain 6.3 X 10 ⁵ and temperature 298 K. The final concentration of each pitaya extract is 2 mg / ml It was. The radical scavenging ability of the pitaya extract was calculated according to the following formula: scavenging rate = (h ₀ -h _x ) / h ₀ X 100%, where h ₀ and h _x are the samples containing the extract, respectively ESR signal intensity of the sample without extract.

7. Alkyl radical scavenging ability

Alkyl radicals were produced by AAPH. The reaction mixture containing test samples prepared at the indicated concentrations diluted with 40 mM AAPH, 40 mM 4-POBN and PBS (pH 7.4) was incubated for 30 minutes in a 37 ° C. water bath (Hiramoto and others 1993) and Teflon Carb Placed in a filler tube. The final concentration of each pitaya extract was 200 μg / mL. Spin addition products were recorded using an ESR spectrometer. The following measurement conditions were used: center field 3475 G, control frequency 100 kHz, control amplitude 2 G, microwave power 10 mW, gain 6.3 X 10 ⁵ , and temperature 298 K. The radical scavenging ability of the pitaya extract was Calculated according to the following formula: scavenging rate = (h ₀ -h _x ) / h ₀ X 100%, where h ₀ and h _x are the samples with and without extract, respectively. ESR signal strength.

8. Culture of Cells

Cancer cell lines AGS (human gastric cancer cell line), HeLa (human cervical cancer cell line), and MCF-7 (human breast cancer cell line) were obtained from the Korea Cell Line Bank (KCLB, Seoul, Korea). These cell lines were incubated with DMEM or RPMI 1640 medium supplemented with 10% (v / v) heat-inactivated fetal bovine serum (FBS), 100 units / ml penicillin, and 100 μg / ml streptomycin. Incubated in a 37 ° C., 5% CO ₂ atmosphere.

9. Viability Analysis of Cancer Cells

The effect of pitaya extract on the viability of various cancer cell lines was measured by MTT colorimetric assay (Hansen and others 1989). Briefly, cancer cells in log phase were dispensed into 96-well plates (2 × 10 ³ to 1 × 10 ⁴ cells per well). Incubated for 72 hours in the presence of various concentrations of extract (125-1000 μg / mL) or standard material (quercetin; 12.5-200 μM / mL). 0.1 mg of MTT was added to each well and the cells were incubated at 37 ° C. for 4 hours. The growth medium was then carefully removed and DMSO (150 μl) was added to each well to dissolve the formazan crystals formed. Absorbance at 570 nm was recorded immediately using a microplate reader (Tecan, Salzburg, Austria). Cell viability is expressed as a percentage of untreated control cells.

10. Determination of the bioactivity index

The bioactivity index (BI) can be used by consumers to select fruits or vegetables based on beneficial properties. It can also be used as a tool for ranking data in epidemiological studies (Sun and others 2002). According to a recent study, BI was determined by the following equation: BI = (total antioxidant activity value + antiproliferative activity value) / 2, where total antioxidant activity value = sample value / highest antioxidant value, antiproliferative activity value = Highest IC ₅₀ value / sample IC ₅₀ value.

11. Statistical Analysis

All analyzes were performed three times and data were expressed as mean W SD values. IC ₅₀ values were calculated from dose-response curves and if necessary the following formula was used: Y = 100 * A1 / (X + A1), where A1 = IC ₅₀ , Y = response and X = inhibitory concentration (Y = 100%, X = 0). IC ₅₀ values were assessed by paired Student's t-test. Variable regression analysis using Sigma plot software Version 9.0 (Jandel CoRPP., San Raphael, Calif., USA) confirmed statistically significant relationships between independent variables. The p-value <0.05 was considered statistically significant. Pearson's correlation analysis was performed using Sigma State Software Version 3.1 (Jandel CoRPP., San Raphael, Calif., USA) to analyze the relationship between polyphenol and flavonoid content and cell viability ratio.

Experiment result

1. Total Polyphenol and Flavonoid Content

The total phenolic content of the flesh and skin of red and white pitaya was measured according to the Folin-Ciocalteu method (Wu and others 2006). The total extractable phenolic content from the skin and pulp of red pitaya was 14.82 ± 1.07 mg GAE / g and 4.91 ± 0.55 mg GAE / g, respectively, and 15.94 ± 0.93 mg GAE / g and 3.52 ± 0.60 mg GAE / g. Table 1 shows the polyphenol and flavonoid contents and% yields in different pitaya extracts. As shown in Table 1, the polyphenol content of the methanol extraction of the red pitaya peel (RPP) and the white pitaya peel (WPP) is shown in the red pitaya flesh (RPF) and It was about 3- and 5-fold higher than that of the white pitaya flesh (WPF). RPP had the highest flavonoid content (18.16 ± 1.00 RE / g), followed by WPP (14.33 ± 0.58 RE / g), RPF (9.56 ± 0.11 RE / g), and WPF (3.52 ± 0.12 RE / g). .

The results in Table 1 are expressed as mean ± standard deviation. * P <0.05 compared to control.

Taken together, RPP and WPP had similar levels of polyphenols and flavonoids, while RPF contained more polyphenols and flavonoids than WPF.

2. Free radical scavenging activity

Since conventional methods of antioxidant activity assessment are specific to only one property, one of the major issues when evaluating the antioxidant activity of biological materials is the choice of analytical method. Many chemical analysis methods measure the ability of a tested substance to inhibit the oxidation of a target substrate by certain free radicals such as superoxide anions or hydroxyl or peroxy radicals (Hassimotto and others 2005). Since ESR is known for sensitive, direct and accurate monitoring of reactive species (Guo and others 1999), 80% methanol extract of red and white pitaya pulp and bark using catechins as a standard It was used to compare DPPH, hydroxyl and alkyl radical scavenging ability of.

3. DPPH radical scavenging ability

DPPH is a stable free radical whose level is greatly reduced upon exposure to proton radical scavengers (Sanchez-Moreno 2002). As shown in Table 2 below, the 80% methanol extract of WPP showed the highest DPPH radical scavenging activity (68.12 ± 2.87%), followed by RPP (56.85 ± 5.65%), RPF (33.25 ± 1.84%), and WPF (23.83 ± 3.33%). The concentration of all extracts here was 25 μg / ml. As expected, catechin showed good antioxidant activity (83.76 ± 2.3 at 10 μg / ml). There was a clear correlation between the phenolic content of the extract and the DPPH radical scavenging activity: linear correlation coefficient, r ² = 0.949 (FIG. 1).

Phenolic components are commonly found in fruits and have been reported to exhibit antioxidant activity, which is derived from the reactivity of their phenolic moieties and is known to eliminate free radicals via hydrogen or electron cycles (Shahidi and Wanasundara 1992). The stronger antioxidant activity of WPP compared to RPP in the DPPH system is due to the higher levels of polyphenol content of WPP: the correlation coefficient (r ² = 0.785) for flavonoid content was lower than that of polyphenols (FIG. One). RPP, on the other hand, showed a higher flavonoid content compared to WPP (see Table 1). Thus, WPP appears to be more useful as a DPPH free radical scavenger.

4. hydroxyl radical scavenging activity

The hydroxyl radicals generated in the Fe ²⁺ / H ₂ O ₂ system in this experiment were captured by DMPO-forming spin adducts and measured using an ESR spectrometer (Saito and others 2008). For phenolic compounds derived from plants, the oxidation product of phenolic compounds is aldehydes and dimers (Halliwel and Gutteridge 1999). As shown in Table 2, the scavenging activities of the RPP, RPF, WPP and WPF extracts were 64.45 ± 5.29%, 47.14 ± 4.47%, 62.12 ± 5.36%, and 58.85 ± 3.82%, respectively. The concentrations of the extracts were all 2 mg / mL. Catechin exhibited hydroxyl radical scavenging activity of 81.11 ± 1.8% at a concentration of 0.1 mg / mL. Since both RPP and WPP contained large amounts of polyphenols and flavonoids, they showed acceptable activity. WPF, on the other hand, showed higher activity than RPF despite containing the lowest amount of polyphenols and flavonoids. Thus, no clear correlation was found between polyphenol and flavonoid content and hydroxyl radical scavenging activity. As shown in FIG. 1, the correlation between polyphenol and flavonoid content and hydroxyl radical scavenging activity was very weak: r ² = 0.496 and r ² = 0.224. Because of their high reactivity, hydroxyl radicals may not accurately reflect the ability of antioxidant molecules to confer oxidative defenses in non-place-specific methods (Adebajo and Gesser 2001). Nevertheless, the results of this experiment suggest that red and white pitaya pulp and bark methanol extracts can provide some protection against hydroxyl radicals.

5. Alkyl radical scavenging activity

Alkyl radicals are major intermediates in various hydrocarbon reactions and can be easily detected by ESR (Kim and others 2010). Similar to the DPPH radical scavenging activity, the RPP and WPP extracts exhibited a slightly higher degree of radical scavenging activity compared to that of the RPF and WPF extracts (33.84 ± 4.61% and 27.62 ± 5.60%) (49.98 ± 2.52% and 42.36 ± 5.00%). The concentrations of the extracts used in the experiment were all 200 μg / mL. Catechin showed strong alkyl radical scavenging activity (90.25 ± 3. 1%) at a concentration of 12.5 μg / mL (see Table 2). The correlation between total polyphenol and flavonoid content and alkyl radical scavenging activity was very significant: r ² = 0.821 and r ² = 0.977 (FIG. 1). The results suggest that, although not universal, flavonoids are also very important antioxidant phenolic compounds. Phenolic antioxidants are known to capture peroxy radicals to protect organics from oxidative degradation, but since self-oxidation involves peroxy and alkyl radicals that act as chain carriers, oxidative degradation can be achieved by trapping alkyl radicals. Protection from is also important (Nisizawa and others 1987). In terms of scavenging activity, the red (and not flesh) skins of red and white pitaya have shown potential as a rich source of alkyl radical scavenging activity.

6. Effect of Pitaya Extract on the Viability of Cancer Cell Lines

Inhibits growth in vitro against three types of cancer cell lines, human gastric cancer cell line (AGS), human cervical cancer cell line (HeLa), and human breast cancer cell line (MCF-7) of red and white Pitaya pulp and bark extract The effects are shown in Table 2 above. Different pitaya extracts showed different antiproliferative effects on different cell lines. These extracts showed survival inhibitory effects against cancer cell lines in the following rankings: WPP> RPP> RPF> WPF (Table 2). In particular, the bark extract of white and red pitaya showed excellent proliferation inhibitory activity against human gastric cancer cell line AGS and breast cancer cell line MCF-7. It was observed that antiproliferative activity correlated with polyphenol and flavonoid content. Polyphenol and flavonoid content and cell viability ratio of the tested extracts were determined.

Table 3 shows Pearson's correlation coefficients for all assays performed on the extracts.

^a is ^a significant value at p <0.05, ^b is a significant value at p <0.01.

A negative correlation was found between the percentage of cell viability of HeLa, AGS, and MCF-7 cancer cell lines and the total polyphenol content of RPP, RPF, WPP, and WPF (r = −0.133 to −0.960). Similarly, a negative correlation coefficient was found between the flavonoid content of the white and red pitaya extract and the proliferation of AGS, HeLa, and MCF-7 cells. Overall, regardless of the cell lines tested, Pitaya's bark extract showed higher cancer cell antiproliferative activity than the pulp extract. These results suggest that the anti-proliferative effect on pitaya extracts on cancer cell lines may be derived from the combined effects of the polyphenols and flavonoids they contain.

7. Correlation Between Antioxidant Activity and Antiproliferative Effect

Experimental results of the present invention confirmed that the WPP extract having a high content of polyphenols and DPPH radical scavenging activity shows the strongest antiproliferative effect against cancer cell lines. However, there was no direct correlation between antioxidant activity and antiproliferative effects. Antiproliferative activity against cancer cells of different pitaya extracts did not show a clear correlation with antioxidant activity (FIG. 2). DPPH radical scavenging activity showed the strongest correlation for HeLa cell growth IC ₅₀ (r ² = .0965). Inhibition of cancer cell proliferation by pitaya extract cannot be explained by their polyphenol content alone. This suggests that certain phenolic compounds do not contribute individually to the antiproliferative activity of the extract but may instead result from the synergistic action of polyphenols and flavonoids and / or other phytochemical combinations present in the extract. The results also suggest that the polyphenols present in the tested pitaya extract play an important antioxidant role.

8. Importance of Bioactivity Index

It provides a bioactivity index (BI) that can provide a brief reference on which fruit to choose when buying a consumer's fruit. Since WPP is the most potent scavenger of DPPH radicals and the growth inhibitor of most tested cancer cell lines, it was used as a relative reference to the calculation of BI values of other extracts. As shown in Table 2, the skin and pulp extracts of the white pitaya had higher BI values compared to the corresponding red pitaya extract. Compared to total antioxidant activity or antiproliferative activity itself, BI is a more useful value in determining extract activity.

9. Conclusion

In conclusion, the present inventors have demonstrated that there are significant differences in the polyphenol and flavonoid content of red and white phytaya pulp and bark, and experimentally that the abundance of various antioxidant and antiproliferative substances are present in the bark of white pitaya. Confirmed. In addition, phytaya extracts have anti-proliferative effects in cancer cell lines, proving that they are very valuable substances that help prevent and treat chronic diseases such as cancer.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the same is by way of illustration and example only and is not to be construed as limiting the scope of the present invention. Thus, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof.

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Claims (5)

Anticancer composition comprising a white pitaya ( Hylocereus undatus ) extract as an active ingredient.
The composition of claim 1, wherein the white pitaya extract is a bark or pulp extract.
The composition of claim 1, wherein the pitaya extract is a solvent extract of water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, acetone, ethyl acetate, butyl acetate or 1,3-butylene glycol.
The composition of claim 1, wherein the composition is in the form of a pharmaceutical composition for the treatment or prevention of cancer.
The composition of claim 1, wherein the composition is in the form of a functional food composition for alleviating or ameliorating cancer.

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