Platycodon grandiflorum root extract inhibits Aß deposition by breaking the vicious circle linking oxidative stress and neuroinflammation in Alzheimer's disease.

Alzheimer's disease (AD) is a progressive neurodegenerative disease accompanied by irreversible cognitive impairment. A deleterious feedback loop between oxidative stress and neuroinflammation in early AD exacerbates AD-related pathology. Platycodon grandiflorum root extract (PGE) has antioxidant and anti-inflammatory effects in several organs. However, the mechanisms underlying the effects of PGE in the brain remain unclear, particularly regarding its impact on oxidative/inflammatory damage and Aß deposition. Thus, we aim to identify the mechanism through which PGE inhibits Aß deposition and oxidative stress in the brain by conducting biochemical and histological analyses. First, to explore the antioxidant mechanism of PGE in the brain, we induced oxidative stress in mice injected with scopolamine and investigated the effect of PGE on cognitive decline and oxidative damage. We also assessed the effect of PGE on reactive oxygen species (ROS) generation and the expressions of antioxidant enzymes and neurotrophic factor in H2O2- and Aß-treated HT22 hippocampal cells. Next, we investigated whether PGE, which showed antioxidant effects, could reduce Aß deposition by mitigating neuroinflammation, especially microglial phagocytosis. We directly verified the effect of PGE on microglial phagocytosis, microglial activation markers, and pro-inflammatory cytokines in Aß-treated BV2 microglial cells. Moreover, we examined the effect of PGE on neuroinflammation, inducing microglial responses in Aß-overexpressing 5XFAD transgenic mice. PGE exerts antioxidant effects in the brain, enhances microglial phagocytosis of Aß, and inhibits neuroinflammation and Aß deposition, ultimately preventing neuronal cell death in AD. Taken together, our findings indicate that the therapeutic potential of PGE in AD is mediated by its targeting of multiple pathological processes.

Heat Treatment Enhances the Neuroprotective Effects of Crude Ginseng Saponin by Increasing Minor Ginsenosides.

Ginsenoside is the primary active substance of ginseng and has many pharmacological effects, such as anti-cancer, immune, regulating sugar and lipid metabolism, and antioxidant effects. It also protects the nervous and cardiovascular systems. This study analyzes the effects of thermal processing on the bioactivities of crude ginseng saponin. Heat treatment increased the contents of minor ginsenosides in crude saponins, such as Rg3, and heat-treated crude ginseng saponin (HGS) had better neuroprotective effects than non-treated crude saponin (NGS). HGS reduced glutamate-induced apoptosis and reactive oxygen species generation in pheochromocytoma 12 (PC12) cells, significantly more than NGS. HGS protected PC12 cells against glutamate-induced oxidative stress by upregulating Nrf2-mediated antioxidant signaling and downregulating MAPK-mediated apoptotic signaling. HGS has the potential for the prevention and treatment of neurodegenerative disorders, such as Alzheimer's and Parkinson's disease.

Extract of Aster koraiensis Nakai Leaf Ameliorates Memory Dysfunction via Anti-inflammatory Action.

Aster koraiensis Nakai (AK) leaf reportedly ameliorates health problems, such as diabetes. However, the effects of AK on cognitive dysfunction or memory impairment remain unclear. This study investigated whether AK leaf extract could attenuate cognitive impairment. We found that AK extract reduced the production of nitric oxide (NO), tumour necrosis factor (TNF)-α, phosphorylated-tau (p-tau), and the expression of inflammatory proteins in lipopolysaccharide- or amyloid-ß-treated cells. AK extract exhibited inhibitory activity of control specific binding on N-methyl-D-aspartate (NMDA) receptors. Scopolamine-induced AD models were used chronically in rats and acutely in mice. Relative to negative controls (NC), hippocampal choline acetyltransferase (ChAT) and B-cell lymphoma 2 (Bcl2) activity was increased in rats chronically treated with scopolamine and fed an AK extract-containing diet. In the Y-maze test, spontaneous alterations were increased in the AK extract-fed groups compared to NC. Rats administered AK extract showed increased escape latency in the passive avoidance test. In the hippocampus of rats fed a high-AK extract diet (AKH), the expression of neuroactive ligand-receptor interaction-related genes, including Npy2r, Htr2c, and Rxfp1, was significantly altered. In the Morris water maze assay of mice acutely treated with scopolamine, the swimming times in the target quadrant of AK extract-treated groups increased significantly to the levels of the Donepezil and normal groups. We used Tg6799 Aß-overexpressing 5XFAD transgenic mice to investigate Aß accumulation in animals. In the AD model using 5XFAD, the administration of AK extract decreased amyloid-ß (Aß) accumulation and increased the number of NeuN antibody-reactive cells in the subiculum relative to the control group. In conclusion, AK extract ameliorated memory dysfunction by modulating ChAT activity and Bcl2-related anti-apoptotic pathways, affecting the expression of neuroactive ligand-receptor interaction-related genes and inhibiting Aß accumulation. Therefore, AK extract could be a functional material improving cognition and memory.

Crude Saponin from Platycodon grandiflorum Attenuates Aß-Induced Neurotoxicity via Antioxidant, Anti-Inflammatory and Anti-Apoptotic Signaling Pathways.

Although Platycodon grandiflorum saponins exhibit many beneficial biological effects in various diseases and conditions, how they protect nerve cells against neurodegenerative diseases and Alzheimer's disease (AD) pathology is unknown. We investigated whether P. grandiflorum crude saponin (PGS) protects neurons from neurodegeneration caused by amyloid beta (Aß)-induced oxidative stress. Hippocampal neuron HT-22 cells were used in the in vitro experiment, and AD mice (5XFAD mice) were used as the in vivo model. Intracellular reactive oxygen species (ROS) was stained with DCF-DA and assessed using fluorescence microscopy. To elucidate the mechanism underlying neuroprotection, intracellular protein levels were assessed by western blotting. In 5XFAD mice, an animal model of AD, nerve damage recovery due to the induction of Aß toxicity was evaluated by histological analysis. PGS attenuates Aß-induced neurotoxicity by inhibiting Aß-induced reactive oxygen species (ROS) production and apoptosis in HT-22 cells. Furthermore, PGS upregulated Nrf2-mediated antioxidant signaling and downregulated NF-κB-mediated inflammatory signaling. Additionally, PGS inhibited apoptosis by regulating the expression of apoptosis-associated proteins. In addition, PGS ameliorated Aß-mediated pathologies, leading to AD-associated cognitive decline. Conclusions: Taken together, these findings suggest that PGS inhibits Aß accumulation in the subiculum and cerebral cortex and attenuates Aß toxicity-induced nerve damage in vitro and in vivo. Therefore, PGS is a resource for developing AD therapeutics.

Antioxidant and Anti-Melanogenic Activities of Heat-Treated Licorice (Wongam, Glycyrrhiza glabra × G. uralensis) Extract.

Melanin is a brown or black pigment that protects skin from ultraviolet radiation and reactive oxygen species (ROS). However, overproduction of melanin is associated with lentigines, melasma, freckles and skin cancer. Licorice has shown antioxidant, anti-tumor, anti-platelet, anti-inflammatory and immunomodulatory activities and is used as a natural treatment for skin whitening. We aimed to confirm the potential of Wongam, a new cultivar of licorice developed by the Rural Development Administration (RDA), as a whitening agent in cosmetics. In addition, we verified the effect of heat treatment on the bioactivity of licorice by comparing antioxidant and anti-melanogenic activities of licorice extract before and after heating (130 °C). The heat-treated licorice extract (WH-130) showed higher radical-scavenging activities in the ABTS+ (2,2'-azino-bis-(3-ethylbenzothiazolin-6-sulfonic acid) diammonium salt) and DPPH (2,2-diphenyl-1-picrylhydrazyl) assays. In addition, WH-130 inhibited melanogenesis more effectively due to downregulation of tyrosinase in B16F10 melanoma cells than non-heated licorice extract. Moreover, heat treatment increased total phenolic content. In particular, isoliquiritigenin, an antioxidant and anti-melanogenic compound of licorice, was produced by heat treatment. In conclusion, WH-130, with increased levels of bioactive phenolics such as isoliquiritigenin, has potential for development into a novel skin whitening material with applications in cosmetics.

Antioxidative and antidiabetic effects of germinated rough rice extract in 3T3-L1 adipocytes and C57BLKS/J-db/db mice.

BACKGROUND: To overcome disadvantages of germinated brown rice, we germinated rough rice and tested effects of its useful ingredients on prevention of diabetes. OBJECTIVE: This study investigated the in vitro antioxidant and in vivo antidiabetic effects of rough rice (Oryza sativa L.) with hulls, before and after germination. Rough rice was germinated for 4 days and extracted with water at 120°C. DESIGN: This study measured antioxidants and antioxidative effects and inhibitory activities against α-amylase and α-glucosidase of rough rice before and after germination and investigated antidiabetic effects of rough rice through animal experiments. RESULTS: All these factors increased after germination. Also, α-amylase and α-glucosidase inhibition and glucose uptake by 3T3-L1 adipocytes were significantly increased after germination. Oral administration of the germinated rough rice extract for 8 weeks significantly increased insulin levels and decreased blood glucose levels in a C57BLKS/J-db/db mice model. Immunohistochemical analysis showed that germinated rough rice effectively protected against liver, kidney, and pancreatic tissue damage. DISCUSSION: Useful ingredients in germinated rough rice could be used to prevent diabetes. CONCLUSIONS: These results suggest that germinated rough rice extract had a beneficial effect on diabetes by increasing the antioxidant activity and further purification studies are necessary to elucidate the mechanism of the extract's antidiabetic activity.

Physical properties of surimi sausages subjected to high hydrostatic pressure treatment.

We aimed to investigate the effect of high pressure treatment (HPT) on the physical properties of surimi sausages. For protein gelation, high hydrostatic pressure of 400, 500, and 600 MPa was applied for 5, 15, and 30 min, respectively. Elasticity of samples containing 50% surimi was 36.68%, but that of samples containing 70% surimi was 36.87-42.88%. Shear and puncture forces for 50% surimi samples subjected to heat treatment were 1543.25 N and 3337.92 N/mm, respectively, while the shear and puncture forces for 70% surimi samples under all treatment conditions were 226.41-429.61 N and 911.72-1486.98 N/mm, respectively. After HPT, the number of pores increased from 27 to 73 with increasing pressure and time while the pores were elliptically shaped for samples subjected to heat treatment after HHPT. These results suggest that HPT improves the physical properties of surimi sausages with lower starch content.

Differences in anti-inflammatory effect of immature and mature of Rubus coreanus fruits on LPS-induced RAW 264.7 macrophages via NF-κB signal pathways.

BACKGROUND: Rubus coreanus fruit (RF) has been used as a traditional medicine formulation to treat various diseases including diarrhea, asthma, and cancer in East Asia (Korea, China, and Japan). RF, which is native to Korea, has a larger fruit size than that of exotic species. In this study, we aimed to compare the anti-inflammatory activities of immature and mature RF extracted with different solvents. METHODS: Mature and immature RF (MRF and IRF) were extracted with 30% ethanol, 70% ethanol and water at room temperature. The antioxidant activity was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) assays. Anti-inflammatory activity was determined by measuring nitric oxide (NO) production, expression of inflammatory proteins (inducible NO synthase [iNOS], cyclooxygenase [COX]-2, nuclear factor [NF]-κB, and inhibitor of NF-κB [IκB]), and inflammatory cytokines using polymerase chain reaction in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. RESULTS: The IRF 30% ethanol extract showed higher radical scavenging activity in DPPH and ABTS assays (half-maximal inhibitory concentration [IC50] 16.0 ± 0.5 and 15.9 ± 0.4) than MRF did. In addition, the IRF 30% ethanol extract (200 µg/mL) significantly reduced the production of the inflammatory mediator NO by approximately 80% and inhibited iNOS, COX-2, phosphorylated (p)-IκB, and p-NF-κB activation compared with MRF. Moreover, IRF extract decreased the inflammatory cytokines tumor necrosis factor-α, interleukin (IL)-1ß, and IL-6 compared with the MRF extract. CONCLUSIONS: This study revealed that IRF showed more beneficial effects than MRF did in LPS-stimulated RAW 264.7 macrophages, suggesting that IRF may be a useful anti-inflammatory agent.

Influence of organic acids and heat treatment on ginsenoside conversion.

BACKGROUND: Heat treatments are applied to ginseng products in order to improve physiological activities through the conversion of ginsenosides, which are key bioactive components. During heat treatment, organic acids can affect ginsenoside conversion. Therefore, the influence of organic acids during heat treatment should be considered. METHODS: Raw ginseng, crude saponin, and ginsenoside Rb1 standard with different organic acids were treated at 130°C, and the chemical components, including ginsenosides and organic acids, were analyzed. RESULTS: The organic acid content in raw ginseng was 5.55%. Organic acids were not detected in crude saponin that was not subjected to heat treatment, whereas organic acids were found in crude saponin subjected to heat treatment. Major ginsenosides (Rb1, Re, and Rg1) in ginseng and crude saponin were converted to minor ginsenosides at 130°C; the ginsenoside Rb1 standard was very stable in the absence of organic acids and was converted into minor ginsenosides in the presence of organic acids at high temperatures. CONCLUSION: The major factor affecting ginsenoside conversion was organic acids in ginseng. Therefore, the organic acid content as well as ginsenoside content and processing conditions should be considered important factors affecting the quality of ginseng products.

Effect of sorghum ethyl-acetate extract on benign prostatic hyperplasia induced by testosterone in Sprague-Dawley rats.

Benign prostatic hyperplasia (BPH) is commonly observed in men > 50 years worldwide. Phytotherapy is one of the many treatment options. Sorghum (Sorghum bicolor L.) contains various health-improving phytochemicals with antioxidant and inhibitory activities on cell proliferation, both in vitro and in vivo. To confirm the effects of Donganme sorghum ethyl-acetate extract (DSEE) on BPH, we induced BPH in Spragye-Dawley rats using exogenous testosterone. We measured prostate weight, examined prostrates histopathologically, and analyzed mRNAs associated with male hormones and proteins associated with cell proliferation in the prostate. DSEE inhibited weight gain of the prostate; decreased mRNA expressions of androgen receptor and 5α-reductase II; and improved histopathological symptoms, the protein-expressed ratio of Bax/Bcl-2, and the oxidative status of BPH induced by testosterone in SD rats. Therefore, DSEE may have potential as a preventive or therapeutic agent against BPH.

Protective Effect of Safflower Seed on Cisplatin-Induced Renal Damage in Mice via Oxidative Stress and Apoptosis-Mediated Pathways.

Cisplatin, a platinum chelate with potent antitumor activity against cancers of the testis, ovary, urinary bladder, prostate, and head and neck, has adverse effects on the kidney, bone marrow, and digestive organs, and its use is particularly limited by nephropathy as a side effect. In the present study, safflower seed extract was administered to a mouse model of cisplatin-induced acute renal failure to investigate its activity. Cisplatin (20[Formula: see text]mg/kg body weight) was administered by intraperitoneal injection to mice that had received oral safflower seed extract (100 or 200[Formula: see text]mg/kg body weight per day) for the preceding 2 days. Three days after the cisplatin injection, serum and renal biochemical factors; oxidative stress, inflammation, and apoptosis-related protein expression; and histological findings were evaluated. Cisplatin-treated control mice showed body-weight, food intake and water intake loss, and increased kidney weight, whereas the administration of safflower seed extract attenuated these effects ([Formula: see text], [Formula: see text]). Moreover, safflower seed extract significantly decreased the renal functional parameters urea nitrogen and creatinine in the serum ([Formula: see text] and [Formula: see text], respectively). Safflower seed extract also significantly reduced the enhanced levels of reactive oxygen species in the kidney observed following cisplatin treatment, with significance. The expression of proteins related to the anti-oxidant defense system in the kidney was down-regulated following cisplatin treatment, but safflower seed extract significantly up-regulated the expression of the anti-oxidant enzyme catalase. Furthermore, safflower seed extract reduced the overexpression of phosphor (p)-p38, nuclear factor-kappa B p65, cyclooxygenase-2, inducible nitric oxide synthase, ATR, p-p53, Bax, and caspase 3 proteins, and mice treated with safflower seed extract exhibited less renal histological damage. These results provide important evidence that safflower seed extract exerts a pleiotropic effect on several oxidative stress- and apoptosis-related parameters and has a renoprotective effect in cisplatin-treated mice.

Comparison of functional components in various sweet potato leaves and stalks.

The functional components of leaves and stalks from 14 sweet potato cultivars were investigated by determining lutein, ß-carotene, chlorophyll, tannin and phenolic acid contents. It was found that the contents of the functional components in different cultivars differ significantly (p<0.05). Lutein, ß-carotene and total chlorophyll contents were high in leaves and ranged from 19.01-28.85, 35.21-52.01 and 440.9-712.2 mg/100 g, respectively. The tannin and total phenolic acid contents of sweet potato leaves ranged from 2,280-4,460 and 2,640.2-4,200.9 mg/100 g, respectively. Significant correlations have been observed among cultivar, lutein, ß-carotene, chlorophyll, and other antioxidants. The leaves of Healthymi cultivar contained the highest level of lutein, ß-carotene and total chlorophyll, and Geonpungmi cultivar contained the highest level of the other antioxidant, among the all cultivars examined. Sweet potato leaves and stalks contain abundant functional components that make them potentially useful as fresh vegetables or processed foods.

Changes of phenolic-acids and vitamin E profiles on germinated rough rice (Oryza sativa L.) treated by high hydrostatic pressure.

This study was performed to investigate changes in the phenolic acid and vitamin E profiles of germinated rough rice following high hydrostatic pressure treatment (HPT). Rough rice was germinated at 37°C for two days and subjected to 0.1, 10, 30, 50, and 100MPa pressures for 24h. The total phenolic acid content increased from 85.37µg/g at 0.1MPa to 183.52µg/g at 100MPa. The highest gallic acid (4.29µg/g), catechin (9.55µg/g), p-coumaric acid (8.36µg/g), ferulic acid (14.99µg/g), salicylic acid (14.88µg/g), naringin (6.18µg/g), trans-cinnamic acid (45.23µg/g), and kaempferol (40.95µg/g) contents occurred in the sample treated at 100MPa after germination. The maximum vitamin E content of about 2.56 (BG) and 4.34mg/100g (AG) were achieved at 30MPa. These result suggest that a combination of HPT and germination are efficient method for enhancement of functionality in rough rice, and clarify the influence of HPT conditions on the vitamin E and phenolic acid in germination rough rice.

A silk peptide fraction restores cognitive function in AF64A-induced Alzheimer disease model rats by increasing expression of choline acetyltransferase gene.

This study investigated the effects of a silk peptide fraction obtained by incubating silk proteins with Protease N and Neutrase (SP-NN) on cognitive dysfunction of Alzheimer disease model rats. In order to elucidate underlying mechanisms, the effect of SP-NN on the expression of choline acetyltransferase (ChAT) mRNA was assessed in F3.ChAT neural stem cells and Neuro2a neuroblastoma cells; active amino acid sequence was identified using HPLC-MS. The expression of ChAT mRNA in F3.ChAT cells increased by 3.79-fold of the control level by treatment with SP-NN fraction. The active peptide in SP-NN was identified as tyrosine-glycine with 238.1 of molecular weight. Male rats were orally administered with SP-NN (50 or 300mg/kg) and challenged with a cholinotoxin AF64A. As a result of brain injury and decreased brain acetylcholine level, AF64A induced astrocytic activation, resulting in impairment of learning and memory function. Treatment with SP-NN exerted recovering activities on acetylcholine depletion and brain injury, as well as cognitive deficit induced by AF64A. The results indicate that, in addition to a neuroprotective activity, the SP-NN preparation restores cognitive function of Alzheimer disease model rats by increasing the release of acetylcholine.

Isolation and Identification of an Antiproliferative Compound from Fructose-Tryptophan Maillard Reaction Products.

This study was performed to isolate and identify a compound with antiproliferative activity against human stomach cancer cell lines, from fructose-tryptophan Maillard reaction products (MRPs). The MRPs, prepared from a fructose-tryptophan solution heated at 130 °C for 2 h, were fractionated into five solvent fractions: n-hexane, chloroform, ethyl acetate, butanol, and water. The highest antiproliferative activity was found in the chloroform fraction (85.93% at 200 µg/mL), and the active compound from this chloroform fraction was purified by silica gel column chromatography, TLC, and preparative HPLC. The antiproliferative activity (IC50) of the active compound was 42.24 µg/mL, and the active compound was identified as perlolyrine (C16H10N2O2) by (1)H/(13)C NMR, DEPT, HMBC, and LC-ESI-MS. Therefore, this research may be useful in developing perlolyrine as a functional therapeutic agent.

Physicochemical and in vitro binding properties of barley ß-glucan treated with hydrogen peroxide.

This study investigated the changes in content, purity, physical properties, and in vitro binding properties of barley ß-glucan by oxidation treatment. Barleys (Hordeum vulgare) were oxidized, using different concentrations of hydrogen peroxide (0.2-1.0% H2O2). The total and soluble ß-glucan contents ranged from 8.41% and 4.81% in the control to 9.48% and 6.45% in the 0.6% H2O2 treatment. With increasing H2O2 concentration, the purity of ß-glucan increased from 35% to 70%, whereas molecular weight (MW), viscosity, and water-binding capacities decreased to 2.0 × 10(4)Da, 3.9 cP, and 4.45 g water/g ß-glucan, respectively. Oil binding capacities ranged from 8.29 g of oil/g in non-oxidized ß-glucan to 9.42 g of oil/g in ß-glucan oxidized with 0.6% H2O2. The MW, viscosity, and binding capacities of waxy barley ß-glucan were higher than those of non-waxy barley ß-glucan. Oxidation by hydrogen peroxide improved the physical properties and in vitro binding capacity of barley ß-glucan.

Free and bound form bioactive compound profiles in germinated black soybean (Glycine max L.).

This study investigated the transition between the free and bound forms of functional compounds in germinated black soybean. Black soybean was germinated at 25°C over 6 days and then the free and bound forms of functional compounds were extracted. Total free polyphenol, flavonoid, and phenolic acid contents in raw black soybean increased from 1.03 mg GAE/g, 0.29 mg CE/g, and 315.67 µg/g to 1.44mg GAE/g, 0.64mg CE/g, and 511.01 µg/g, respectively, by 4 days after germination. Changes to phenolic acid compositions can be divided into four groups, and the germination process can convert compounds to phenolic acid via anabolism and catabolism. The highest total free isoflavone content in germinated black soybean (3,724.40 µg/g) was observed at 4 days. Bound polyphenol, flavonoid, phenolic acid, and isoflavone contents decreased as the germination period increased. These results suggest that the germination process increased compound functionality in black soybean.

Physicochemical Properties of ß-Glucan from Acid Hydrolyzed Barley.

This study was performed to investigate changes in the content and purity, as well as physical characteristics of ß-glucan extracted from acid hydrolyzed whole grain barleys. Waxy and non-waxy barleys (Hordeum vulgare) were hydrolyzed with different concentrations of HCl (0.1~0.5 N) for 1 h. As the HCl concentration increased, the contents of total and soluble ß-glucan from acid hydrolyzed barley decreased. However the ratio of soluble/total ß-glucan content and purities of ß-glucan significantly increased. The ratio of ß-(1→4)/ß-(1→3) linkages, molecular weight, and viscosity of soluble ß-glucan of raw barleys were 2.28~2.52, 6.0~7.0×10(5) g/mol, and 12.8~32.8 centipoise (cP). Those of isolated soluble ß-glucan were significantly decreased to 2.05~2.15, 6.6~7.8×10(3) g/mol, and 3.6~4.2 cP, respectively, with increasing acid concentration. The re-solubility of raw barley ß-glucan was about 50%, but increased to 97% with increasing acid concentration. Acid hydrolysis was shown to be an effective method to produce ß-glucan with high ratio of soluble ß-glucan content, purity, water solubility, and low viscosity.

Changes in ginsenoside compositions and antioxidant activities of hydroponic-cultured ginseng roots and leaves with heating temperature.

BACKGROUND: This study evaluated changes in ginsenoside compositions and antioxidant activities in hydroponic-cultured ginseng roots (HGR) and leaves (HGL) with heating temperature. METHODS: Heat treatment was performed at temperatures of 90°C, 110°C, 130°C, and 150°C for 2 hours. RESULTS: The ginsenoside content varied significantly with heating temperature. The levels of ginsenosides Rg1 and Re in HGR decreased with increasing heating temperature. Ginsenosides F2, F4, Rk3, Rh4, Rg3 (S form), Rg3 (R form), Rk1, and Rg5, which were absent in the raw ginseng, were formed after heat treatment. The levels of ginsenosides Rg1, Re, Rf, and Rb1 in HGL decreased with increasing heating temperature. Conversely, ginsenosides Rk3, Rh4, Rg3 (R form), Rk1, and Rg5 increased with increasing heating temperature. In addition, ginsenoside contents of heated HGL were slightly higher than those of HGR. The highest extraction yield was 14.39% at 130°C, whereas the lowest value was 10.30% at 150°C. After heating, polyphenol contents of HGR and HGL increased from 0.43 mg gallic acid equivalent/g (mg GAE eq/g) and 0.74 mg GAE eq/g to 6.16 mg GAE eq/g and 2.86 mg GAE eq/g, respectively. CONCLUSION: Antioxidant activities of HGR and HGL, measured by 1,1-diphenyl-2-picrylhydrazyl and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging ability, increased with increasing heating temperature. These results may aid in improving the biological activity and quality of ginseng subjected to heat treatments.