• Title/Summary/Keyword: inhibitory compounds

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Inhibitory Effect of the Hexane Extract of Saussurea lappa on the Growth of LNCaP Human Prostate Cancer Cells (목향 헥산추출물의 LNCaP 전립선암세포 증식 억제 효과)

  • Park, So-Young;Kim, Eun-Ji;Lim, Do-Young;Kim, Jong-Sang;Lim, Soon-Sung;Shin, Hyun-Kyung;Yoon Park, Jung-Han
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.1
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    • pp.8-15
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    • 2008
  • Saussurea lappa (SL) has been used to reduce abdominal pain and tenesmus in traditional oriental medicine. SL and major compounds of SL, sesquiterpene lactones, have been suggested to possess various biological effects, including anti-tumor, anti-ulcer, anti-inflammatory, anti-viral and cardiotonic activities. Recently, it has been reported that ethanol extracts from roots of SL have antiproliferative effects on gastric cancer cells. To explore the possibility that SL has chemopreventive effects on prostate cancer, we examined whether the hexane extract of SL (HESL) inhibits the growth of LNCaP human prostate cancer cells. Cells were incubated with various concentrations ($0{\sim}4$ mg/L) of HESL in DMEM/F12 containing 5% charcoal stripped fetal bovine serum. HESL substantially decreased viable cell numbers and induced apoptosis of LNCaP cells in dose-dependent manners. HESL increased the levels of cleaved caspase-8, -9, -7 and -3, and poly (ADP-ribose) polymerase. HESL increased the levels of the pro-apoptotic Bak and truncated-Bid proteins whereas it had no effect on the anti-apoptotic Bcl-2, Bcl-xL, or Mcl-1. The present results indicate that HESL inhibits the growth of human prostate cancer cells by inducing apoptosis, which involves the activation of the caspase cascades.

The effect of two Terpenoids, Ursolic acid and Oleanolic acid on epidermal permeability barrier and simultaneously on dermal functions

  • Lim Suk Won;Jung Sung Won;Ahn Sung Ku;Kim Bora;Ryoo Hee Chang;Lee Seung Hun
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.29 no.2 s.43
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    • pp.205-232
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    • 2003
  • Ursolic acid (UA) and Oleanolic acid (ONA), known as urson, micromerol and malol, are pentacyclic triterpenoid compounds which naturally occur in a large number of vegetarian foods, medicinal herbs, and plants. They may occur in their free acid form or as aglycones for triterpenoid saponins, which are comprised of a triterpenoid aglycone, linked to one or more sugar moieties. Therefore UA and ONA are similar in pharmacological activity. Lately scientific research, which led to the identification of UA and ONA, revealed that several pharmacological effects, such as antitumor, hepato-protective, anti-inflammatory, anticarcinogenic, antimicrobial, and anti-hyperlipidemic could be attributed to UA and ONA. Here, we introduced the effect of UA and ONA on acutely barrier disrupted and normal hairless mouse skin. To evaluate the effects of UA and ONA on epidermal permeability barrier recovery, both flanks of 8-12 week-old hairless mice were topically treated with either 0.01-0.1 mg/ml UA or 0.1-1 mg/ml ONA after tape stripping, and TEWL (Transepidermal water loss) was measured . The recovery rate increased in those UA or ONA treated groups (0.1 mg/ml UA and 0.5 mg/ml ONA) at 6 h more than $20\%$ compared to vehicle treated group (p<0.05). Here, we introduced the effects of UA and ONA on acute barrier disruption and normal epidermal permeability barrier function. For verifying the effects of UA and ONA on normal epidermal barrier, hydration and TEWL were measured for 1 and 3 weeks after UA and ONA applications (2mg/ml per day). We also investigated the features of epidermis and dermis using electron microscopy (EM) and light microscopy (LM). Both samples increased hydration compared to vehicle group from f week without TEWL alteration (p<0.005). EM examination using RuO4 and OsO4 fixation revealed that secretion and numbers of lamellar bodies and complete formation of lipid bilayers were most prominent $(ONA{\geq}UA>Vehicle)$. LM finding showed that thickness of stratum corneum (SC) was slightly increased and especially epidermal thickening and flattening was observed (UA>ONA>Veh). We also observed that UA and ONA stimulate epidermal keratinocyte differentiation via $PPAR\;\alpha$. Protein expression of involucrin, loricrin, and filaggrin increased at least 2 and 3 fold in HaCaT cells treated with either $ONA\;(10{\mu}M)$ or UA $(10{\mu}M)$ for 24h respectively. This result suggested that the UA and ONA can improve epidermal permeability barrier function and induce the epidermal keratinocyte differentiation via $PPAR\;{\alpha}$. Using Masson-trichrome and elastic fiber staining, we observed collagen thickening and elastic fiber elongation by UA and ONA treatments. In vitro results of collagen and elastin synthesis and elastase inhibitory activity measurements were also confirmed in vivo findings. These data suggested that the effects of UA and ONA related to not only epidermal permeability barrier functions but also dermal collagen and elastic fiber synthesis. Taken together, UA and ONA can be relevant candidates to improve epidermal and dermal functions and pertinent agents for cosmeseutical applications.

Biological Activity of Extracts from Chrysanthemum incidicum Linne by Ultrafine Grinding (미세분쇄에 의한 감국(Chrysanthemum incidicum Linne) 추출물의 생리활성)

  • Cho, Young-Je
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.1
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    • pp.110-117
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    • 2014
  • In this study, the biological activity of water and ethanol extracts from Chrysanthemum incidicum Linne by ultrafine grinding for functional food source are examined. The content of phenolic compounds from Chrysanthemum incidicum Linne were the highest when extracted for 6 hr with 70% ethanol. The extraction yield of water and ethanol extracts were $7.12{\pm}1.61$ mg/g and $7.51{\pm}2.14$ mg/g, respectively. With ultrafine grinding, water and ethanol extracts were $8.63{\pm}1.15$ mg/g and $9.33{\pm}1.35$ mg/g, respectively. In determining anti-oxidative activity of Chrysanthemum incidicum Linne extracts, DPPH of normal grinding extracts was 83.52% and ultrafine grinding was 92.37%. In ABTS radical cation decolorization, normal grinding, fine grinding, and ultrafine grinding extracts were 90% or higher. In antioxidant protection factor (PF), water and ethanol extracts of ultrafine grinding showed relatively high anti-oxidative activities of each 1.82 PF and 2.16 PF, respectively. The TBARS value of ultrafine grinding extracts were lower than normal grinding and fine grinding extracts. The inhibition activity on xanthin oxidase of Chrysanthemum incidicum Linne extracts was 67.53% in ultrafine grinded water extracts and 83.45% in ultrafine grinded ethanol extracts. Inhibition on xanthin oxidase of ethanol extracts showed a higher inhibition effect than water extracts, and ultrafine grinding was higher than normal grinding. In angiotensin converting enzyme inhibition activity, ultrafine grinding water extract was 24% or higher, and ethanol extract was 34% or higher. The elastase inhibition activity of ultrafine grinding extract was 25.56%, which was higher than 20.34% of fine grinding extracts. Water extracts did not show hyaluronidase inhibition activity but ethanol extracts showed 35% of hyaluronidase inhibition activity. The determining expression inhibition of iNOS and COX-2 protein in macrophage by Chrysanthemum incidicum Linne extracts with a Western blot analysis, iNOS and COX-2 protein expression inhibition by Chrysanthemum incidicum Linne ethanol extracts were 40% and 15%, respectively at 100 ${\mu}g/mL$ concentration. The inhibitory patterns of iNOS and COX-2 protein expression was concentration dependent. The result suggests that Chrysanthemum incidicum Linne extracts by ultrafine grinding may be more useful than normal grinding as potential sources due to anti-oxidation, angiotensin converting enzyme and xanthine oxidase inhibition, anti-inflammation effect.

Antibacterial, Antioxidant, and Antiaging Effects of the Ethanol Extract of Dolnamul (Sedum sarmentosum) and the Production of the Oil in Water Cream (돌나물(Sedum sarmentosum) 에탄올 추출물의 항균, 항산화, 항노화 효과와 수중유적형 크림의 제조)

  • Kim, Young Dae;Kim, Young Min;Mo, Eun Kyoung
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.43 no.3
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    • pp.211-221
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    • 2017
  • This study was performed to investigate the functional properties and characteristics of Dolnamul (Sedum sarmentosum) as a cosmetic ingredient. Lyophilized sedum powder was extracted with ethanol and stored at $-20^{\circ}C$ for the following experiments. Total polyphenol compounds of the ethanol extract of sedum (SE) was $27.98{\pm}0.34g/kg$(dry weight): epicatechin ($162.14{\pm}5.07mg/kg$), epigallocatechin ($55.99{\pm}2.49mg/kg$), and kaempferol ($47.96{\pm}3.02mg/kg$) were contained in the SE. The SE had organic radical scavenging capacity ($78.43{\pm}1.08%$) and metal reducing power (FRAP value $2.54{\pm}0.12$). FTC and TBARS assays confirmed that the SE inhibited the early stage of lipid peroxidation ($62.03{\pm}0.38%$) as well as the final stage of lipid peroxidation ($55.36{\pm}2.05%$), respectively. The SE (5 mg/mL, dry weight) was proved to have antibacterial effect on the growth of Propionibacterium acnes. The inhibitory percentages of the SE on elastase and collagenase activities were $38.94{\pm}7.09%$ and $78.94{\pm}2.49%$, respectively. Compare to the control group, the SE treated group induced an increase of Col3A1 expression and collagen production ($58.11{\pm}1.07%$). The oil in water emulsion (0.5% SE adding group) showed pH 6.88 and 1.47 g/mL of density. The hardness changes of the SE adding emulsions were not detected during the stored periods at various temperatures ($-20-45^{\circ}C$) for four weeks. It is considered that the SE has antibacterial, antioxidant, and antiaging activities.

Effects of Green Tea Extract on Intestinal Mucosal Esterification of $^{14}C$-Oleic Acid in Rats (녹차 추출물이 흰쥐 소장세포의 지방 에스테르화 과정에 미치는 영향)

  • Seo, Yun-Jung;Noh, Sang-K.
    • Food Science and Preservation
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    • v.15 no.3
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    • pp.450-455
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    • 2008
  • Previously, we have shown that green tea extract lowers the intestinal absorption of cholesterol, fat, and other fat-soluble compounds. We conducted this study to determine whether green tea extract affects the rate of $^{14}C$-oleic acid esterification into various lipids in the intestinal mucosa of rats. Male Sprague-Dawley ruts were had free access to a nutritionally adequate AIN-93G diet and deionized water. Initially, the rat's mucosal content of total lipids was measured following 1 mL olive oil administration with (green tea group) or without (control group) 100 mg green tea extract powder. At 1 h and 5 h, intestinal segments were extracted for total lipid analysis. Secondly, to measure mucosal esterification rates of lipids, an abdominal incision was made along the midline, and a 10-cm long jejunal segment of the small intestine was ligated in situ. Then, micellar solutions with or without green tea extract were injected into the ligated jejunal segments and incubated for 10 mill. The micellar solution contained $200.0\;{\mu}$ Ci $^{14}C$-oleic acid, $200.1\;{\mu}mol$ unlabelled oleic acid, $66.7\;{\mu}mol$ 2-monooleoylglycerol, $66.7\;{\mu}mol$ palmitoyl-sn-glycero-3-phosphocholine, 2.2 mmol glucose, $50.0\;{\mu}mol$ albumin, and 16.5 mmol Na-taurocholate per L of phosphate buffered saline (pH, 6.3) with or without 8.87 g green tea extract powder. At 10 min, each rat was sacrificed by cervical dislocation under anesthesia and the segment was removed for lipid analysis. Significant differences were observed in mucosal triglyceride content at 1 h and 5 h in ruts given green tea extract. Significant differences in the rate of $^{14}C$-oleic acid esterification into triglycerides and phospholipids fractions were observed between control and green tea groups. However, There were no significant differences in other lipid fractions. These results indicate that the lowered esterification rates of $^{14}C$-oleic acid into triglycerides and phospholipids fractions is attributable to presence of green tea extract. This may be associated with an inhibitory effect of green tea catechin on the mucosal processes of lipids, leading to the inhibition of intestinal absorption of lipids.

Anti-inflammatory and Antioxidant Effects of Spiraea prunifolia Sieb. et Zucc. var. simpliciflora Nakai in RAW 264.7 Cells (조팝나무 뿌리 열수 추출물이 RAW264.7 세포에서 미치는 항산화 및 항염증 활성)

  • Sim, Mi-Ok;Lee, Hyun Joo;Jang, Ji Hun;Lee, Hyo Eun;Jung, Ho-Kyung;Kim, Tae-Muk;No, Jong hyun;Jung, Jakyun;Jung, Da Eun;Cho, Hyun-Woo
    • Korean Journal of Plant Resources
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    • v.30 no.4
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    • pp.335-342
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    • 2017
  • Spiraea prunifolia Sieb. et Zucc. var. simpliciflora Nakai (SSN) has been used for the anti-inflammation in traditional folk medicine. To compare water and methanol extracts of SSN, we analyzed major components using LC IT TOF MS. The major components of hot water extract were identified as caffeic acid and p-coumaric acid, but methanol extract was not well established. However, methanol extract was detected with less polarity compounds compared to hot water extract. Next, we investigated the inhibitory effects of SSN water extract on the lipopolysaccharide (LPS)-induced inflammatory response or $H_2O_2-induced$ oxidative stress in Raw 264.7 macrophage cells. SSN strongly suppressed the production of nitric oxide in LPS-induced inflammatory response without cytotoxcity. The SSN possessed free radical scavenging activities such as DPPH ($IC_{50}=320.2{\mu}g/m{\ell}$), ABTS ($IC_{50}=124.0{\mu}g/m{\ell}$), and superoxide anion radical ($IC_{50}=122.6{\mu}g/m{\ell}$). The total phenol and flavonoid content of SSN was 56.7 mg/g, and 15.1 mg/g, respectively. Furthermore, SSN decreased the $H_2O_2-induced$ cytotoxicity by enhancing the cell viability, and SSN significantly reduced the intracellular reactive oxygen species (ROS) level. Therefore, SSN may be recommended as an effective strategy to prevent and/or treat various inflammation and ROS-induced diseases.

Evaluations on Deodorization Effect and Anti-oral Microbial Activity of Essential Oil from Pinus koraiensis (잣나무 정유의 소취효과 및 구강균에 대한 항균활성 평가)

  • Hwang, Hyun Jung;Yu, Jung-Sik;Lee, Ha Yeon;Kwon, Dong-Joo;Han, Woong;Heo, Seong-Il;Kim, Sun Young
    • Korean Journal of Plant Resources
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    • v.27 no.1
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    • pp.1-10
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    • 2014
  • Essential oils of various plants have been known for potential biological effects such as antibacterial, antifungal, spasmolytic, antiplasmodial activities and insect-repellent property. Recently, the essential oils have attracted considerable interest in oral disease therapy. This essential oil has been known as being effective on easing sick house syndrome, giving forest aroma therapy effect and acting as repellent against pest. The essential oil of Pinus koraiensi, a native plant from Hongcheon-gun, Gangwon-do, was obtained by hydrodistillation. In light of its medicinal importance, in this study its composition, antibacterial activity and the reducing effect of offensive odor have been analyzed. The composition of essential oil was determined by GC and GC-MS. We have identified 14 compounds, of which 1R-${\alpha}$-pinene (19.38 %), 3-carene (10.21 %), camphene (9.82 %), limonene (9.00 %), bicyclo[2,2,1] heptan-2-ol (8.76 %) and ${\beta}$-phellandrene (7.98 %) were the main components. Essential oils from P. koraiensis, Chamaecyparis obtusa, Abies holophylla and Pinus densiflora were compared in terms of alleviating effect of malodors caused from formaldehyde, ammonia, trimethylamine and methylmercaptan. P. koraiensis essential oil was found to decrease the amounts of ammonia and trimethylamine by 75.17 % and 77.36 %, respectively. Antibacterial activity against Streptococcus mutans and Streptococcus sobrinus, which were known as oral cavity inducer, was investigated using the paper disc agar diffusion method. The inhibition zone was observed against S. mutans (5.97 mm) and S. sobrinus (1.40 mm), respectively. P. koraiensis essential oil shown effective deodorization and inhibitory activity against oral cavity in this study might be potential material in oral sanitary industry.

Anti-oxidant and α-Glucosidase Inhibition Activity of Extracts or Fractions from Diospyros lotus L. Leaves and Quantitative Analysis of Their Flavonoid Compounds (고욤잎 추출물과 분획물의 항산화 및 alpha-glucosdiase 저해 활성 및 플라보노이드 화합물의 정량)

  • Kim, Seon-Young;Kim, Sang Jun;Kim, Ji-Ae;Kim, Da Hye;Kwak, Seol Hwa;Chung, Chang Ho;Jeon, In Hwa;Jang, Seon Il;Jeong, Seung-Il
    • Journal of Life Science
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    • v.24 no.9
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    • pp.935-945
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    • 2014
  • Persimmon leaves were commonly consumed as beverages, but were also used as popular folk medicine in Asia. The purpose of this work was to assess the biological activities of Diospyros Lotus L. extracts (DLLE). Various solvent extracts, including n-Hexnae, $CHCl_3$, EtOAc, and n-BuOH fractions, were obtained from the methanol extract of Diospyros Lotus L. leaves. The increasing interest in the powerful biological activity of plant phenolics and flavonoids outlined the necessity for determining their content in medicinal herbs. In this study, the total polyphenol and flavonoid contents (TPC and TFC) in the EA fraction were higher than those of other fractions. The biological activities of DLLE were tested using the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity assay, as well as superoxide dismutase (SOD) activity as an anti-oxidant effect and ${\alpha}$-glucosidase inhibitory activity as an anti-diabetic effect. The EA fraction with high TPC and TFC values showed the highest anti-oxidant effect and high ${\alpha}$-glucosidase inhibition. The EA fractions were further purified into eight fractions using open column chromatography. Higher anti-oxidant and anti-${\alpha}$-glucosidase activity were observed in polar fractions. The content of the flavonoids, including quercein-3-O-rutinoside, kaempferol-3-O-glucoside, myricetin, luteolin, and kaempferol, were analyzed in effective fractions using high-performance liquid chromatography (HPLC). The results suggest that DLLE have anti-oxidative and anti-diabetic effects and thus, have the potential as anti-diabetic materials and as a source for natural health products.

Effects of the Fermentation Periods on the Qualities and Functionality of the Vegetable Fermentation Broths (식물자원 발효액의 품질과 기능성에 미치는 발효기간의 영향)

  • Kim, Na-Mi;Lee, Jong-Won;Do, Jae-Ho;Park, Chae-Kyu;Yang, Jae-Won
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.6
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    • pp.293-299
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    • 2005
  • To determine optimal fermentation period of vegetables mixed with black sugar without innoculation of microorganisms, changes in chemical components, quality characteristics of the fermented broth and physiological functionality during the fermentation period were investigated, pH and $^{\circ}BX$ of the fermented broths were decreased gradually during the fermentation period. Except for radish, L and a color values of fermented broths were increased but b values were decreased during fermentation period. Viscosity of fermented broths of vegetables were decreased after 3 months of fermentation. ${\alpha}-Amylase$ activity in fermentation broth of brocolli, eggplant, cabbage, chicory, aralia, radish were increased to 460, 430, 180, 420, 560, 260 after six months fermentation period. In radish and tomato fermentation broth, invertase activity were increased to 200 and 460 units and cellulase activity were increased to 280 and 140 after six months fermentation period. The content of total phenolic compounds and electron donating ability were the highest after 2 to 4 months fermentation period and decreased thereafter. No significant level of tyrosinase inhibitory activity and SOD-like activity were observed. In the sensory evaluation test of aralia fermentation broth of droop, sweet and sour flavor and bitter, astringent taste were decreased during the fermentation period and droop tastes were highest in 3 months. In radish fermentation broth, radish flavor and pungent taste were decreased and sweet taste was increased during fermentation period. Acceptability in overall was the greatest after three months. Based on the results stated above, optimal fermentation period was appropriated 3 or 4 months.

Onion Beverages Improve Amyloid β Peptide-Induced Cognitive Defects via Up-Regulation of Cholinergic Activity and Neuroprotection (양파(Allium cepa L.) 음료의 콜린성 활성 증가 및 뇌신경세포 보호로 인한 Amyloid β Peptide 유도에 대한 인지장애 개선 효과)

  • Park, Seon Kyeong;Kim, Jong Min;Kang, Jin Yong;Ha, Jeong Su;Lee, Du Sang;Kim, Ah-Na;Choi, Sung-Gil;Lee, Uk;Heo, Ho Jin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.11
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    • pp.1552-1563
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    • 2016
  • To examine the cognitive function of onion (Allium cepa L.) beverages (odourless and fortified), we analyzed in vitro neuronal cell protection against $H_2O_2$-induced cytotoxicity and performed in vivo tests on amyloid beta ($A{\beta}$)-induced cognitive dysfunction. Cellular oxidative stress and cell viability were evaluated by DCF-DA assay and MTT assay. These results show that fortified beverage resulted in better neuronal cell protection than odourless beverage at lower concentration ($0{\sim}100{\mu}g/mL$). Fortified beverage also showed more excellent acetylcholinesterase (AChE) inhibitory activity ($IC_{50}$: 4.20 mg/mL) than odourless beverage. The cognitive functions of odourless beverage and fortified beverage in $A{\beta}$-induced neurotoxicity were assessed by Y-maze, passive avoidance, and Morris water maze tests. The results show improved cognitive function in both groups treated with beverages. After in vivo tests, cholinergic activities were determined based on AChE inhibition and acetylcholine levels, and antioxidant activities were measured as SOD, oxidized glutathione (GSH)/total GSH ratio, and MDA levels in mouse brain tissue. In a Q-TOF UPLC/MS system, main compounds were analyzed as follows: odourless beverage (five types of sugars and three types of phenolics) and fortified beverages (six types of phenolics and two types of steroidal saponins).