 Gen info
- Eriobotrya japonica (loquat) is a large evergreen shrub or tree in the family Rosaceae, grown commercially for its orange fruit. It is also cultivated as an ornamental plant.
- E. japonica was formerly thought to be related to the genus Mespilus. It is still sometimes mistakenly called Japanese medlar, the name it takes in other European languages. (3)
- The plant has been cultivated in China for over 1,000 years. Chinese immigrants are presumed to have carried loquat to Hawaii and California.
(3)
- Etymology: The name loquat derives from Cantonese lou gwat (pinyin: luju) meaning 'black orange'. The phrase 'black orange' originally referred to unripened kumquats, which are dark green in color, but the name was mistakenly applied to loquat by the ancient Chinese poet Su Shi, a mistake that was widely taken up by the Cantonese thereafter. In Louisiana, many refer to loquats as "misbeliefs" from the Louisiana Creole word for the tree, misplis. (3)
- Loquat has been cultivated in China for over 1,000 years. Chinese immigrants may have brought it to Hawaii and California. (3)
- There are over 800 loquat cultivars in Asia
.
- China is the biggest producer of loquat in the world, more than five times of the second-largest producer, Spain, followed by Pakistan and Turkey. (3) China has a cultivation area of 170,000 ha and an annual output of one million tons. (9)
- In the UK, the plant has gained the Royal Horticultural Society's Award of Garden Merit. (3)
 Botany
• E. japonica is a large, evergreen shrub or small tree, with a rounded crown, short trunk, and woolly new twigs. The tree can grow to 5–10 meters (16–33 feet) tall but is often smaller, about 3–4 m (10–13 ft). The fruit begins to ripen during spring to summer, depending on the temperature in the area. Leaves are alternate, simple, 10–25 centimeters (4–10 inches) long, dark green, tough and leathery in texture, with a serrated margin, and densely velvety-hairy below with thick yellow-brown pubescence; the young leaves are also densely pubescent above, but this soon rubs off. Flowers are 2 cm (3⁄4 in) in diameter, white, with five petals, and produced in stiff panicles of three to ten flowers, with a sweet, heady aroma that can be smelled from a distance. Fruits grow in clusters, oval, rounded or pear-shaped, 3–5 cm (1+1⁄8–2 in) long, with a smooth or downy, yellow or orange, sometimes red-blushed skin. Succulent, tangy flesh is white, yellow, or orange and sweet to subacid or acid, depending on the cultivar. Each fruit contains from one to ten ovules, with three to five being the most common. Several ovules mature into large, brown seeds, with the seeds varying in numbers in each fruit on the same tree, usually between one and four. (3)
Distribution
- Introduced, cultivated, not naturalized.
- Native to
China.
 Constituents
- Studies have identified 164 compounds from the leaves, including triterpenes, flavonoids, sesquiterpene glycosides, megastigmane derivatives, phenylpropanoids, and organic acids, in addition to 169 volatile oils. (6)
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BuOH fraction of methanol extract of leaves yielded antioxidant chlorogenic acid, quercetin-3-sambubioside; and methyl chlorogenate, kaempferol- and quercetin-3-rhamnosides, together with inactive ursolic acid and 2α-hydroxyursolic acid from the EtOAc fraction. (see study below) (5)
- Study of CHCl3 extract yielded four triterpene esters, namely, 23-trans-p-coumaroyltormentic acid (1), 23-cis-p-coumaroyltormentic acid (2), 3-O-trans-caffeoyltormentic acid (3), and 3-O-trans-p-coumaroyl-rotundic acid (4), along with three common ursolic derivatives. (see study below) (8)
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Phytochemical screening of 80% methanol extract of stems revealed presence of carbohydrates, terpenes, tannins, and flavonoids. Further analysis isolated three triterpenic acids, oleanolic, ursolic, and corosolic acids, and four flavonoids, naringenin, quercetin, kaempferol 3-O-ß-glucoside and quercetin
3-O-α-rhamnoside. (see study below) (11)
 - Loquat leaves were found rich in fiber, minerals (potassium, calcium, magnesium, iron, and sodium), and vitamins (B2m B6, and B12) and lower in energy, sugar and fat. Ten phenolic compounds were characterized. Naringenin, procyanidin C1, epicathechin, and rutin were the more abundant compounds in LLE. (see study below) (23)
- Study of dried leaves isolated a sesquiterpene glycoside, nerolidol-3-O-α-L-rhamnopyranosyl(1-->4)-
α-L-rhamnopyranosyl(1-->2)-[α-L-rrhamno-pyranosyl(1-->6)]-ß-D-glucopyranoside. (see study below) (24)
- Study of leaves isolated three new flavonoid glycosides, along with 15 known flavonoids, characterized as (2S)- and (2R)-naringenin 8-C-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosides, and cinchonain Id 7-O-β-D-glucopyranoside, respectively.
(see study below) (27)
- Bioassay-guided fractionation led to the isolation of a new triterpene, 3β-hydroxyl-21β-acetoxyl-urs-12-en-28-carboxylate (1), along with 7 known triterpenoids, methyl corosolate (2), ursolic acid (3), oleanolic acid (4), methyl maslinate (5), α-amyin (6), 3β,19α,23-trihydroxy-urs-12-ene (7) and uvaol (8). (see study below) (44)
- UHPLC-QTOF-MS analysis to depict the phytochemical profile of loquat roots, leaves, stems, seeds, and fruits tentatively annotated 349 compounds, representing phytochemical classes that included flavonoids, phenolic acids, lignans, stilbenes, and terpenoids. (see study below) (46)
Properties
- Studies have suggest antioxidant, antidiabetic, antihyperlipidemic, cytotoxic, anticancer, anti-inflammatory, antinociceptive, antiviral, anti-tumor promoting, anti-allergic, anti-arthritic, antimetastatic, neuroprotective, cardioprotective, antitussive, expectorant, anti-apoptotic, antifibrotic, non-mutagenic, antigenotoxic, hepatoprotective, anti-melanogenesis, anti-acne, anti-aging, antifungal potentiating, anti-proliferative, PED4 inhibitory, antiosteoclastogenesis, anti-obesity, cosmeceutical properties.
Parts used
Leaves, stems, seeds, fruits.
 Uses
Edibility
- Fruits are edible, the flavor described as"floral" with hints of apricot and peach. They are eaten fresh or mixed with other fruits in fruit salads and fruit cups. Also canned or processed into confections; used for making jam, jelly, and chutney, or poached in light syrup. Immature fruits are used for making tarts and pies. (3)
- Fruits also used in juices or smoothies. In Ecuador, loquat used for batidos, mixed with milk, ice, or other fruits. (3)
- Fruits also used as natural sweetener for many types of food
preparations, for marmalades and jelly, sauces and juices, pies and pastries. (3)
- Loquat tea, called Biwa Cha, a health beverate in Japan, is made from loquat leaves roasted at 350°C for 30 mins. (Also see below: study on Loquat flower tea 61)
Folkloric
- No reported folkloric medicinal use in the Philippines.
-
Powdered leaves used to treat diarrhea, depression, and to counter alcoholic intoxication. (3)
- In Chinese traditional medicine, dried leaves used for treatment of coughing caused by pulmonary inflammation, dyspnea due to asthma and cough, nausea, restlessness, and thirst. (6)
- In Japanese folk medicine, leaves used for treatment of stomach ache, ulcers, chronic bronchitis, cancer, and diabetes. (6)
- Leaf decoction put on wounds, cancers, and ulcers.
Others
- Wine: Fruit also used in fermentation to make light wine. The liquor nespolino is made from seeds, reminiscent of nocino and amaretto. Loquat seeds and apricot kernels contain cyanogenic glucosides, but the drinks are prepared from varieties containing only small amounts - such as Mogi and Tanaka - with only minimal risk of cyanide poisoning. (3)
- Wood: Used as alternative to pear wood. Used for making rulers and other writing instruments.
- Perfume: Flowers used for making perfume in Europe. (3 )
- Culture: The pipa, due to its golden color, represents gold and wealth in China. It is one in a bowl of fruits and vegetables to represent auspicious wishes or the Five Prosperities or wurui. (3)
Studies
• Antioxidant Flavonoids / Leaves:A methanol extract and fractions of E. japonica leaves showed strong antioxidant activity, with EtOAc and n-BuOH soluble fractions showing strong activity than others. Antioxidant flavonoids and chlorogenic acid showed prominent inhibitory activity against free radical generation in dichlorofluorescein (DCF) method. (see constituents above) (5)
• Anti-Inflammatory / Antinociceptive / Leaves:Study evaluated the anti-inflammatory and antinociceptive properties of n-BuOH fraction of E. japonica leaves (LEJ). Studies included use of IFN-γ/LPS activated murine peritoneal macrophage model, thermal nociception models such as tail immersion and hot plate test, and chemical nociception induced by intraperitoneal acetic acid and subplantar formalin in mice. Results showed LEJ exhibited potent inhibitory effects on inflammatory mediators including nitric oxide, iNOS, COX-2, TNF-α, and IL-6 via attenuation of NF-kB translocation to the nucleus. LEJ also exhibited excellent antinociceptive activity in both central and peripheral mechanism as a weak opioid agonist. Results suggest potential as anti-inflammatory and analgesic agents for treatment of pains and inflammatory diseases. (7)
• Antiviral: Study of CHCle extract yielded four tritrpene esters, along with three common ursolic derivatives. The compounds were evaluated for antiviral properties. Only compound 3, 3-O-trans-
caffeoyltormentic acid significantly reduced rhinovirus infection. The compounds were ineffective towards HIV-1 and Sindbis virus replication. (see constituents above) (8)
• Antitumor-Promoting / Anti-Inflammatory / Triterpene Acids / Leaves: Study of methanol extract of leaves isolated 16 triterpene acids from ethyl acetate-soluble fraction. Twelve of the compounds, 1-4, 6, 8, and 15, were evaluated for inhibitory effects in TPS-induced inflammation in mice. All compounds tested showed marked anti-inflammatory effect, with 50% inhibitory dose (ID50) of 0.03-0.43 mg per ear. On evaluation against Epstein-Barr virus antigen (EBV-EA) activation induced by TPA, compounds 12 and 13 showed potent inhibitory effects on EBV-EA induction. Compound 12, euscaphic acid, exhibited marked antitumor-promoting activity in an invivo two-stage carcinogenesis test of mouse tumor using DMBA as initiator and TPA as promoter. (10)
• Antifungal / Antioxidant / Stems: In a study of 80% methanol extract of E. japonica stems for antimicrobial activity, the extract significantly inhibited growth of Candida albicans, with no effect on other bacterial and fungal strains tested. The extract showed good antioxidant activity, with high values for oxygen radical absorbance capacity and trolox equivalent antioxidant capacity, while showing low polyphenol content. (see constituents above) (11)
• Anti-Allergic Activity / Inhibition of Mast-Cell Activation / Seeds: Study evaluated the anti-allergic activity of E. japonica seed extract. Inhibition of histamine release-mediated type 1 allergy was used as index. The extract inhibited histamine release from rat mast cells, suggesting usefulness in allergic disease treatment. In a guinea pig allergic rhinitis model, the extract reduced the frequency of sneezing and nose-scratching. (12)
• Subchronic Toxicity Study / Leaves: Study evaluated the potential subchronic toxicity of E. japonica leaf extract (EJE) through a 13-week repeated oral dose study in Sprague-Dawley rats. Three treatment groups received 250, 500, and 1000 mg/k/d. The 13-week study showed no treatment-related adverse effects re: clinical symptoms, body weight, food and water consumption, urinalysis, ophthalmology, necropsy findings, hematology, biochemistry and histopathological changes. While some changes were observed, they did not show a dose-response relationship, and were within normal range for control rats. (13)
• Anti-Inflammatory for Allergic Asthma / Leaves: Study evaluated the anti-inflammatory activities of E. japonica (EJ) leaf extract in an ovalbumin (OVA)-induced murine asthma model and human tracheal smooth muscle cell (HTSMC). The EJ significantly reduced levels of BALF's (bronchoalveolar lavage fluid) NO, EPO, MMPs, IL-4, IL-13, and serum IgE, and also decreased inflammatory cell infiltration and mucus production. EJ attenuated proliferation of HTSMC, inhibited overexpression of ERK 1/2 and translocation of NFkB in HTSMC as well as iNOS and COX-2 expression in RAW 264.7 cell. Results suggest EJ effectively protects against allergic airway inflammation and is a potential therapeutic option for allergic asthma management. (14)
• Effect on Liver Function in DMN-Hepatopathy / Seeds: Study of seed extracts showed presence of unsaturated fatty acids linolenic and linoleic acids and sterol ß-sitosterol in the 70% EtOH and MeOH extracts. Extracts were administered orally to rats with dimethylnitrosamine-induced hepatopathy. Results showed liver function-improving effects evidenced by significantly lower AST, ALT, and hydroxyproline levels, and significantly higher retinoid levels in extract treated rats. The extracts inhibited the development of liver fibrosis in hepatopathic rats. The unsaturated linolenic and linoleic acids and ß-sterol in the extracts may also contribute to improvement of liver function. (15)
• Reversal of Insulin Resistance / Antihyperlipidemic: Study evaluated the effect of E. japonica on insulin resistance in mice fed a high-fat (HF) diet. Oral loquat was five for 4 weeks. Results showed loquat was effective in ameliorating the HF diet-induced hyperglycemia, hyperleptinemia, hyperinsulinemia, and hypertriglyceridemia, as well as decreasing the levels of free fatty acid (FFA), increasing adipose PPARγ (perixisomal proliferator-activated receptor γ) and hepatic PPARα mRNA levels. Loquat significantly decreased body weight gain, weights of white adipose tissue and visceral fat accompanying suppressed leptin mRNA levels. Results provide nutritional bias for use of loquat as a functional food factor with potential benefits for prevention of diabetes and hyperlipidemia. (16)
• Antitumor Activity / Leaves: In a search for antitumor agents from natural sources, study of E. japonica leaves isolated megastigmane glycosides and polyphenolic constituents, which were found to inhibit 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced activation of Epstein-Barr virus early antigen in Raji cells. Roseoside and procyanidin B-2 were among active compounds in an invitro assay. Further assessment of the two compounds in an invivo two-stage carcinogenesis assay on mouse skin, roseoside significantly delayed carcinogenesis induced by peroxynitrite (initiator) and TPA (promoter), with a potency comparable to green tea polyphenol, (-)-epigallocathechin 3-O-gallate, in the same assay. (17)
• Anti-Arthritic / Anti-Inflammatory / Leaves: Study evaluated the effect of leaves infusion on acute and persistent experimental articular inflammation in Swiss mice. Paw edema was induced by carrageenan (100 mg/kg), acute knee inflammation induced by zymosan (100 mg/kg), and persistent inflammation by Complete Freund's Adjuvant (CFA) (30 and 100 mg/kg). Chromatographic analysis of the extract revealed corosolic acid, oleanolic acid, and ursolic acid. Results showed anti-inflammatory activity in the pleurisy model, inhibition of leukocyte migration, protein extravasation and nitric oxide production. In the articular inflammation model, the extract reduced the number of leukocytes in the joint cavity, paw edema and hyperalgesic. In the persistent inflammation model, the extract reduced paw edema and cold hyperalgesic. Results indicated anti-inflammatory and antihyperalgesic potential, suggesting potential for the infusion as complementary treatment of acute and chronic articular inflammatory diseases. (18)
• Counteraction Against ROS and NO Stimulated by Chloramphenicol: Chloramphenicol is a toxic antibiotic used for certain infections, with aplastic anemia one of its side effects. In the presence of chloramphenicol, blood cells suffered oxidative stress, with significant increase in reactive oxygen species (ROS). Fruit extracts of E. japonica markedly decreased ROS in leukocytes and erythrocytes, the oxidative stress caused by the antibiotic. The immediate antioxidant effect of Ej could be associated with the action of vitamin A. The protective action of the fruit on mature leukocytes and erythrocytes and beneficial effect on blood cells suggest the extract can be used as an antioxidant agent complementing the administration of chloramphenicol. (19)
• Anti-Inflammatory Effects / Mechanisms / Loquat Tea: Loquat tea, called Biwa Cha in Japanese, is made from loquat leaves roasted at 350°C for 30 mins, and used as a health beverage in Japan. Study evaluated the anti-inflammatory effects and molecular mechanisms of loquat tea (LTE) in both cell and animal models. LTE, especially the C fraction, inhibited the production of pro-inflammatory factors including iNOS, NO, IL-6, RANTES, and TNFα. Cellular signaling data showed downregulation of TGF-ß-activated kinase (TAK1)-mediated both mitogen-activated protein kinase (MAPK) and NF-kB pathways involved in the inhibition of pro-inflammatory factors by C fraction. Mouse paw edema model confirmed the invivo anti-inflammatory effects of LTE. (20)
• Anticancer / Antioxidant / Fruit Juice: Study evaluated the invitro anticancer effect of E. japonica fruit juice on two cancer cell lines, human cervical cancer (HeLa), rhabdomyosarcoma (RD), and rat embryonic fibroblast (REF) as normal cell. The juice showed high antioxidant effect (100%) in 150 µg/ml concentration, followed by 88% in 100 µg/ml concentration. The juice exhibited significant cytotoxic effect (p<0.05) on HeLa cell line, more than on RD, with highest effect at 500 µg/ml in 48 hr. (21)
• Antimetastatic / Leaves: Study evaluated the anti-metastatic action of EtOAc fraction of leaves of E. japonica. Results showed potent inhibitory effects on MMP-2 and MMP-9 activities and expression via down-regulation of NF-kB translocation to the nucleus in B16F10 cells. Cell migration and invasion were down-regulated by extract. The extract significantly suppressed lung metastasis in vivo. Isolated compounds ursolic acid and 2α-hydroxyursolic acid from the extract also significantly suppressed MMP-2 and MMP-9 activities, indicating they are active components of the extract. Results suggest potential as a valuable antimetastatic agent for treatment of cancer metastasis. (22)
• Antidiabetic / Antihyperlipidemic / Oral Toxicity Study / Leaves: Study evaluated the antidiabetic and antihyperlipidemic effects of aqueous leaf extract (LLE) in mice fed a high-fat and high-glucose (HFG) diet for 10 weeks. LLE was administered at doses of 150, 200, and 250 mg/kbw, compared to metformin and pravastatin. Results showed LLE dose-dependently ameliort3d hyperglycemic, insulin resistance, oxidative stress, and hyperlipidemia in NFG diet-fed mice. The medial lethal dose of LLE was higher than 5000 mg/kbw. (23)
• Hypoglycemic / Sesquiterpene Glycoside / Leaves: Study of dried leaves isolated a sesquiterpene glycoside, nerolidol-3-O-α-L-rhamnopyranosyl(1-->4)-α-L-rhamnopyranosyl(1-->2)-[α-L-rrhamno-pyranosyl(1-->6)]-ß-D-glucopyranoside. The compound was tested for hypoglycemic effects in normal and alloxan-induced diabetic mice. Doses of 25 and 75 mg/kg exerted significant (p<0.05) hypoglycemic eff4ct in alloxan-diabetic mice, with a slight effect in normal mice. (24)
• Antioxidative Hesperitin and Gallic Acid / Flowers: HPLC analysis of E. japonica flower extract (EjFE) yielded hesperitin and gallic acid as major antioxidants. The flower extract revealed significantly high level of total polyphenols. The EJFE showed high ability to scavenge free radicals, reducing power, and Fe+2 chelating activity, which was attributed to high content of hesperitin and gallic acid in the flowers. (25)
• Acute and Subacute Toxicity Studies of Leaf Triterpene Acid / Safety: Study evaluated the toxicity of E. japonica leaf triterpene acid (ELTA) in ICR mice. Results showed no mortality nor toxicity in ICR mice in both acute (0.30, 0.65, 1.39, and 3.00 g/kbw) and subacute (150, 300, and 600 mg/kbw) 28-day toxicity studies. There were no adverse effects on hematological, clinical biochemistry, and histopatho-logical evaluation. Results suggest safety and a potential for ELTA as a dietary supplement. (26)
• Cytotoxicity Against Human Oral Tumor Cell Lines / Polyphenols / Leaves: Study of leaves isolated three new flavonoid glycosides, along with 15 known flavonoids, characterized as (2S)- and (2R)-naringenin 8-C-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosides, and cinchonain Id 7-O-β-D-glucopyranoside, respectively. The polyphenols were assessed for cytotoxic activity against two human oral tumor (human squamous cell carcinoma and human salivary gland tumor) cell lines. (27)
• Neuroprotective Against ß-Amyloid-Induced Oxidative Stress and Memory Impairment: Study evaluated the protective effect of E. japonica extract against Aß peptide-induced oxidative stress. DPPH assay showed the extract scavenged 40% of DPPH radicals. The extract inhibited Aß1-42-mediated neuronal cell death. It also suppressed increase in intracellular ROS triggered by Aß1-42 peptide. Mice treated with extract showed restoration of alternation behavior and reversal of Aß1-42-induced memory impairment. Extract also inhibited the increase in lipid peroxidation and restored superoxide dismutase activity. Results suggest protection from oxidative stress and cognitive deficits induced by Aß peptide. (28)
• Airway Remodeling Effects in Cough Variant Asthma / Leaves: Study, guided by traditional Chinese medicine theory of exterior-interior relationship between lungs and large intestine, evaluated the pathogenesis of cough variant asthma (CVA) and the treatment mechanism. Study explored the airway remodeling effects of EJL in CVA from perspective of the intestinal flora and the matrix metallo-peptidase 9tissue inhibitor of metalloproteinases-1 (MMP-9/TIMP-1) pathway. Results confirmed the positive effects of EJL on CVA. After administration of EJL, the number of coughs and the WAt/Pbm ratio decreased, the cough latency was prolonged, body weight increased, and general status improved. EJL decreased inflammatory cell infiltration and improved histopathological structure of the lung tissue. There was also significant inhibitory effects on expression of α-SMA, MMP-9, and TIMP-1, with normalized intestinal flora to a certain extent. Results suggest EJL alleviated airway remodeling of CVA mice, which may be related to the inhibition of MMP-P/TIMP-1 pathway and regulation of the intestinal flora. (29)
• Cardioprotective / Anti-Apoptosis / Anti-Fibrosis / Leaves: Myocardial apoptosis and fibrosis are contributing factors for development of hypertension-induced heart failure. Study evaluated the potential effects of E. japonica leaf extract (EJLE) against hypertension-induced cardiac apoptosis and fibrosis in spontaneously hypertensive rats (SHRs). Results showed supplementation with EJLE effectively attenuated cardiac apoptosis and fibrosis and also enhanced cell survival in hypertensive SHR hearts. (30)
• Antitussive / Expectorant / Fallen Leaves: In Chinese traditional medicine, dried leaves are used to treat cough with phlegm. Study evaluated fallen loquat leaves for effect on coughing and expectoration in mice. Both aqueous and ethanol extracts of growing and fallen leaves of loquat showed antitussive and expectorant activities. The aqueous extract of growing loquat leaves with higher flavonoid content displayed stronger expectorant activity while ethanol extract of fallen leaves with higher content of triterpenoid induced a stronger antitussive effect. (31)
• Anti-Inflammatory / PPY / Leaves: Pulmonary inflammation is associated with increased levels of iNOS, COX-2, and proinflammatory cytokines. Study used lipopolysaccharide (LPS) to include iNOS, COX-2, and cytokines (TNFα, IL1ß, and IL-8) productions in human lung epithelial cells (A-549). E. japonica leaf (Pi-Pa-Ye, PPY), a traditional Chinese medicine for treatment of pulmonary inflammation was capable of suppressing LPS-induced cytokine productions in a dose-dependent manner. Analysis of the anti-inflammatory effects of ursolic aid and oleanolic acid, the triterpene compounds present in PPY, showed ursolic acid significantly inhibited LPS-induced IL-8 production and iNOS mRNA expression. Oleanolic acid showed none of those effects. Study suggests the potential of PPY and its active component, ursolic acid, in the treatment of pulmonary inflammation. (32)
• Anti-Allergic / Leaves: Study evaluated the effect of E. japonica leaves (LEJL) on anaphylactic reaction and its possible mechanisms of action. LEJL inhibited compound 48/80-induced systemic anaphylactic reactions and serum histamine release in mice. LEJL decreased the production of TNF-α in phorbol 12-myristate 13-acetate and A23187-stimulated human mast cells. Results suggest potential for α as an anti-allergic agent. (also: see study 12) (33)
• Antimutagenic Antigenotoxic / Antioxidant / Leaves: Study evaluated the mutagenic/ antimutagenic, genotoxic/antigenotoxic, and antioxidant potentials of aqueous and total oligomers flavonoid (TOF) extracts from E. japonica. The highest protective effect against methyl methanesulfonate and 2-aminoanthracene was obtained in the presence of aqueous extract, with IC50 values of 80 and 140 µg/plate, respectively, against S. typhimurium TA104. The extract (500 µg/plate) also significantly reduced the genotoxicity induced by nitrofurantoin and aflatoxin B1 with IC50 values of 140 and 240 µg/assay, respectively. Results showed E. japonica extracts showed neither mutagenic nor genotoxic effect. E. japonica prevented the genotoxicity of some carcinogenic subtances probably through its antioxidant capacities. (34)
• α-Amylase Inhibition / Antioxidant / Leaves: Study evaluated the antioxidant activity and α-amylase inhibitory activity of E. japonica extracts of leaves. Total flavonoid and total phenolic contents were 0.38ss mg QAE/mg and 3.810 mg GAE/mg for methanolic and hexane extracts respectively. The ME showed higher DPPH free radical scavenging of 87% and lowest IC50 of 0.5336, which was below ascorbic acid used as control. Hexane extract showed higher α-amylase inhibitory activity of 24% at 1 µg/ml. Results provide support for the plant as an antidiabetic agent at higher concentrations. (35)
• Effect on Allergic Contact Dermatitis / Seeds: Study evaluated the anti-allergic activity of Eriobotrya japonica seeds extract (ESE). Oral administration dramatically inhibited ear swelling due to allergic contact dermatitis induced by repeated application of two antigens: 4-ethoxymethylene-2-phenyl-2-oxazolin-5-one (oxazolone) and dinitrofluorobenzene (DNFB). Increase of histamine content in inflamed ear tissue induced by oxazoline and DNFB was significantly antagonized by oral ESE. ESE suppressed eosinophil peroxidase and myeloperoxidase activity in both models. TNFα in the inflamed region caused by DNFB was also significantly suppressed. Results suggest ESE may be effective for treating allergic contact dermatitis. (36)
• Antiproliferative on Human Cancer Cells / Antioxidant / Aerial Parts: Study evaluated evaluated the effects of seed, flesh (seedless fruit) and leaves of loquat on antioxidative and anti-prolliferation in human cancer cells. Antioxidative indexes of leaf and seed ethanol extracts were high and similar to BHA and BHT. Antioxidative activities of seed and leaf ethanol extracts were higher in loquat flesh. The antiproliferation effect of seed and leaf ethanol extracts on liver cancer cell (H460), stomach cancer cell line (AGS), and lung cancer cell line (A549) showed higher values compared to flesh ethanol extract. Results suggest antioxidative and cancer preventive properties. (37)
• Hypoglycemic / Seeds: Study evaluated the hypoglycemmic effects of E. japonica seeds in type 2 diabetic Otsula Long-Evans Tokushima fatty (OLZEZTZFZ) rats and KK-A mice. Rats and mice were fed on a diet containing 10% powdered E. japonica seeds for 4 months. Serum insulin was significantly lower in OLETF rats fed on the Ej seed diet. Ej seeds suppressed increment of blood glucose and effectively improved glucose tolerance in the KK-A mice. Results suggest the seeds had a hypoglycemic property. (38)
• Hepatoprotective / Carbon Tetrachloride Hepatotoxicity / Leaves: Study evaluated the hepato-protective potential of Ej leaf extract and various fractions against CCl4-induced hepatotoxicity in rats. CCl4-treated rats given 250 and 500 mg/kg of ME of leaves or its fractions showed significantly lower levels of biochemical parameters such as ALT, AST, AP, total protein, GGT, and bilirubin levels. (39)
• Skin Care Effects / Leaves: Study evaluated 18 triterpenoids from E. japonica leaves for anti-melanogenesis, anti-acne, anti-allergy, and anti-aging activities. Eight compounds showed anti-melanogenesis activity, of which ursolic acid (1) and maslinic acid (7) were most potent with selective index similar to arbutin. Twelve compounds exhibited anti-acne effect, with ursolic acid (1), maslinic acid (7), corosolic acid (8) and euscaphic acid (12) showing highest activity against P. acnes. Four displayed anti-allergy and anti-inflammatory activity; 3-epicorosolic acid (9) and euscaphic acid (12) showed marked activity against β-hexosaminidase release. Ursolic acid (1), pomolic acid (10), colosolic acid (8),and its methylated derivative (6) exhibited highest anti-aging activity via stimulation of collagen and hyaluronic acid (HA) production. Results suggest potential applications as ingredients of functional foods or cosmetics products. (40)
• Antifungal Potentiating Activity Against Cyptococcus neoformans / Seeds and Leaves: Study evaluated the antifungal potential of various extracts of Ej against clinical isolates of Cryptococcus neoformans. The methanol extract of seeds and hexane extract of leaves exhibited the best antifungal activity with MIC values of 32 µg/mL. The combination of both extracts with nystatin and clotrimazole showed synergistic interactions with a 32-fold reduction in the MIC values of nystatin. Results suggest a potential source of new antifungals that could be used for treatment of cryptococcosis. (41)
• Inhibitory Effect on Migration, Adhesion, and Invasion of Human Breast Cancer Cells: Study evaluated the inhibitory effects of loquat methanol extracts of seeds and leaves on adhesion, migration, invasion and matrix metalloproteinase (MMP) activities of MDA-MB-231 breast cancer cell line. Results indicated the methanol extracts inhibited adhesion, migration, and invasion of human breast cancer cells partially through inhibition of MMP activity. The leaf extract showed more anti-metastatic effect. Results suggest potential as a chemopreventive agent in limiting breast cancer invasion and metastasis. (42)
• Anti-Proliferative and Apoptosis Induction in Human Leukemia Cell Lines / Corosolic Acid: Study evaluated the anti-proliferative activity of four triterpenes derived from Ej, corosolic acid (CA), ursolic acid (UA), maslinic acid (MA) ad oleanolic acid (OA), in human leukemia cell lines. CA showed the strongest antiproliferative activity in all leukemia cell lines tested. CA induced chromatin condensation, DNA fragmentation, Sub-G1 phase DNA, activation of caspase-3, -8, and -9 and cleavage of PARP in HL-60. Results suggest CA has antiproliferative effect on leukemia cells via induction of apoptosis mediated by mitochondrial dysfunction and caspase activation. CA has potential as a chemotherapeutic agent for treatment of human leukemia. (43)
• Triterpenoids as Natural PDE4 Inhibitors / Leaves: An ethanolic extract of leaves of Ej exhibited inhibitory activity against phosphodiesterase-4D (PDE4D), which is a therapeutic target of inflammatory disease. Bioassay-guided fractionation led to the isolation of a new triterpene, 3β-hydroxyl-21β-acetoxyl-urs-12-en-28-carboxylate (1), along with 7 known triterpenoids, methyl corosolate (2), ursolic acid (3), oleanolic acid (4), methyl maslinate (5), α-amyin (6), 3β,19α,23-trihydroxy-urs-12-ene (7) and uvaol (8). Compounds 2, 3 and 8 inhibited PDE4D2 effectively with IC50s of 3.06, 2.18, and 5.17 µM, respectively, which may provide a novel mechanism for the anti-inflammatory activity of Ej leaves. (44)
• Antiosteoclastogenesis Effect / Leaves: A previous study showed leaves of Ej exhibited potential to suppress ovariectomy-induced bone mineral density deterioration, and ursolic acid, the major bioactive component, suppressed osteoclast differentiation. Study revealed 11 additional terpenoids from the leaves with potent antiosteoclastogenesis effect. Pomolic acid showed particularly strong inhibitory activity, more potent than that of ursolic acid. (45)
• Butyryl Cholinesterase Inhibitory / Tyrosinase Inhibitory / Antioxidant / Leaves and Roots: UHPLC-QTOF-MS analysis to depict the phytochemical profile of loquat roots, leaves, stems, seeds, and fruits tentatively annotated 349 compounds, representing phytochemical classes that included flavonoids, phenolic acids, lignans, stilbenes, and terpenoids. In vitro antioxidant and enzyme inhibition assay evaluated the biological activity of different organs of Ej. Roots exhibited highest antioxidant activity in DPPH, ABTS, CUPRAX and FRAP assays showing 181.88, 275.48, 325.18, and 169.74 mg Trolox equivalent (TE)/g, respectively. Root extract strongly inhibited butyryl cholinesterase (3.64 mg galantamine equivalent GALAE/g), while leaves, stems, seeds and fruits showed comparable inhibition of both acetyl and butyryl cholinesterases. All tested organs exhibited invitro tyrosinase inhibition (57.27-71.61 mg Kojic Acid Equivalent KAE/g). Results suggest potential for food and pharmaceutical exploitation of different organs, especially roots, for enrichment with health-promoting phenolics and triterpenes. (46)
• Mercury Chloride Induced Hepatotoxicity / Flowers: Mercury (II) hepatotoxicity can enter the body through marine diets and amalgams Study evaluated the protective effect of Ej flower extract (EJFE) on HgCl2-induced hepatotoxicity in rats. Results showed HgCl2-induced oxidative damage led to a significant decrease in glutathione (GSH) and total antioxidant capacity (TAC). HPLC analysis of EJFE revealed hesperitin and gallic acid as major antioxidants in EJFE. Results showed the flower extract provided significant protection against HgCl2 induced hepatotoxicity in all diagnostic parameters via strengthening of antioxidant defense mechanisms and may have therapeutic function in free radical mediated diseases. (47)
• Antidiabetic / Antihyperlipidemic / Flowers: Study evaluated the effects of flower extracts of Ej on diabetes and hyperlipidemia in streptozotocin (STZ)-induced diabetic mice. Ej significantly lowered blood glucose, HbA1c, plasma triglycerides (TG), and total cholesterol (TC), but increase the size of islets of Langerhans within the pancreas. Ej notably elevated expression levels of p-Akt/t-Akt and
p-AMPK/t-AMPK
in skeletal muscles, implying the glucose-lowering effects may act through two pathways involvement in the insulin-Akt or/and AMPK activation. The antidiabetic and hypolipidemic activity may be related to tormentic acid, the major component of Ej. (49)
• Effect on Alcoholic and Non-Alcoholic Fatty Liver / Leaves: Study evaluated the potential protective effect of hot water extract of E. japonica leaves on EtOH- or free fatty acid (FFA)-induced fatty liver injury in vitro. Results showed potential preventive effects against both models of fatty liver disease by significant inhibition of oxidative stress by decreasing intracellular ROS formation and increasing the activities of antioxidant enzymes. It prevented lipid accumulation by restoring lipid metabolism by balancing FFA synthesis and ß-oxidation. (50)
• Inhibition of α-Amylase and α-Glucosidase: Study compared the inhibitory effects of alcoholic extracts from different Ej plant parts (roots, stems, leaves, flowers, pulp, seeds) on α-glucosidase and
α-amylase and the kinetic characteristics of enzymatic activity. Results showed alcohol extracts from different plant parts have α-glucosidase and α-amylase inhibitory activities. The order of α-glucosidase activity was flower > stem > root > leaf > pulp > seeds, while with α-amylase, root > stem > flower > leaf > pulp > seed. The E. japonica root had strongest inhibitory activity on α-amylase with IC50 of 1.51 g/L, which was reversible competitive inhibition type. (51)
• Efficacy / Cosmeceutical Safety / Leaves: Study evaluated the antioxidant, anti-inflammatory, and anti-melanogenic activities of EJ leaf ethanol extract (EJEE) and its potential irritation potential to skin and eye. Total phenolic content by HPLC was 88.68 mg tannic acid equivalent/g. EJEE showed concentration dependent DPPH radical scavenging activity. Anti-inflammatory effect of 0.5% (w/v) was demonstrated by reduction in lipopolysaccharide-induced nitric oxide and TNFα levels in RAW 264.7 cells. EJEE also significantly inhibited melanogenesis in melanocyte-stimulating hormone-induced B16F1 cells. EJEE did not show any irritation in skin and eye, and can be used as a cosmetic ingredient for skin improvement. (52)
• Relief of Allergic Rhinitis and Skin Conditions / Leaves / Clinical Trial: Randomized, controlled, double-blind trial on healthy adults age>20 to evaluated the efficacy of E. japonica leaves in the treatment of allergic rhinitis using 2.5 g of placebo or leaf supplements once daily for 4 weeks. Results showed significant differences in variability of itchy nose, itchy eyes, and eye symptoms. Arm skin transepidermal water loss was improved only in E. japonica supplementation group. Study suggests Ej leaves can be used as functional food ingredient to relieve allergic symptoms. (53)
• Effect on Adipogenesis / Anti-Obesity / Leaves: Study evaluated the anti-obesity effects of Eriobotrya japonica leaf extracts in 3T3-L1 adipocytes and ob/ob mice. 80% MeO)H, 50% EtOH, and processed water extracts of Ej leaves effectively inhibited lipid accumulation and expression of adipogenic transcription factors peroxisome proliferator-activated receptor (PPARγ) and CCAAP/enhancer-binding protein (C/EBPα) in 3T3-L1 adipocytes. Oral treatment with 50% EtOH extract at 200 or 400 mg/kbw for 12 weeks significantly reduced body weight and plasma triglycerides levels. Food efficiency ratio (FER) was significantly suppressed after treatment with water extract. Plasma protein level of adiponectin was high increased with 400 mg/kbw of 50% EtOH extract. Results suggest the 50% EtOH extract of Ej has an anti-obesity effect through regulation of adipogenic transcription factors, and plasma lipid and adiponectin levels in 3T3-L1 adipocytes and ob/ob mice. (54)
• Silver Nanoparticles / Anticancer, Anti-Allergic, Anti-Inflammatory: Study reports on the biomedical applications of silver NPs synthesis using leaf extracts of E. japonica. The AgNPs inhibited the proliferation of MCF-7 and HeLa cells, and reduced inflammation. Treatment with AgNPs significantly decreased allergic disorder. The AgNPs stimulated the phagocytosis process in BMDMs. Results suggest potential for preventing inflammation, reduce allergic disorders, and prevent bacterial infection through up-regulation of phagocytosis. The NPs can be improved into adjuvants, immune-modulating substances, nano-drug delivery systems. (55)
• Inhibition of 11ß-HSD1 / Potential for Metabolic Syndrome and T2 Diabetes / Leaves: Inhibition of 11ß-hydroxysteroid dehydrogenase 1 (11ß-HSD1), which catalyzes the conversion of inactive 11-ketoglucocorticoids to active 11ß-hydroxyglucocorticoids, is a promising strategy to treat symptoms of metabolic syndrome, including obesity and type 2 diabetes. Study evaluated loquat leaves following hints from a pharmacophore-based virtual screening and bioactivity-guided approach. Determination of 11ß-HSD1 and 11ß-HSD2 inhibitory activities in cell lysates revealed triterpenes from ursane type as low micro-molar inhibitors of 11ß-HSD1: corosolic acid (1), 3-epicorosolic acid methyl ester (4), 2-α hydroxy-3-oxo urs-12-en-28-oic acid (6), tormentic acid methyl ester (8), and ursolic acid (9). A mixture of constituents with moderate activities displayed a pronounced additive effect. Growing evidence suggest selective inhibition of 11ß-HSD1 lowers blood glucose concentrations, counteracts the accumulation of visceral fat and ameliorates related metabolic abnormalities in type 2 diabetes. (56)
• Cinchonain 1b / Effect on Insulin Secretion: Study evaluated Ej water extract (EJWE) and derived compounds viz., cinchonain 1b, procyanidin B-2, chlorogenic acid, and epicatechin for effects on insulin secretion from INS-1 cells following oral administration in rats. Results showed the EJWE significantly increased (p<0.05) insulin secretion from INS-1 cells in a dose-dependent manner. Cinchonain 1b significantly enhanced (p<0.05) insulin secretion from INS-1 cells, while epicatechin inhibited significantly (p<0.05) insulin secretion from INS-1 cells. Results suggest cinchonain 1b has an insulinotropic effect and suggests possible used or the management of T2 diabetes. (58)
• Estrogenic / Antiproliferative: Study screened herbal extracts commercially used in Asia for estrogenic activity with recombinant yeast system with both human estrogen receptor (ER) expression plasmid and a reporter plasmid. Eriobotrya japonica was among ones that showed estrogenic potency. In antiproliferative assay against five human cancer cell lines, E. japonica showed strong cytotoxicity in Er-negative breast cancer (MDA-MD-231), cervix epitheloid (HeLa), and lung (A549) carcinoma cell lines. (59)
• 3-O-(E)-p-coumaroyl Tormentic Acid / Apoptotic Cell Death in Human Leukemia Cell Line / Leaves: Study of Ej leaves isolated 11 triterpene acids, 1-11, which were evaluated for inhibition of DNA toposiomerase I (Topo) and cytotoxicity against human leukemia (HL60) and melanoma cell lines (CRL1579). Among the compounds tested, δ-oleanolic acid (4) ursolic acid (5), 3-O-(E)-p-coumaroyl tormentic acid (8), and betulinic acid (10) exhibited potent Topo I inhibitory activity (IC50 20.3-36.5 µM) and cytotoxicity against HL60 (EC50 5.0-8.1 µM). Compound 8 exhibited induction of apoptosis evidenced by DNA fragmentation and membrane phospholipid exposure in flow cytometry. Compound 8 induced apoptotic cell death in HL60 mainly via mitochondrial pathway partly by Topo I inhibition. Study suggests potential for compound 8 as drug for treatment of leukemia. (60)
• Loquat Flower Tea: Study evaluated the antioxidant and anti-inflammatory activities of loquat flower water extract (LFWE), along with the potential for developing sugar-free LF tea. Results showed LFWE at temperature above 80°C, heating for 60 min had higher content of bioactive compounds. Sensory evaluation revealed highest overall acceptability scores of LF tea extracted for 45 min (p<0.05). Study suggests potential of LF as functional beverages and foods. (61)
Availability
Wild-crafted.
Fruit and leaf extracts, teas in the cybermarket. |
Uses
