• Title/Summary/Keyword: Release effect

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Effect of ${\gamma}$-mangostin through the inhibition of 5-hydroxytryptamine$_{2A}$ receptors in 5-fluoro-${\alpha}$-methyltryptamine-induced head-twitch responses of mice

  • Nattaya Chairungsrie;Furukawa, Ken-Ichi;Takeshi Tadano;Kensuke Kisara;Yasushi Ohizumi
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.170-170
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    • 1998
  • In order to discover new types of 5-hydroxytryptamine antagonists, we have devoted our attention to investigating naturally occurring compounds having anti-5HT activity in vitro. Recently, ${\gamma}$-mangostin [1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-bytenyl)-9H-xanthen-9-one] from the fruit hull of Garcinia mangostana Linn has been shown to be a selective antagonist for 5-hydroxytryptamine$_{2A}$ receptors in smooth muscle and platelets. It is of interesting that y-mangostin which does not have a nitrogen atom, possesses marked 5-$HT_{2A}$ receptor blocking activity. The present study was undertaken to investigate the effects of ${\gamma}$-mangostin on central 5-HT receptors by using animal behavioural models. Intracerebronventricular injection of ${\gamma}$-mangostin (10-40n mol/mouse) inhibited 5-fluoro-${\alpha}$-methyltryptamin (5-FMT) (45 mg kg$^{-1}$, i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (5-HT-uptake inhibitor). Neither the 5-FMT- nor the 8-hydroxy-2-( di-n-propylamino )tetralin (5-HT$_{1A}$-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by ${\gamma}$-mangostin. The locomotor activity stimulated by 5-FMT through the activation of at-adrenoceptors did not alter in the presence of ${\gamma}$-mangostin. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. ${\gamma}$-Mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation and the binding of [$^3H$]-spiperone, a specific 5-$HT_{2A}$ receptor antagonist, to mouse brain membranes. Kinetic analysis of the [$^H3$]-spiperone binding revealed that ${\gamma}$-mangostin increased the $_{d}$ value without affecting the $B_{max}$ value, indicating the mode of the competitive nature of the inhibition by ${\gamma}$-mangostin. These results suggest that ${\gamma}$-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-$HT_{2A}$ receptors not by blocking the release of 5-HT from the central neurone. ${\gamma}$-Mangostin is a promising 5-$HT_{2A}$ receptors antagonist in the central nervous system.m.

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Evaluating the Effect of Upper Dams Release on Downstream Water Quality in Nakdong River Basin (낙동강수계 다목적댐군의 방류량과 하류 수질과의 관계 분석)

  • Choi, Jung-Kyu;Kim, Yu-Kyung;Jung, Yong-Rak;Shin, Sang-Il;Chung, Se-Woong
    • Proceedings of the Korea Water Resources Association Conference
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    • 2007.05a
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    • pp.1307-1311
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    • 2007
  • 유역의 자연 유출량이 줄어드는 갈수기 동안 낙동강 본류의 수질은 상류지역의 댐 방류량에 큰 영향을 받는다. 따라서 수질이 취약한 중 하류부지역의 수량과 수질을 종합적으로 고려한 낙동강 수계의 물 관리를 위해서는 댐 방류량과 하류 수질의 정량적인 관계에 근거한 다목적댐군의 연계운영이 필요하다. 본 연구의 목적은 정상상태 하천수질모델을 이용하여 낙동강수계 다목적댐군의 방류량과 하류 하천의 수질 관계를 정량적으로 분석하고, 갈수기 동안 낙동강 수질개선을 위해 필요한 적정 댐 용수공급 시나리오를 제시하는데 있다. 낙동강수계 댐 군의 하류 하천 수질을 고려한 저수지운영 계획 수립을 지원하기 위하여 1차원 정상상태 수질예측모델인 QUAL2E를 구축하고 실측 유량과 수질자료를 이용하여 모델을 보정하고 검증하였다. 검증된 모델은 낙동강수계 상류에 위치한 안동댐, 임하댐, 그리고 중 하류 지류에 위치한 합천댐과 남강댐의 용수공급 시나리오별 하천 수질개선 효과를 분석하는데 적용하였다. 연구결과 낙동강 수질이 악화되는 갈수기 동안 중 하류부에 위치한 상수원의 수질을 개선하기 위해서는 합천댐과 남강댐에서보다는 상류에 위치한 안동댐과 임하댐에서 용수를 추가 공급하는 것이 더욱 효과적인 것으로 평가되었다. 댐 방류량 증감에 따라 수질영향을 가장 크게 받는 하천구간은 수질오염도가 가장 크게 나타나는 금호강합류점${\sim}$고령교구간인 것으로 분석되었다. 본 연구결과는 낙동강과 같이 수량이 부족한 하천은 오염부하량 삭감 대책과 함께 갈수기 유량조절이 매우 중요한 요소임을 보여주며, 주기적인 수질악화를 겪는 낙동강 중 하류 지역의 수질개선을 위한 상류 다목적댐군의 연계운영 계획 수립에 활용될 수 있을 것으로 사료된다.치모의 결과와 현장에서 관측한 유속장을 비교함으로써 본 연구에서 제시한 실제 탁수배제능력을 검증하였다.를 구축하였다는데 의의가 있다.로와 접하는 건물의 경우 모서리부 광고 효과가 지배적이며 대부분 곡선돌출형이 사용되고 있었다. 그러므로 모서리 저층부를 필로티로 계획하여 보행흐름을 원활하게 하고 대신 입면을 투명하게 하여 간접광고(내부전시) 효과를 유도하는 것이 좋다. 특히 원형모서리는 건물 특화 성격이 강하므로 불가피할 경우 소형 액센트 광고 위치를 미리 벽면으로 할애하는 것이 경관 및 입면계획에 유리한 것으로 분석되었다. 불확실도 해석모형 등의 새로운 기능을 추가하여 제시하였다. 모든 입출력자료는 프로젝트 단위별로 운영되어 data의 관리가 손쉽도록 하였으며 결과를 DB에 저장하여 다른 모형에서도 적용할 수 있도록 하였다. 그리고 HyGIS-HMS 및 HyGIS-RAS 모형에서 강우-유출-하도 수리해석-범람해석 등이 일괄되게 하나의 시스템 내에서 구현될 수 있도록 하였다. 따라서 HyGIS와 통합된 수리, 수문모형은 국내 하천 및 유역에 적합한 시스템으로서 향후 HydroInformatics 구현을 염두에 둔 특화된 국내 수자원 분야 소프트웨어의 개발에 기본 토대를 제공할 것으로 판단된다.았다. 또한 저자들의 임상병리학적 연구결과가 다른 문헌에서 보고된 소아 신증후군의 연구결과와 큰 차이를 보이지 않음을 알 수 있었다. 자극에 차이가 있지 않나 추측되며 이에 관한 추후 연구가 요망된다. 총대장통과시간의 단축은 결장 분절 모두에서 줄어들어 나타났으나 좌측결장 통과시간의 감소 및 이로 인한 이 부위의 통과시간 비율의 저하가 가장 주요하였다. 이러한 결과는 차가운 생수 섭취가 주로 결장 근위부를 자극하는 효과를 발휘하는 것이

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A Comparative Study on the Pharmaceutical Properties of Rectal Suppository containing Omeprazole Complexes (오메프라졸복합체 함유 직장좌제의 특성비교)

  • Hwang, Sung-Joo;Park, Sung-Bae;Rhee, Gye-Ju
    • Journal of Pharmaceutical Investigation
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    • v.25 no.3
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    • pp.227-237
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    • 1995
  • Omeprazole(OMP) complexes such as inclusion complexes of OMP with $hydroxypropyl-{\beta}-cyclodextrin$(HPCD) and ${\beta}-cyclodextrin({\beta}-CD)$, OMP-cholestyramine(CHL) and OMP-ethylenediamine(OMP-ED) were prepared, respectively. The partition coefficients in Witepsol H-15 /pH 7.4 phosphate buffer solution of OMP complexes$(OMP-HPCD;\;3.69{\pm}0.26,\;OMP-{\beta}-CD;\;4.08{\pm}0.21,\;OMP-CHL;\;4.36{\pm}0.25\;and\;omeprazole\;sodium(OMP-Na);\;3.64{\pm}0.37)$ were higher than that of OMP $(2.66{\pm}0.47)$. OMP was not completely dissolved until even 3 hrs, but all the OMP complexes studied were released about 100% in 20 min. The rectal suppositories containing OMP or each above OMP complex were prepared using Witepsol H-15 base, and their dissolution and stability were examined, and pharmacokinetic study were investigated after their rectal administrations to the rabbits. While the suppository containing OMP was released only less than 60% in 150 min, $OMP-{\beta}-CD$, OMP-CHL, OMP-Na and OMP-ED suppositories were all released about 65% in 20 min. Especially, OMP-HPCD suppository released OMP about 70% in 10 min. All the additives such as sodium laurylsulfate, eglumine, arginine and PVP increased drug release from OMP-HPCD suppository to some extent. The decomposition rate constants of OMP in the suppositories were $9.117{\times}10^{-3}\;day^{-l}$ for OMP suppository, $2.121{\times}10^{-2}$ for OMP-HPCD, $1.607{\times}10^{-2}$ for $OMP-{\beta}-CD$, $9.26{\times}10^{-3}$ for OMP-Na, $6.769{\times}10^{-3}$ for OMP-CHL and $5.58{\times}10^{-3}\;day^{-l}$ for OMP-ED suppository, respectively. Additives such as arginine, eglumine and ED had some stabilizing effect for OMP-HPCD, OMP-CHL and OMP-Na suppositories, respectively. After 6 month-storage at $30^{\circ}C$, 75% RH, OMP-CHL suppository was most stable. The values of Tmax for OMP-HPCD and OMP-Na suppositories were $11.7{\pm}2.36\;and\;11.4{\pm}2.56\;min$, respectively. The values of Cmax for OMP-HPCD and OMP-CHL suppository were $2.31\;{\mu}g/ml\;(p<0.01)\;and\;1.89\;{\mu}g/ml\;p<0.01)$, respectively. The values of AUC for OMP and $OMP-{\beta}-CD$ suppository were $61.9{\pm}25.79\;and\;68.6{\pm}29.48\;{\mu}g\;{\cdot}\;min/ml$, and the corresponding values for OMP-HPCD and OMP-CHL were $106.1{\pm}43.16\;(p<0.05)\;and\;127.3{\pm}42.52\;{\mu}g\;{\cdot}\;min/ml(p<0.01)$, respectively. The above results indicate the OMP-HPCD and OMP-CHL suppositories have the excellent bioavailabilties in vivo study.

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Effects of Castration and Injection Time of rbST on Dry Matter and Nutrient Intake in Holstein Bulls (거세와 rbST 투여 시기가 Holstein 수소의 건물 및 영양분 섭취량에 미치는 영향)

  • 권응기;김현섭;윤상기;강우성;김병완;김종복;홍병주
    • Journal of The Korean Society of Grassland and Forage Science
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    • v.18 no.1
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    • pp.61-68
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    • 1998
  • This research was canied out to investigate the effect of castration and injection time of sustained release recombinant bovine somatotropin(SR-rbST) on dry matter intake(DM1) and nutrient intake of surgically castrated 32 Holstein young bulls by growth stage. The main results were as follows: 1. DM intakes were not different between in bull and steer groups, but those in rbSTl and rbST2 were 7.88 and 7.65kg respectively, which were lower 6-9% compared to bull and steer groups. 2. Actual DM intake to DM requirement of Beef cattle(NRC) was 88.5~97.7%, while net energy intake was sufficient for NE requirement in all groups during all growth stage except rbST group during fmishing stage. 3. Overall mean concentrate intake to body weight in steer group was the highest as 1.94%, and then those in rbST groups were 1.87~1.89% which were higher 0.07~0.09% unit than in bull group. 4. Feed conversion ratios(DM) in bull, rbSTl and rbST2 groups were 8.29, 8.18 and 7.60kg respectively, which were improved 12.4, 13.9 and 22.6%, respectively, compared to steer group.

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Effects of Slow Release Recombinant Porcine Somatotropin (rpST) Administration on Growth Performance and pST and IGF-1 of Blood in Finishing Pigs (지속형 유전자 재조합 pST(Recombinant Porcine Somatotropin; rpST) 투여가 비육돈의 성장, 혈중 pST 및 IGF-1 농도에 미치는 영향)

  • 김영화;문홍길;박준철;정현정;김인철;이상진;장병선;정정수;정일병
    • Journal of Animal Science and Technology
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    • v.48 no.5
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    • pp.663-670
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    • 2006
  • The present study was performed to investigate the effect of plant type recombinant porcine somatotropin (pST) adminstration on growth performance and blood profile of finishing pigs. Forty-eight Landrace barrows weighing 78 kg were employed for six week growth trial. Twelve barrows were allocated into various rpST types ; the control (CONT), the 4:1 type rpST (TRT 1), the 1:1 type rpST (TRT 2); and the 4:1 type rpST group(TRT 3) respectively. CONT group were not planted rpST. TRT 1 group was treated with rpST once a week for 6 weeks. Each dose contained the rpST equivalent to 100mg from initial to two weeks and 125mg from three weeks to finial week. TRT 2 and TRT 3 groups were planted rpST four times contained the rpST equivalent to 100mg during trial period from initial to two weeks, and 125 mg from three weeks, to four weeks, respectively. All pigs were fed a commercial feed containing 0.9% lysine ad lib. Daily gain increased by 19.4% in TRT 1(p<0.05) compared to the CONT. rpST improved feed/gain by 13.4~28.9% in all treatment groups(p<0.05). Back fat thickness of the all rpST treated groups were 23.3~29.2% thinner than that of the CONT. These results indicated that the rpST stimulated growth performance in finishing pigs and plant type rpST could be used as a growth stimulant for finishing pigs.

Water Quality Modelling of Flood Control Dam by HSPF and EFDC (HSPF-EFDC 모델을 연계한 홍수조절댐 수질 변화 예측)

  • Lee, Young-Gi;Hwang, Sang-Chul;Hwang, Hyun-Dong;Na, Jin-Young;Yu, Na-Young;Lee, Han-Jin
    • Journal of Environmental Impact Assessment
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    • v.27 no.3
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    • pp.251-266
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    • 2018
  • This study predicted the effect of operation pattern of flood control dam on water quality. Flood control dam temporarily impound floodwaters and then release them under control to the river below the dam preventing the river ecosystem from the extreme flood. The Hydrological Simulation Program Fortran (HSPF) and the Environmental Fluid Dynamics Code (EFDC) were adapted to predict the water quality before and after the dam construction in the proposed reservoir. The non-point pollutant delivery load from the river basin was estimated using the HSPF, and the EFDC was used to predict the water quality using the provided watershed boundary conditions from the HSPF. As a result of water quality simulation, it is predicted that the water quality will be improved due to the decrease of pollution source due to submergence after dam construction and temporary storage during rainfall. There would be no major water quality issues such as the eutrophication in the reservoir since the dam would impound the floodwater for a short time (2~3 days). In the environmental impact assessment stage of a planned dam, there may be some limitations to the exact simulation because the model can not be sufficiently calibrated. However, if the reliability of the model is improved through the acquisition of actual data in the future, it will be possible to examine the influence of the water environment according to various operating conditions in the environmental impact assessment of the new flood control dam.

Effect of Salt Fermentation on the Physicochemical Properties and Antioxidant Activities of Sea Urchin Roe from Anthocidaris crassispina and Pseudocentrotus depressus (염장처리가 성게 알의 이화학 품질 특성과 산화방지 활성에 미치는 영향)

  • Choi, Bogyoung;Surh, Jeonghee
    • Korean Journal of Food Science and Technology
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    • v.47 no.4
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    • pp.460-467
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    • 2015
  • Sea urchin roe obtained from Anthocidaris crassispina and Pseudocentrotus depressus was briefly salt-fermented (5%), followed by ethanol treatment (1%) and the physicochemical properties as well as antioxidant activity were investigated. Compared to raw sea urchin roes, the salted one showed a significantly low amount of water (p<0.001) high salinity (p<0.05), ash content (p<0.001) and Na content (p<0.001). With salt-fermentation, the redness (p<0.05) and yellowness (p<0.001) of roe decreased noticeably, indicating the decomposition of endogenous carotenoids. Accordingly, the salted roe showed a lower DPPH radical scavenging activity than its unsalted counterpart. Additionally, it showed a significantly lower metal-chelating activity (p<0.05) and metal chelator content (e.g. ortho-phenolics) displayed by a negligible difference in titratable acidity. The salted roe showed significantly increased hardness (p<0.05) and total reducing capacity (p<0.001), which were attributed to the protein coagulation and the release of antioxidants bound to macromolecules after the ethanol treatment, respectively.

Production and Embryo Transfer of In Vivo Embryos by Repeated Superovulation Treatment of Hanwoo Cattle (한우의 반복 과배란 처리에 의한 체내 수정란의 생산과 이식)

  • Shin, Sang-Min;Kim, Yong-Jun;Lee, Hae-Lee;Shin, Dong-Su;Kim, Yong-Su;Kim, Sue-Hee;Lee, Young-Jun
    • Journal of Embryo Transfer
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    • v.24 no.1
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    • pp.47-55
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    • 2009
  • This study was performed to investigate the possibility of repeated superovulation treatment at interval from 27 days to 41 days in Hanwoo cattle and to compare with superovulation effect between doses of FSH 200 mg and FSH 400 mg. Different doses of FSH (200 mg or 400 mg) were injected at Day 8 after controlled internal drug release (CIDR) treatment for superovulation of Hanwoo donors following CIDR treatment (Day 8 after the estrus). Superovulation was repeated four times for one donor and number of corpus luteum (CL), number of embryos, number of transferable embryos and pregnancy rate after embryo transfer (ET) were investigated. 5 cows were used for each FSH treatment (10 cows in total). Average number of CL were $10.16{\pm}3.85$ and $11.56{\pm}2.35$ for the donors treated with FSH 200mg and FSH 400mg, respectively. Average number of embryos collected were $8.85{\pm}4.05$ and $8.30{\pm}1.73$ for the donors treated with FSH 200 mg and FSH 400 mg, respectively. Average number of transferable embryos were $5.48{\pm}2.45$ and $4.58{\pm}2.23$ for the donors treated with FSH 200 mg and FSH 400 mg, respectively. The pregnancy rate following ET with embryos collected from 200 mg FSH treated donors and 400 mg FSH treated donors were 61.9% and 53.8% respectively. The numbers of embryos tended to be decreased as the numbers of repeat of superovulation were elapsed. These results indicated that superovulation treatment by about a month to Hanwoo donors is usable and 200 mg of FSH is preferable for simple FSH treatment following CIDR treatment.

Influence of Interferon-${\tau}$ on the Production of Prostaglandins, Cyclooxygenase-2 Expression In Vitro and Release of Progesterone in Bovine Endometrial Cells

  • Lee, Ji-Eun;Lee, Yong-Seung;Yoo, Han-Jun;Lee, Kyoung-Jin;Park, Joung-Jun;Cheong, Hee-Tae;Yang, Boo-Keun;Park, Choon-Keun
    • Journal of Embryo Transfer
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    • v.27 no.4
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    • pp.245-252
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    • 2012
  • The purpose of the present study was to investigate the effect of IFN-${\tau}$ on prostaglandin synthesis, cyclooxygenase-2 (COX-2) gene expression in vitro and concentration of progesterone (P4) in endometrial cells. Epithelial and stromal cells cultured in vitro were isolated from bovine endometrium and stimulated with increasing doses of IFN-${\tau}$ (0, 0.02, 0.2 and 2 ug/ml). Human chorionic gonadotropin (hCG, 1.5 IU/ml) was used as a positive control. Prostaglandin $E_2$ and $F_{2{\alpha}}$ levels in the culture media were analyzed by enzyme immunoassays and total RNA was extracted from the cells for RT-PCR. P4 concentrations of blood samples were assayed by chemiluminescent immuno assays system. In epithelial cells, COX-2 gene expression was increased in the presence of IFN-${\tau}$ (p<0.05), but it was not significantly different in all groups of stromal cells except for 2 ug/ml IFN-${\tau}$ group (p<0.05). Although IFN-${\tau}$ did not affect $PGE_2$ and $PGF_{2{\alpha}}$ production in epithelial cells, it decreased $PGE_2$ and $PGF_{2{\alpha}}$ production significantly in stromal cells (p<0.05). In vivo experiment, blood concentration of P4 was significantly increased after addition of IFN-${\tau}$ (1 ug/ml). The results indicate that PG production was mediated by COX-2 expression in stromal cells but it was not affected in epithelial cells and this suggest that treatment of IFN-${\tau}$ could improve the implantation environment of uterine by maintenance of high P4 concentration.

Anti-oxidative and Anti-cancer Activities of Treculia africana Extract in Human Colon Adenocarcinoma HT29 Cells (대장암세포주 HT29에서의 Treculia africana 추출물의 항산화 및 항암 활성 분석)

  • Oh, You Na;Jin, Soojung;Park, Hyun-jin;Kim, Byung Woo;Kwon, Hyun Ju
    • Journal of Life Science
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    • v.25 no.5
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    • pp.515-522
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    • 2015
  • Treculia africana Decne, a breadfruit species, is native to many parts of West and Tropical Africa. The breadfruit belongs to the family Moraceae and is one of the four members of the genera Treculia. The crude extract of T. africana has been used in folk medicine as an anti-inflammatory agent for various ailments, such as whooping cough. In this study, we evaluated the anti-oxidative and anti-cancer activities of the methanol extract of T. africana Decne (META) and the molecular mechanisms of its anti-cancer effects in human colon carcinoma HT29 cells. The META exhibited anti-oxidative activity through a DPPH radical scavenging capacity and inhibited cell growth in a dose-dependent manner in HT29 cells. META treatment induced apoptosis of HT29 cells, showing an increase in the percentage of both SubG1 cells and Annexin V-positive cells and the formation of apoptotic bodies in a dose-dependent manner. META-mediated apoptosis was associated with the up-regulation of the death receptor FAS and Bax and a decrease in the Bcl-2 expression. META-treated HT29 cells also showed the release of cytochrome c from the mitochondria into the cytosol, activation of caspase-3, caspase-8, and caspase-9, and proteolytic cleavage of poly ADP-ribose polymerase (PARP). These findings suggest META may exert an anti-cancer effect in HT29 cells by inducing apoptosis through both intrinsic and extrinsic pathways.