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Assessment of Prolonged Administration of SynriamTM on Haematological Parameters and Lipid Profiles of Rats 长时间给药对大鼠血液学参数及血脂的影响
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.202306012
David Chukwuma Nwikwe, E. Balogun
A potential antimalarial prospect should have high efficacy with low toxicity. SynriamTM antimalarial drug has been proven to be safe and effective for the treatment of malaria in human with dearth information on rats. This study investigated its potential toxicity from prolonged administration on lipid profiles and haematological indices in rats. Thirty-five Wistar rats were randomized into five groups (A – E) of seven rats each. Animals in group A (control) received 0.5 mL distilled water, while groups B, C, D, and E respectively received 4.0, 8.0, 16.0 and 32.0 mg/kg bwt of the drug once daily for 28 days. The concentrations of serum TC, LDL and atherogenic index showed significant (p<0.05) decrease, while serum TRIG, HDL, and VLDL concentrations had no effect (p>0.05). The drug also had no effect (p>0.05) on the levels of the red blood cell count, PCV, Hb, MCV, MCH, and MCHC. Similarly, it had no effect (p>0.05) on the levels of the WBC, lymphocytes and neutrocytes, while the platelet counts had slight (p<0.05) decrease. Hence, SynriamTM is relatively safe at doses of 4.0-32.0 mg/kg bwt in rats when taken once daily with minimal effects on the lipid profiles and haematological indices.
一个潜在的抗疟前景应该是高效低毒。SynriamTM抗疟药已被证明是安全有效的治疗人类疟疾的药物,但缺乏大鼠的信息。本研究考察了其长期给药对大鼠血脂和血液学指标的潜在毒性。35只Wistar大鼠随机分为5组(A ~ E),每组7只。A组(对照组)给药0.5 mL蒸馏水,B、C、D、E组分别给药4.0、8.0、16.0、32.0 mg/kg bwt,每日1次,连用28 D。血清TC、LDL、动脉粥样硬化指数均有显著性差异(p0.05)。该药对红细胞计数、PCV、Hb、MCV、MCH、MCHC水平无显著影响(p>0.05)。同样,对白细胞、淋巴细胞和中性细胞水平无影响(p>0.05),血小板计数有轻微降低(p<0.05)。因此,每天服用一次的大鼠剂量为4.0-32.0 mg/kg体重时,SynriamTM是相对安全的,对血脂和血液学指标的影响最小。
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引用次数: 0
Effects of Senna alata Aqueous Extract on the Hematological and Biochemical Alterations in Rats Exposed to N-Nitroso-N-Ethyl Urea 番泻叶水提物对n -亚硝基- n -乙基尿素大鼠血液学和生化变化的影响
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230606
Olufunke T. Olugbenga, Joy E. Okpuzo
The effect of carcinogen exposure has been established to alter biochemical and hematological profiles in humans. Secondary metabolites from plant sources like flavonoids, alkaloids, saponins, and others have been found to be potent anticancer agents and also investigated to protect against the effect of environmental carcinogens. Female albino rats were rats exposed to freshly prepared 3 fractionated doses of 50 mg/kg N-Nitroso-N-ethyl urea (carcinogen) dissolved in 1/15 M Phosphate buffer, given intraperitoneally and treated with varying concentrations of Senna alata plant aqueous extracts. At the end of the test period, hematological and biochemical parameters were determined in blood and serum samples. Compared to the control group, the carcinogen exposed rats treated group showed significances in several hematological parameters, including decreases in White blood cell (WBC), Red blood cell (RBC), and Platelet (PLT) counts. Furthermore, in comparison to the control group, the carcinogen exposed rats showed significantly increased blood glucose, serum total cholesterol, Low density lipoprotein (LDL-cholesterol), triacylglycerols levels and High density lipoprotein (HDL-cholesterol) level. The hematological and biochemical parameters in the carcinogen exposed rats treated group were approximately similar to control group. The S. alata extract significantly (P<0.05) restored the hematological and biochemical parameters in N-Nitroso-N-ethyl urea carcinogen exposed rats
接触致癌物会改变人体的生化和血液学特征。来自植物的次生代谢物,如类黄酮、生物碱、皂苷等,已被发现是有效的抗癌剂,也被研究用于保护人体免受环境致癌物的影响。雌性白化大鼠暴露于新鲜配制的3次剂量的50 mg/kg n -亚硝基- n -乙基尿素(致癌物)溶解在1/15 M磷酸盐缓冲液中,腹腔注射不同浓度的番泻草植物水提取物。在试验期结束时,测定血液和血清样品的血液学和生化参数。与对照组相比,暴露于致癌物的治疗组大鼠在几个血液学参数上表现出显著性,包括白细胞(WBC)、红细胞(RBC)和血小板(PLT)计数的减少。此外,与对照组相比,接触致癌物的大鼠血糖、血清总胆固醇、低密度脂蛋白(ldl -胆固醇)、甘油三酯和高密度脂蛋白(hdl -胆固醇)水平显著升高。致癌物接触组大鼠血液学、生化指标与对照组基本相似。紫苏提取物对n -亚硝基- n -乙基脲致癌物暴露大鼠血液学和生化指标有显著恢复作用(P<0.05)
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引用次数: 0
Phycoremediation of Laundry Wastewater Using Chlorella vulgaris (Beijerinck) 普通小球藻(Beijerinck)对洗衣废水的藻修复
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230604
M. A. Akhere
A study of the effect laundry wastewater on the microalga Chlorella vulgaris was carried out. The study was carried out using different treatments 0% (control), 5%, 10%, 20%, 30%, 40%, 50% of laundry wastewater. The microalgal growth responses were determined optically using absorbance on spectrophotometer at 750nm. Samples were analyzed for physicochemical parameters such as pH, temperature, total dissolved solids, conductivity, biochemical oxygen demand and chemical oxygen demand using standard methods. Descriptive statistics, inferential (One-way analysis of variance (ANOVA) and post-hoc test Duncan multiple range (DMR) were done using Microsoft excel 2010 and statistical package for social science SPSS 22. The results showed that different concentrations of laundry wastewater stimulated the growth of Chlorella vulgaris with 50% treatment having the highest yield (3.2), followed by 40% treatment (2.7) and the control (0%) had the least yield of 0.6. There was a significant increase in pH and temperature while there was a decrease in total dissolved solids, biochemical oxygen demand, chemical oxygen demand and conductivity. The level of reduction in COD was from 1340mg/L to 364mg/L, which indicated that Chlorella vulgaris has the potential to bioremediate laundry wastewater.
研究了洗涤废水对普通小球藻的影响。研究采用0%(对照)、5%、10%、20%、30%、40%、50%的洗衣废水处理。在750nm分光光度计上测定微藻的生长响应。采用标准方法分析样品的理化参数,如pH、温度、总溶解固形物、电导率、生化需氧量和化学需氧量。使用Microsoft excel 2010和社会科学统计软件包SPSS 22进行描述性统计、推断性(单因素方差分析(ANOVA))和事后检验邓肯多元极差(DMR)。结果表明:不同浓度的洗衣废水对普通小球藻的生长均有促进作用,其中50%处理产量最高(3.2),40%处理次之(2.7),0%对照产量最低(0.6)。pH和温度均显著升高,总溶解固形物、生化需氧量、化学需氧量和电导率均显著降低。COD从1340mg/L降至364mg/L,表明普通小球藻具有生物修复洗衣废水的潜力。
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引用次数: 0
Effect of Acute Administration of Ethanol Extract of Cannabis sativa Leaf on Oxidative Stress Biomarkers in Male and Female Wistar Rats 急性给予大麻叶乙醇提取物对雄性和雌性Wistar大鼠氧化应激生物标志物的影响
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230607
A. Oluwasola, S.S. Muzzammill, O. Ayoola, A. Odetayo, M. E. Balogun, A. Comfort, N.H Aishat, O. Deborah, O. Adekunle, V.J. Nkemdili, S. Zainab, E. Mariam
Oxidative stress is a phenomenon caused by an imbalance between production and accumulation of oxygen reactive species (ROS) in the cells and tissues and the ability of a biological system to detoxify these reactive products. This study investigated the acute effect of different doses of ethanolic extract annabis sativa (EECS) on oxidative stress biomarkers in male (M) and female (F) Wister rats. Twenty male rats (170 g ± 1.24) and twenty female rats (150 g ± 1.05) were separately assigned into four groups of five animals each for male and female, such that the rats in groups IM and IF, IIM and IIF, IIIM and IIIF and IVM and IVF received orally 1 mL of distilled water, 2 mg/kg body weight (BW) of EECS, 4 mg/kg BW of EECS and 6 mg/kg BW of EECS respectively for twenty one (21) days. Catalase, superoxide dismutase (SOD), Glutathione peroxidase (GPx), Glutathione reductase (GSH), malondialdehyde (MDA), total antioxidant capacity (TAC) and lactate dehydrogenase (LDH) were determined using standard methods. Administration of different doses (2 mg/kg BW, 4 mg/kg BW and 6 mg/kg BW) of EECS significantly (p<0.05) decreased catalase, SOD, GPx, GSH and TAC levels respectively when compared with the control. However, Cannabis sativa (CS) increased MDA and LDH levels significantly (p<0.05) when compared with the control. It was deduced that these alterations in oxidative stress biomarkers were dependent on the doses of CS consumed. Thus, the more the concentration of CS consumed, the more it may affect oxidative stress biomarkers negatively. In addition, all these effects of CS on oxidative stress biomarkers were more in male than in female.
氧化应激是由细胞和组织中氧反应物质(ROS)的产生和积累与生物系统解毒这些反应产物的能力之间的不平衡引起的一种现象。本研究研究了不同剂量大麻醇提取物(EECS)对雄性(M)和雌性(F) Wister大鼠氧化应激生物标志物的急性影响。将20只雄性大鼠(170 g±1.24)和20只雌性大鼠(150 g±1.05)分为4组,雌雄各5只,IM和IF组、IIM和IIF组、IIIM和IIIF组和IVM和IVF组大鼠分别口服蒸馏水1 mL、EECS 2 mg/kg体重(BW)、EECS 4 mg/kg体重(BW)、EECS 6 mg/kg体重(BW) 21 d。采用标准方法测定过氧化氢酶、超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GPx)、谷胱甘肽还原酶(GSH)、丙二醛(MDA)、总抗氧化能力(TAC)和乳酸脱氢酶(LDH)。不同剂量EECS (2 mg/kg BW、4 mg/kg BW和6 mg/kg BW)与对照组相比,过氧化氢酶、SOD、GPx、GSH和TAC水平均显著降低(p<0.05)。而与对照组相比,大麻(CS)显著提高了MDA和LDH水平(p<0.05)。由此推断,氧化应激生物标志物的这些改变依赖于摄入CS的剂量。因此,CS消耗的浓度越大,对氧化应激生物标志物的负面影响越大。此外,CS对氧化应激生物标志物的影响在男性中大于女性。
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引用次数: 0
Antimalarial Activity of Extracts and Partially Purified Fractions of Alstonia boonei De Wild 野白藤提取物及部分纯化组分的抗疟活性研究
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.202306020
P. Uadia, K. Orumwensodia
Alstonia boonei De wild is famed for several bioactive properties; this study measures its in vivo antimalarial potentials as well as phytochemical, nutritional and antioxidant properties. Variants of its stem bark extract were screened for phytochemical, nutritional and antioxidant properties using established procedures. In vivo antimalarial properties of extracts and fractions were determined against Plasmodium berghei NK65 infection in mice using chemo-suppressive, prophylactic, curative and mean survival time (MST) bioassays. Alkaloids, saponins, cardiac glycosides, tannins, flavonoids and phenolics were present in almost all extracts. The plant contained nitrogen free extract (NFE), crude fat, crude protein, moisture, crude ash and crude fibre in reasonable amounts. Extracts demonstrated antioxidant activity against DPPH and ferrous ion radicals. The aqueous and ethanol extracts were more active, decreased parasitaemia and increased MST relative to infected untreated control in the chemo-suppressive and prophylactic bioassays. Solvent-solvent partitioning of the hydro-ethanol extract yielded petroleum ether, dichloromethane-DCM, basified-DCM (BDCM), acidified-DCM (ADCM) and aqueous fractions. BDCM had the highest suppressive activity (70.91% suppression; MST: 16.50 ± 1.19), while the crude extract had the highest prophylactic (64.51% suppression; MST: 16.00 ± 1.22) and curative activities (69.80% suppression; MST: 16.80 ± 0.58). Alstonia boonei De wild possesses antimalarial properties likely associated with its phyto-nutritional composition.
野青藤以几种生物活性特性而闻名;本研究测定了其体内抗疟潜能以及植物化学、营养和抗氧化特性。其茎皮提取物的变体筛选的植物化学,营养和抗氧化性能使用既定的程序。采用化学抑制、预防、治疗和平均生存时间(MST)生物测定法测定提取物和馏分对小鼠伯氏疟原虫NK65感染的体内抗疟特性。几乎所有提取物中都含有生物碱、皂苷、心苷、单宁、黄酮类和酚类物质。该植物的无氮浸出物、粗脂肪、粗蛋白质、水分、粗灰分和粗纤维含量合理。提取物对DPPH和亚铁离子自由基具有抗氧化活性。在化学抑制和预防性生物测定中,与未感染的对照相比,水提物和乙醇提物更有活性,降低了寄生虫血症,增加了MST。对水乙醇提取物进行溶剂-溶剂分配,得到石油醚、二氯甲烷- dcm、碱化- dcm、酸化- dcm和水馏分。BDCM的抑菌活性最高,抑制率为70.91%;MST: 16.50±1.19),而粗提物的预防效果最高(抑制64.51%;MST: 16.00±1.22)和治疗活性(抑制69.80%;Mst: 16.80±0.58)。野青藤具有抗疟特性,可能与其植物营养成分有关。
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引用次数: 0
Evaluation of the Liver Function and Haematological Parameters of Wistar Rats Fed with Casein Protein 饲喂酪蛋白对Wistar大鼠肝功能及血液学指标的影响
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.202306011
R. O. Aikpitanyi-iduitua, B. Eiya
Casein is the major protein found in bovine milk. Universally used in human nutrition for all ages and in the dairy industry, milk is regarded as whole food which provides high quality protein and indispensable micronutrients such as vitamins and minerals. The evaluation of the liver function test and haematological parameters of rats fed with casein protein was carried out. Graded levels of casein protein were incorporated into the diets of experimental rats at 20%, 30% and 50% concentrations. At the end of twenty-eight days, blood samples were collected and analyzed for liver function and haematological parameters. Statistically significant increases were observed in lactate dehydrogenase, gamma glutamyl transferase, alanine transaminase, aspartate transaminase and alkaline phosphatase activity levels when compared with the control. Also the granulocytes and platelets counts were significantly reduced. Consistent consumption of high concentrations of casein proteins may elevate liver enzyme activities and attenuate some haematological parameters.
酪蛋白是牛奶中的主要蛋白质。牛奶被广泛用于所有年龄段的人类营养和乳制品行业,被认为是提供高质量蛋白质和维生素和矿物质等不可或缺的微量营养素的天然食品。对饲喂酪蛋白的大鼠进行肝功能试验和血液学指标评价。按20%、30%和50%的浓度将酪蛋白分级添加到实验大鼠的饮食中。28 d结束时,采集血样,分析肝功能和血液学参数。与对照组相比,乳酸脱氢酶、谷氨酰转移酶、丙氨酸转氨酶、天冬氨酸转氨酶和碱性磷酸酶活性水平均有统计学意义的升高。粒细胞和血小板计数也明显减少。持续摄入高浓度酪蛋白可提高肝酶活性,减弱某些血液学参数。
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引用次数: 0
Vernonia amygdalina Extract Reverts Hematological and Biochemical Alterations in Rats Exposed to N-Nitroso-N-Ethyl Urea 苦杏仁提取物恢复暴露于n -亚硝基- n -乙基尿素的大鼠血液学和生化改变
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230605
Olufunke T. Olugbenga, J. Okpuzor
Environmental carcinogens or exogenous carcinogens includes chemical, biological, and physical agents that have the potential to increase cancer risk because of prolonged high prevalence of exposure. Exposure can be through the respiratory, digestive, cutaneous or other possible contamination routes. N-Nitroso-N-ethyl urea (NEU), an ethylating agent has been described as a very potent transplacental teratogen and carcinogen in rodents. Plants have been investigated to protect against the effect of environmental carcinogens due to their arrays of phytochemicals. 35Female albino rats of average ages 10weeks were rats exposed to freshly prepared 3 fractionated doses of 50 mg/kg N-Nitroso-N-ethyl urea dissolved in 1/15 M phosphate buffer, given intraperitoneally and treated with varying concentrations of Vernonia amygdalina leaf aqueous extracts. At the end of the test period, hematological and biochemical parameters were determined in blood samples. Compared to the control group, the NEU exposed rats treated group showed significances in several hematological parameters, including decreases in white blood cell (WBC), red blood cell (RBC), and platelet (PLT) counts. Furthermore, in comparison to the control group, the NEU exposed rats showed significantly (p<0.05) increased blood glucose, serum total cholesterol, low density lipoprotein (LDL-cholesterol), triacylglycerols levels and igh density lipoprotein (HDL-cholesterol) level. The hematological and biochemical parameters in the NEU exposed rats treated group were similar to control group. V. amygdalina extract significantly (P<0.05) restored the hematological and biochemical parameters in N-Nitroso-N-ethyl urea exposed rats
环境致癌物或外源性致癌物包括化学的、生物的和物理的,由于长期高流行的接触而有可能增加癌症风险的物质。暴露可通过呼吸、消化、皮肤或其他可能的污染途径。n -亚硝基- n -乙基尿素(NEU)是一种乙基化剂,被认为是一种非常有效的啮齿动物胎盘致畸物和致癌物。由于植物中含有大量的植物化学物质,人们已经研究了植物对环境致癌物的保护作用。35平均年龄10周龄的雌性白化大鼠暴露于新鲜配制的3次50 mg/kg n -亚硝基- n -乙基尿素溶解于1/15 M磷酸盐缓冲液中,腹腔注射不同浓度的苦杏仁叶水提取物。在试验期结束时,测定血液样本的血液学和生化参数。与对照组相比,NEU暴露组大鼠的几个血液学参数都有显著性变化,包括白细胞(WBC)、红细胞(RBC)和血小板(PLT)计数的减少。此外,与对照组相比,NEU暴露大鼠血糖、血清总胆固醇、低密度脂蛋白(ldl -胆固醇)、甘油三酯和高密度脂蛋白(hdl -胆固醇)水平显著升高(p<0.05)。治疗组大鼠血液学、生化指标与对照组基本相同。苦杏仁提取物显著(P<0.05)恢复了n -亚硝基- n -乙基尿素暴露大鼠的血液学和生化指标
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引用次数: 0
Chemical Composition and in vitro Antioxidant Properties of Hexane and Methanol Extract of Sesamum indicum Seeds Obtained from Kogi State, Nigeria 尼日利亚科吉州芝麻籽己烷和甲醇提取物的化学成分及体外抗氧化性能
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230608
J. C. Ukpabi-Ugo, Enyinna Wisdom Chukwuma, C. Anosike
The chemical composition and in vitro properties of hexane and methanol extract of Sesamum indicum seeds (SIS) obtained from Kogi State, Nigeria were evaluated. The proximate analysis of the ground seed showed the presence of moisture content (8.56 ± 0.02%), dry matter (91.44 ± 0.02%), ash content (5.70 ± 0.01%), crude protein (19.37 ± 0.08%), crude fiber (6.34 ± 0.03%), fat (52.77 ± 0.02%) and carbohydrates (7.26 ± 0.14%). Phytochemical analysis of both extracts showed the presence of oxalate, hydro cyanide, alkaloids, tannins, total flavonoids, phenol, steroids and terpenes. Flavonoids and phenol contents were higher in both extracts. The flavonoid and phenol concentrations of hexane and methanol extracts were 24.79 ± 0.01 and 25.27 ± 0.02 mg/100 g, 24.32 ± 0.02 mg/100 g and 18.66 ± 0.04 mg/100g, respectively. Hydrogen cyanide was found in lowest concentration in both extracts. Vitamins analysis showed that vitamin E had the highest composite for hexane and methanol extract. Vitamin E concentration was 3.44 ± 0.01 mg/100g and 2.95± 0.02mg/100g respectively while vitamin B6 (0.01 ± 0.00 mg/100g) and vitamin B1 (0.03 ± 0.00 mg/100g) were found in lowest concentration respectively. The mineral analysis showed that potassium (43.33 ± 0.04 and 27.46 ± 0.02 mg/100g) had the highest concentration for methanol and hexane extract, respectively. The results of the DPPH activity of methanol and hexane extract of S. indicum seeds indicated that the activity of the extract were all significantly (p<0.05) lower than the values for ascorbic acid (standard) across all concentrations. However, the DPPH activity of hexane extract indicated that there was no activity in the tested concentrations below100 µg/mL. The result of the FRAP of methanol and hexane extract of SIS showed that there was no activity at the concentrations of 100 µg/ml and 400 µg/ml respectively. However, the activity observed at concentrations above 100 µg/ml and 400 µg/ml were all significantly (p<0.05) lower than the same concentration in ascorbic acid. This result implies that hexane and methanol extract of S. indicum seeds possess nutritional and pharmacological value and can be a rich source of minerals, vitamins and antioxidative supplement.
对产自尼日利亚科吉州的芝麻种子(SIS)的己烷和甲醇提取物的化学成分和体外性质进行了评价。对磨碎的种子进行近似分析,发现其含水量(8.56±0.02%)、干物质(91.44±0.02%)、灰分(5.70±0.01%)、粗蛋白质(19.37±0.08%)、粗纤维(6.34±0.03%)、脂肪(52.77±0.02%)和碳水化合物(7.26±0.14%)。植物化学分析表明,两种提取物均含有草酸、氢氰化物、生物碱、单宁、总黄酮、酚、类固醇和萜烯。两种提取物的黄酮和酚含量均较高。己烷和甲醇提取物的类黄酮和酚含量分别为24.79±0.01和25.27±0.02 mg/100g、24.32±0.02 mg/100g和18.66±0.04 mg/100g。两种提取物中氰化氢的浓度最低。维生素分析表明,正己烷和甲醇提取物中维生素E的复合含量最高。维生素E的浓度分别为3.44±0.01 mg/100g和2.95±0.02mg/100g,最低浓度为维生素B6(0.01±0.00 mg/100g)和维生素B1(0.03±0.00 mg/100g)。矿物分析表明,甲醇和己烷提取物中钾(43.33±0.04 mg/100g)和钾(27.46±0.02 mg/100g)含量最高。甲醇提取物和正己烷提取物的DPPH活性均显著(p<0.05)低于抗坏血酸(标准)。而己烷提取物的DPPH活性表明,浓度低于100µg/mL时,其DPPH活性不明显。甲醇和SIS己烷提取物的FRAP结果显示,分别在浓度为100µg/ml和400µg/ml时没有活性。100µg/ml以上和400µg/ml以上的抗坏血酸活性均显著低于相同浓度的抗坏血酸(p<0.05)。结果表明,正己烷和甲醇提取物具有一定的营养和药理价值,是一种丰富的矿物质、维生素和抗氧化剂的补充来源。
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引用次数: 0
Discovery of Eriodictyol as Putative Exportin-1 Inhibitor for Non-small Cell Lung Cancer Therapy 戊二醇作为非小细胞肺癌推定出口蛋白-1抑制剂的发现
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.20230609
T. Adigun, F. A. Sulaiman, A. Na’Allah, M. Alabi, C. E. Odo, Eunice Toluwalope Adebamiji, I. A. Oluwadare, U. Ozojiofor, Adedayo Pius Omoniyi, Wisdom O. Joel, Kehinde Oyebola Aina, O. Alejolowo, S. Akiode, J. F. Adeegbe
Exportin-1, the ubiquitous nuclear protein transporter, is widely confirmed as an active chemotherapeutic target in non-small cell lung cancer conditions, while Juglans mandshurica is a well-studied anticancer plant in some lung cancer cell lines. We intend to find a novel exportin-1 inhibitor from Juglans mandshurica with better potential, tolerability and pharmaco-dynamo-kinetic properties than the current selective inhibitors of nuclear export in non-small cell lung cancer treatment. OSIRIS DataWarrior, along with Glide standard precision docking, and other Glide modules were employed for compound properties exploration, docking simulations, free energy calculations against exportin-1; density functional theory analysis of the compounds were carried out to estimate their electronic stability, while web-based SWISSADME was employed for ADMET and synthetic accessibility evaluations. This study reveals eriodictyol as having higher binding free energy (-40 kcal/mol) than that of standard (-39.56 kcal/mol) in exportin-1 active site, better synthetic accessibility score (3.15 versus 3.29), high GI absorption, non-blood brain barrier permeant, lacks Brenk and PAINS alert, obeying Lipinski’s, Ghose’s, Veber’s, Egan’s, and Muegge’s rule of drug-likeness and lead-likeness as well as non-cytotoxic to HepG2 cells. We therefore found eriodictyol as a lead-like, non-toxic exportin-1 inhibitor with good predictive stability and pharmacokinetic potential and thus provided data for further validation of eriodictyol as a candidate exportin-1 inhibitor in both preclinical and clinical studies involving lung cancer therapy.
export -1是一种普遍存在的核蛋白转运体,在非小细胞肺癌中被广泛证实是一种活跃的化疗靶点,而在一些肺癌细胞系中,山梨花是一种被充分研究的抗癌植物。我们打算从水杨树中寻找一种新的出口蛋白-1抑制剂,它在治疗非小细胞肺癌方面具有比现有的核出口选择性抑制剂更好的潜力、耐受性和药物动力学-动力学特性。OSIRIS DataWarrior与Glide标准精确对接和其他Glide模块一起用于化合物特性勘探、对接模拟、针对出口的自由能计算;采用密度泛函理论分析化合物的电子稳定性,采用基于web的SWISSADME进行ADMET和合成可达性评价。本研究表明,碘二醇在出口蛋白1活性位点的结合自由能(-40 kcal/mol)高于标准(-39.56 kcal/mol),合成可及性评分(3.15比3.29)较高,GI吸收高,无血脑屏障渗透,缺乏Brenk和PAINS警示,符合Lipinski、Ghose、Veber、Egan和Muegge的药物相似和铅相似规则,对HepG2细胞无细胞毒性。因此,我们发现eriodictyol是一种类似铅的无毒出口蛋白-1抑制剂,具有良好的预测稳定性和药代动力学潜力,从而为进一步验证eriodictyol作为肺癌治疗的临床前和临床研究中的候选出口蛋白-1抑制剂提供了数据。
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引用次数: 0
Phytochemical and Proximate Evaluation of Fresh and Spoilt Fruits of Tomatoes (Solanum lycopersicum L.) Sold in Five Major Markets in Benin City, Edo State, Nigeria 番茄鲜果和变质果的植物化学及近似评价在尼日利亚埃多州贝宁市的五大市场销售
Pub Date : 2023-06-30 DOI: 10.26538/africanscientist.24.2.202306015
A. O. Chime
Tomatoes contribute to healthy, well-balanced diet. They are rich in minerals, vitamins, essential amino acids, sugar and dietary fibres. It contains much vitamin B and C, iron and phosphorus. Tomato fruits are consumed fresh in salads or cooked in sauces, soup and meat or fish dishes. Phytochemical compounds are desirable compounds in our food because of their antioxidant properties. The study of phytochemical and proximate evaluation of fresh and spoilt tomatoes fruits obtained from five markets in Benin City, Edo State, Nigeria was carried out. This aim to investigate the phytochemical and proximate constituents of both fresh and spoilt tomatoes fruit. A total of 400 tomatoes were randomly purchased from the five markets in Benin City, Edo State, Nigeria. In each market, 40 fresh (firm and undamaged) and 40 spoilt (damaged and spoilt) tomatoes were purchased from 10 different sellers. Samples were separately packaged into different sterile containers, labelled, and transported to the laboratory immediately for phytochemical and proximate analysis. The phytochemical and proximate composition analyses were carried out using the official methods of analysis of analytical chemists laboratory procedures. The result shows a significant difference in value of phytochemical and proximate composition in both fresh and spoilt tomato fruits. The value of crude carbohydrate, crude protein, crude fat, saponin, flavonoids and alkaloids were higher in fresh tomato fruits than spoilt fruit while moisture, crude ash, crude fibre, tannins and polyphenols were higher in spoilt tomato fruits than in fresh fruits. This study has shown that spoilage reduces some important phytochemical and proximate constituents of tomato fruits
西红柿有助于健康、均衡的饮食。它们富含矿物质、维生素、必需氨基酸、糖和膳食纤维。它含有大量的维生素B和C、铁和磷。西红柿水果可以在沙拉中新鲜食用,也可以煮在酱汁、汤、肉或鱼中食用。植物化学化合物是我们食物中理想的化合物,因为它们具有抗氧化特性。对从尼日利亚埃多州贝宁市的五个市场获得的新鲜和变质番茄果实进行了植物化学和近似评价研究。本研究的目的是研究新鲜和变质番茄果实的植物化学成分和近似成分。从尼日利亚埃多州贝宁市的五个市场随机购买了总共400个西红柿。在每个市场,从10个不同的卖家那里购买了40个新鲜的(结实的、未损坏的)和40个变质的(损坏的、变质的)西红柿。样品分别包装到不同的无菌容器中,贴上标签,并立即运送到实验室进行植物化学和近似分析。植物化学和近似成分分析采用分析化学家实验室程序的官方分析方法进行。结果表明,新鲜和变质番茄果实的植物化学和近似成分值存在显著差异。新鲜番茄果实的粗碳水化合物、粗蛋白质、粗脂肪、皂苷、黄酮类和生物碱含量高于变质番茄果实,水分、粗灰分、粗纤维、单宁和多酚含量高于新鲜番茄果实。本研究表明,腐败降低了番茄果实中一些重要的植物化学成分和近似成分
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African Scientist
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