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Phytochemical Analysis and in vitro Antioxidant Potential of Aqueous and Ethanol Extracts of Irvingia gabonensis Stem Bark 山竹茎皮水提取物和乙醇提取物的植物化学分析及体外抗氧化能力
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.039
C. Otitolaiye, A. Omonkhua, K. Oriakhi, E. Okello, I. Onoagbe, F. Okonofua
Background: Irvingia gabonensis extracts are documented to possess antidiabetic, hypocholesterolemic, and antioxidant activities. The phytochemical components of medicinal plants are responsible for their therapeutic properties, particularly those with antioxidant properties. Objectives: The quantitative phytochemicals and in vitro antioxidant properties of the aqueous and ethanol extracts of I. gabonensis stem bark were assessed in this study. Materials and Methods: Standard techniques were used to measure the concentrations of phenols, flavonoids, tannins, alkaloids, steroids, and saponins in water and alcohol extracts of this plant. Total Antioxidant Power (TAP) and the extract's capacity to scavenge free radicals including superoxide, nitric oxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis-(3-ethylbenzoth iazoline-6-sulfonic acid) (ABTS + ), β-carotene, and hydrogen peroxide were also evaluated. The extracts' Ferric-Reducing Potential (FRAP) was also assessed. Results: The alcohol extract had significantly ( P < 0.05) higher concentrations of all the phytochemicals measured as well as near significantly ( P <0.066) higher TAP in comparison to the aqueous extracts. In general, the in vitro antioxidant capacity of the ethanol extract surpassed that of the water extract. The ethanol extract had IC 50 values that were comparable to or less than the reference standards for its ability to neutralize nitric oxide, H 2 O 2 , superoxide, and DPPH radicals. Conclusion: The outcomes of the quantitative phytochemical analysis and in vitro antioxidant effects of aqueous and ethanol extracts of I. gabonensis stem bark clearly show their potential as an excellent reservoir of bioactive compounds and scavengers of deleterious oxidants; properties that could be explored therapeutically.
背景:葛藤提取物被证明具有抗糖尿病、降胆固醇和抗氧化活性。药用植物的植物化学成分对其治疗特性负责,尤其是那些具有抗氧化特性的植物。目的:本研究对山竹茎皮水提取物和乙醇提取物的植物化学成分和体外抗氧化性能进行了定量评价。材料与方法:采用标准技术测定该植物水提物和醇提物中酚类、黄酮类、单宁、生物碱、甾体和皂苷的含量。还评估了提取物的总抗氧化能力(TAP)和清除自由基的能力,包括超氧化物、一氧化氮、2,2-二苯基-1-苦基肼(DPPH)、2,2-锌基双-(3-乙基苯并噻唑啉-6-磺酸)(ABTS+)、β-胡萝卜素和过氧化氢。还评估了提取物的铁还原潜力(FRAP)。结果:与水提取物相比,醇提取物具有显著(P<0.05)高的所有植物化学物质浓度,以及接近显著(P<0.01)高的TAP。总的来说,乙醇提取物的体外抗氧化能力超过了水提取物。乙醇提取物的IC50值与其中和一氧化氮、H2 O2、超氧化物和DPPH自由基的能力相当或低于参考标准。结论:山竹茎皮水提取物和乙醇提取物的定量植物化学分析结果和体外抗氧化作用清楚地表明,它们是生物活性化合物的良好库和有害氧化剂的清除剂;可以在治疗上探索的特性。
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引用次数: 1
Role of Polyphenols and Flavonoids as Anti-Cancer Drug Candidates: A Review 多酚和黄酮类化合物作为抗癌候选药物的作用:综述
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.022
Medha Mohan Hegde, K. Lakshman, Mrs. Medha, Mohan Hegde
Natural drug-based chemotherapeutic have advanced at an unprecedented rate over the past decade. Owing to protective roles in vegetation, and exceptional antioxidant qualities, polyphenols and flavonoids have demonstrated promising clinical implications in malignancies amongst other plant metabolites. It is widely debated how dietary flavonoids and polyphenols can prevent cancer. Flavonoids are believed to execute a significant role in cancer prevention and treatment, as corroborated from experimental studies, epidemiological research, and human clinical trials. Carcinogen deactivation, antimutagenic, cell cycle arrest, apoptosis and differentiation, suppression of vasculature, oxidative stress, and reversion of multidrug resistance are among the many mechanisms of action that have been discovered. The present review outlines the classification of various polyphenols and flavonoids and their potential as anticancer therapeutic agents.
在过去的十年里,以天然药物为基础的化疗以前所未有的速度取得了进展。由于多酚和黄酮类化合物在植物中的保护作用和卓越的抗氧化性能,在其他植物代谢产物中,它们在恶性肿瘤中具有良好的临床意义。饮食中的黄酮类化合物和多酚类化合物如何预防癌症一直备受争议。实验研究、流行病学研究和人体临床试验证实,黄酮类化合物在癌症预防和治疗中发挥着重要作用。致癌物失活、抗突变、细胞周期停滞、细胞凋亡和分化、血管系统抑制、氧化应激和多药耐药性逆转是已经发现的许多作用机制之一。本文综述了各种多酚和黄酮类化合物的分类及其作为抗癌治疗剂的潜力。
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引用次数: 1
Macro-microscopic and HPTLC Atlas of Canavalia gladiata (Jacq.) DC. Fruit 林花的宏观显微镜和HPTLC图谱。水果
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.030
Susikumar Sundharamoorthy, Gokula Kannan Sundharamoorthy, A. Mandal, Shakila Ramachandran, S. Govindaraju, Sunil Kumar Koppala Narayanan
Background: Canavalia gladiata (Jacq.) DC. (Family Leguminosae) is a large annual or perennial climber with a terete glabrous stem, native to Indo-Malaysian and also distributed in tropical, subtropical regions. C. gladiata (Jacq.) DC. is generally confused with another closely related species i.e. C. ensiformis (Linn.) DC (Jack bean). The tender pods of both the above species have close similarity in morphology, especially shape and size of fruit, therefore it is difficult to differentiate on their vegetative and also fruiting stages. The plant C. ensiformis mentioned as a synonym of C. gladiata in many of the earlier literature though they are 2 different taxa. Some authors published different colour seeds in the name of C. gladiata . It is doubtful if C. ensiformis (Linn.) DC. or C. gladiata (Jacq.) DC was studied during that analysis. Objectives: A systematic pharmacognostical study has been executed to identify the correct botanical source. Materials and Methods: All the studies were carried out by standard procedures in Pharmacopoeias and other authentic literature. Results: Macroscopically surface characters followed by odour and taste, anatomically TS of the pericarp, plecenta, testa, cotyledon and radical, powder microscopically epidermal cells with stomata and prismatic crystal cystolith, trichomes, testa palisade cells, sclereids with different shape and size, brownish content, starch grains, tracheids, fibres and prismatic crystals of calcium oxalate are the unique diagnostic characters observed. HPTLC with different spots having unique Rf values in the pericarp, testa, cotyledon and seeds will be helpful for critical identification of the species. Conclusion: The findings of the present study will be helpful in the identification and differentiation of related species as the whole drug or in powder form.
背景:加拿大夏花(Jacq.)DC。(豆科)是一种大型一年生或多年生攀援植物,茎圆柱状无毛,原产于印度-马来西亚,也分布于热带和亚热带地区。C.gladiata(Jacq.)DC。通常与另一个亲缘关系密切的物种,即C.ensiformis(Linn.)DC(Jack bean)混淆。上述两种的嫩荚在形态上,特别是果实的形状和大小上有着密切的相似性,因此在营养期和结果期都很难区分。在许多早期文献中,C.ensiformis植物被称为C.gladiata的同义词,尽管它们是两个不同的分类群。一些作者以C.gladiata的名义发表了不同颜色的种子。ensiformis(Linn.)是否为DC是值得怀疑的。或C.gladiata(Jacq.)DC。目的:进行了一项系统的生药学研究,以确定正确的植物来源。材料和方法:所有研究均按照药典和其他权威文献中的标准程序进行。结果:从宏观上看,表面特征其次是气味和味道,从解剖学上看,果皮、软毛、种皮、子叶和根的TS,粉末显微镜下的表皮细胞有气孔和棱柱状晶体膀胱石,毛状体,种皮栅栏细胞,不同形状和大小的硬骨片,褐色含量,淀粉粒,管胞,草酸钙的纤维和棱柱状晶体是观察到的独特的诊断特征。在果皮、种皮、子叶和种子中具有独特Rf值的不同斑点的HPTLC将有助于物种的关键鉴定。结论:本研究的结果将有助于整个药物或粉末形式的相关物种的鉴定和分化。
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引用次数: 0
Essential Oils of Rosmarinus officinalis and Eucalyptus globulus Cultivated in the Mountainous Region of the State of Rio de Janeiro (Brazil): Chemical Profile and Antileishmanial Activity 里约热内卢州(巴西)山区栽培的迷迭香和蓝桉精油:化学成分和抗炎活性
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.032
R. C. Zauli, T. Santos, Alberto Wisniewski Jr, P. Xander, A. C. Pascoal
The present study aimed to characterize the chemical profile of essential oils of Rosmarinus officinalis (EORo) and Eucalyptus globulus (EOEg) cultivated in the mountainous region of the state of Rio de Janeiro, Brazil, and to verify the leishmanicidal potential, as well as to determine the cytotoxicity in vitro in mammalian cells. EORo had α-Pinene (37.99%), Cineol (21.48%), D-Verbenone (5.78%) and Limonene (3.28%) as major constituents. The EOEg had as major components Cineol (75.52%), Limonene (8.82%) and o-Cymeno (7.81%). The EOEg had a lower IC 50 value of 14.03 ± 2.08 µg/mL, while EORo had an IC 50 value of 31.12 ± 4.6 µg/mL, both during the 24-hr exposure period. In the 48-hr period, the IC 50 value was almost twice as high with rosemary oil, while in eucalyptus oil there was no significant difference when exposed in this period. The selectivity of EOs was demonstrated in murine cells, showing almost 30 times less toxic to the cell than to the parasite. It can be concluded that this is a pioneering study on the potential of these essential oils against the leishmania parasite. Furthermore, the low toxicity effect on the host cell encourages future studies and in vivo applications.
本研究旨在表征巴西巴西里约热内卢州山区种植的迷迭香(Rosmarinus officinalis, EORo)和蓝桉(Eucalyptus globulus, EOEg)精油的化学成分,并验证其杀利什曼尼潜能,同时测定其体外对哺乳动物细胞的细胞毒性。EORo的主要成分为α-蒎烯(37.99%)、桉树油(21.48%)、d -马尾草酮(5.78%)和柠檬烯(3.28%)。其主要成分为桉叶油(75.52%)、柠檬烯(8.82%)和o-Cymeno(7.81%)。在24小时的暴露期间,EOEg的ic50值为14.03±2.08µg/mL, EORo的ic50值为31.12±4.6µg/mL。在48小时内,迷迭香油的ic50值几乎是其两倍,而桉树油在这段时间内没有显著差异。在小鼠细胞中证明了EOs的选择性,显示对细胞的毒性几乎比对寄生虫的毒性低30倍。可以得出结论,这是一项关于这些精油对抗利什曼原虫潜力的开创性研究。此外,对宿主细胞的低毒性作用鼓励未来的研究和体内应用。
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引用次数: 0
Rubia cordifolia L. Crude Aerial Part Extracts Show a High Potential as Antimalarials against Chloroquine Resistant Plasmodium falciparum Strains in vitro 风叶粗提物作为抗氯喹耐药恶性疟原虫的体外抗疟药物具有很高的应用潜力
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.031
Magara Jeremiah, L. Kamau, G. Nyambati, H. Ozwara
Introduction: Plasmodium falciparum human malaria parasite is resistant to most available medicines in Africa, necessitating research for new drugs. Rubia cordifolia L. is used in traditional malaria treatment in Kenya despite no supporting scientific data. Objectives: To evaluate anti-plasmodial efficacy of extracts from the aerial part of Rubia cordifolia against chloroquine sensitive (3D7) and resistant (W2) Plasmodium falciparum strains. Methods: Hexane, methanol and water were separately used in crude extractions from open shade dried aerial plant parts. Phytochemical composition was determined qualitatively. Anti-plasmodial efficacy of serial dilutions (range; 0.4 to 50 μg/ml) of each extract were evaluated in vitro and compared using ANOVA and Tukey’s HSD test, at p <0.05). Results: All the extracts significantly inhibited parasites growth, in a dose dependent manner. At 50 μg/ml, inhibition was (84.07%, 77.94% and 66.08%) for hexane, methanol and water extracts respectively against W2 and (80.06%, 78.36% and 60.92%) against 3D7 strain. Hexane extract showed IC 50 0.551 µg/ml and 2.747 micrograms/ml against W2 and 3D7 respectively. Methanol extract, IC 50 1.231 and 3.528 µ g/ml respectively, aqueous extract showed moderate activity, IC 50 5.348 μg/ml and 17.341 µg/ml against the strains respectively. Chloroquine resistant (W2 strain) was more responsive to the extracts than 3D7 strain. Conclusion: Anti-plasmodial activities were in the order, Hexane>methanol>aqueous and were attributed to the phytochemicals present in the extracts. This presents evidence of R. cordifolia as anti-malarial drugs’ source. Further work is required to identify, purify, and characterize active molecules for development of anti-malaria drugs.
引言:恶性疟原虫人类疟原虫对非洲大多数可用药物具有耐药性,因此需要研究新药。茜草在肯尼亚被用于传统的疟疾治疗,尽管没有支持的科学数据。目的:评价茜草地上部分提取物对氯喹敏感株(3D7)和耐药株(W2)的抗疟原虫效果。方法:采用正己烷、甲醇和水分别从遮荫干燥的气生植物部位提取粗提物。定性测定了植物化学成分。在体外评估每种提取物的系列稀释液(范围:0.4至50μg/ml)的抗疟原虫效力,并使用ANOVA和Tukey’s HSD测试进行比较,在p甲醇>水溶液条件下,将其归因于提取物中存在的植物化学物质。这提供了茜草作为抗疟疾药物来源的证据。还需要进一步的工作来鉴定、纯化和表征抗疟疾药物的活性分子。
{"title":"Rubia cordifolia L. Crude Aerial Part Extracts Show a High Potential as Antimalarials against Chloroquine Resistant Plasmodium falciparum Strains in vitro","authors":"Magara Jeremiah, L. Kamau, G. Nyambati, H. Ozwara","doi":"10.5530/pres.15.2.031","DOIUrl":"https://doi.org/10.5530/pres.15.2.031","url":null,"abstract":"Introduction: Plasmodium falciparum human malaria parasite is resistant to most available medicines in Africa, necessitating research for new drugs. Rubia cordifolia L. is used in traditional malaria treatment in Kenya despite no supporting scientific data. Objectives: To evaluate anti-plasmodial efficacy of extracts from the aerial part of Rubia cordifolia against chloroquine sensitive (3D7) and resistant (W2) Plasmodium falciparum strains. Methods: Hexane, methanol and water were separately used in crude extractions from open shade dried aerial plant parts. Phytochemical composition was determined qualitatively. Anti-plasmodial efficacy of serial dilutions (range; 0.4 to 50 μg/ml) of each extract were evaluated in vitro and compared using ANOVA and Tukey’s HSD test, at p <0.05). Results: All the extracts significantly inhibited parasites growth, in a dose dependent manner. At 50 μg/ml, inhibition was (84.07%, 77.94% and 66.08%) for hexane, methanol and water extracts respectively against W2 and (80.06%, 78.36% and 60.92%) against 3D7 strain. Hexane extract showed IC 50 0.551 µg/ml and 2.747 micrograms/ml against W2 and 3D7 respectively. Methanol extract, IC 50 1.231 and 3.528 µ g/ml respectively, aqueous extract showed moderate activity, IC 50 5.348 μg/ml and 17.341 µg/ml against the strains respectively. Chloroquine resistant (W2 strain) was more responsive to the extracts than 3D7 strain. Conclusion: Anti-plasmodial activities were in the order, Hexane>methanol>aqueous and were attributed to the phytochemicals present in the extracts. This presents evidence of R. cordifolia as anti-malarial drugs’ source. Further work is required to identify, purify, and characterize active molecules for development of anti-malaria drugs.","PeriodicalId":19813,"journal":{"name":"Pharmacognosy Research","volume":" ","pages":""},"PeriodicalIF":0.7,"publicationDate":"2023-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49107775","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Total Polyphenolic Content, Antioxidant Activity and Chromatographic Profiling of Extracts of Ardissia solanacea 青枯提取物的总多酚含量、抗氧化活性及色谱分析
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.038
J. Chopade, Asha B. Thomas, S. Chitlange
Background: The current study focuses on the preliminary phytochemical analysis, antioxidant potential and identification of phytochemicals in Ardissia solanacea leaves extract using chromatography and HR-MS. Materials and Methods: The occurrence of phytoconstituents in different extracts of Ardissia solanacea were assessed by standard procedures. In vitro antioxidant potential was determined by Hydrogen peroxide and DPPH method. The extract was fractionated by Flash Chromatography. The fractions were analysed using HPTLC and further analyzed by HR-MS method to detect and characterize the active phytoconstituents present in it. Results: The highest concentration of flavonoids (371.91± 0.167 mg/g of Quercetin Equivalent), phenolics (10.138±0.010 mg/g of Gallic acid Equivalent) and tannins (148.23±0.510 mg/g of Tannic acid Equivalent) was observed in the ethanol extract. The antioxidant activity by DPPH and H 2 O 2 assay demonstrated that the ethanolic extract (AsEt) showed highest anti-oxidant potential (74.21% and 83.16% respectively). The ASEt was fractionated by using Flash chromatography. As a result, Out of 11 fractions, one fraction namely AsEt3 was selected further based on HPTLC results. The HR-MS analysis of ASEt3 indicated presence of thirteen compounds wherein bergapten was predominantly identified. Conclusion: It was revealed that the leaves of Ardissia solanacea possesses high antioxidant potential. The known phytoconstituents namely quercetin and taxifolin along with one unknown compound were identified through the HR-MS study. Using mass library data, we report herein 2 flavonoids and 1 phenolic in the AsEt extract.
背景:本研究采用色谱法和HR-MS法对青枯叶提取物中的植物化学成分进行了初步分析、抗氧化潜力和植物化学成分鉴定。材料与方法:采用标准方法对青枯不同提取物中植物成分的含量进行了测定。采用过氧化氢和DPPH法测定体外抗氧化能力。提取物通过快速色谱法进行分级。结果:乙醇提取物中黄酮类化合物(371.91±0.167mg/g槲皮素当量)、酚类化合物(10.138±0.010mg/g没食子酸当量)和单宁(148.23±0.510mg/g鞣酸当量)含量最高。DPPH和H2 O2测定的抗氧化活性表明,乙醇提取物的抗氧化能力最高(分别为74.21%和83.16%)。ASEt采用快速色谱法进行分级。结果,在11个级分中,基于HPTLC结果进一步选择了一个级分,即AsEt3。ASEt3的HR-MS分析表明存在13种化合物,其中主要鉴定了佛手柑内酯。结论:青枯叶具有较高的抗氧化能力。通过HR-MS研究鉴定了已知的植物成分,即槲皮素和紫杉醇以及一种未知化合物。利用大量文库数据,我们在此报道了AsEt提取物中的2种黄酮类化合物和1种酚类化合物。
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引用次数: 0
Water Lily (Nymphaea nouchali Burm. f): An Ancient Treasure of Food and Medicine 睡莲(Nymphaea nouchali Burm.f):古代食物和药物的瑰宝
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.024
Basani Kiranmai, M. Sandhyarani, Ashok Kumar Tiwari
Nymphaea nouchali (Syn. Nymphaea stellata Willd.) from family Nymphaeaceae, is a species of perennial aquatic flowering plant with huge round floating leaves and rhizomes. It is well-known and prominent herb in Ayurveda and Siddha system of medicines with multiple medicinal properties. It comes from southern and eastern regions of Asia, and is a national blossom of Sri Lanka and Bangladesh. Scientific investigation has revealed that it exhibits vast range of pharmacological actions, namely antihyperglycemic, antioxidant, antimicrobial, analgesic, antiinflammatory, antipyretic, antitumor, hepatoprotective, antiulcer, antihelmintic, antinociceptive, immunomodulatory activities etc. Polyphenols, flavonoids, sterols, alkaloids, saponins, tannins, protein, nymphasterol, nymphayol have been recognized as important factors in the medicinal effects of N. nouchali . The present review focuses on pharmacological and phytochemical investigation of N. nouchali .
牛睡莲(Nymphaea nouchali)是睡莲科的一种多年生水生开花植物,具有巨大的圆形漂浮叶和根茎。它是阿育吠陀和悉达教药物体系中著名和突出的草药,具有多种药用特性。它来自亚洲南部和东部地区,是斯里兰卡和孟加拉国的国花。科学研究表明,它具有广泛的药理作用,即抗高血糖、抗氧化、抗菌、镇痛、抗炎、解热、抗肿瘤、保肝、抗溃疡、抗过敏、抗伤害、免疫调节等活性,若虫醇已被认为是影响努查利猪笼草药效的重要因素。本文对牛乳杆菌的药理和植物化学研究进行了综述。
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引用次数: 0
Antidiabetic Potential and Chronic Toxicity of Hydroalcoholic Extract of Echeveria subrigida Leaves 马尾莲叶水醇提取物的抗糖尿病作用及慢性毒性研究
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.034
B. Heredia-Mercado, F. Delgado-Vargas, L. U. Osuna-Martínez, E. Noguera-Corona, J. López-Valenzuela, R. Ramos-Payán, G. López-Angulo
Background: Echeveria subrigida extracts have biological activities of human health importance. However, the in vivo effects on glucose levels and chronic toxicity are unknown. Objectives: To analyse the in vivo hypoglycemic and antihyperglycemic effects (50, 100, and 200 mg/kg b.w.) and chronic toxicity (1000 mg/kg b.w. for 270 days) of the hydroalcoholic extract of E. subrigida (HE–Es) in BALB/c mice. Materials and Methods: The HE–Es was analysed by HPLC. Glucose levels were measured to establish the effects on glycemia. Different parameters were registered in the toxicity assay: e.g. , feed consumption, appearance/behaviour, biochemical and haematological parameters and liver and kidney histologies. Results: Quercetin–3-O -β-glucoside and isorhamnetin–3-O -β-glucoside were the main flavonoids in the HE–Es. Glycemia was reduced by the HE–Es (200 mg/kg b.w., 49.1%) and glibenclamide (10 mg/kg b.w., 52%) treatments. Comparing the antihyperglycemic activities, similar reductions were found between HE–Es (100 mg/kg b.w., 29.32%; 200 mg/kg, 28.99%) and acarbose (10 mg/kg b.w., 19.87%) treatments. On the other hand, the HE–Es was innocuous in mice (LD 50 > 1000 mg/kg b.w.), and the results suggested that HE–Es had adaptogenic, and immunostimulant activities. The hepatic and renal histologies were normal; however, male mice showed level zero steatosis that disappeared in the HE–Es satellite after treatment withdrawal. Conclusion: This study reports for the first time the in vivo effects on blood glucose levels of HE–Es and chronic toxicity of a Crassulaceae plant, supporting the antidiabetic potential and safety of HE–Es. Future studies must corroborate the effects of HE–Es in humans, allowing its use in high-value formulations.
背景:刺五加提取物具有重要的生物活性,对人体健康具有重要意义。然而,体内对葡萄糖水平的影响和慢性毒性尚不清楚。目的:分析枯草芽孢杆菌水醇提取物(HE–Es)在BALB/c小鼠体内的降血糖和抗高血糖作用(50、100和200 mg/kg体重)以及慢性毒性(1000 mg/kg体重,持续270天)。材料与方法:采用高效液相色谱法对HE–Es进行分析。测量血糖水平以确定对血糖的影响。毒性试验中记录了不同的参数:例如,饲料消耗、外观/行为、生化和血液学参数以及肝脏和肾脏组织学。结果:槲皮素-3-O-β-葡萄糖苷和异鼠李素-3-O-β葡萄糖苷是HE–Es中的主要黄酮类化合物。HE–Es(200 mg/kg体重,49.1%)和格列本脲(10 mg/kg体重,52%)治疗可降低血糖。比较抗高血糖活性,HE–Es(100 mg/kg体重,29.32%;200 mg/kg体重,28.99%)和阿卡波糖(10 mg/kg体重,19.87%)的治疗效果相似。另一方面,HE–Es在小鼠中是无害的(LD 50>1000 mg/kg b.w.),结果表明,HE–Es具有适应和免疫刺激活性。肝肾组织学正常;然而,雄性小鼠表现出零级脂肪变性,在停药后在HE–Es卫星中消失。结论:本研究首次报道了HE–Es对血糖水平的体内影响和景天科植物的慢性毒性,支持了HE–Es的抗糖尿病潜力和安全性。未来的研究必须证实HE–Es对人类的影响,使其能够用于高价值的配方中。
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引用次数: 0
Analytical Quality by Design (AQBD) Assisted Development and Validation of HPTLC Method for Estimation of Rottlerin in Topical Patch Formulation 设计质量分析(AQBD)辅助高效液相色谱法测定外用贴剂制剂中罗特勒素的含量
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.029
K. Bodas, Vaibhav Mukund Shinde, Deshmukh Vishal, D. Sheetal
Background: Rottlerin, a natural polyphenolic ketone is a major constituent of Mallotus philippensis (Lam.) Mull. Arg. plant. Although, less explored it has diverse array of therapeutic applications. Objectives: The current work aimed to develop novel, simple, speedy, accurate, potent High Performance Thin Layer Chromatography Method (HPTLC) to separate, and quantify rottlerin from the herbal topical patch In-House formulation. Materials and Methods: This was the foremost attempt to develop and validate HPTLC method using Analytical Quality by design (AQbD) approach. Box Behnken design (BBD) coupled with response surface methodology approach was followed for the systematic optimization. The end results of toluene content, chamber conditioning time, and solvent front on R f value of rottlerin was studied. The optimised method was validated as per ICH guidelines. Results: For HPTLC, stationary phase used was aluminium plates 60F 254 coated with silica gel as. AQbD optimised conditions were mobile phase proportion namely toluene: ethyl acetate: methanol: ammonia (5:4:2:0.2), development distance 80 mm, band width 6mm, and chamber saturation time 10 min. The method generated well resolved and compact bands at R f of 0.41±0.05. The developed method exhibited high accuracy, precision, robustness, and recovery. The quantity of Rottlerin in developed herbal patch was found to be 134.8 ng/band. Conclusion: In a nutshell, the present study undeniably vouches for a QbD based method development approach for Rottlerin and can be extrapolated to estimate it in other herbal extracts, or marketed formulations.
背景:马丽莲(Mallotus philippensis)是一种天然多酚类酮,是马丽莲(Mallotus philippensis)的主要成分。考虑。参数。工厂。虽然,较少探索它有各种各样的治疗应用。目的:建立一种新的、简单、快速、准确、有效的高效薄层色谱法(HPTLC)分离和定量中药外用贴剂制剂中鹿茸素的方法。材料和方法:这是首次尝试开发和验证采用分析质量设计(AQbD)方法的HPTLC方法。采用Box Behnken设计(BBD)结合响应面法进行系统优化。研究了甲苯含量、腔室调理时间、溶剂锋面等因素对转化剂R - f值的最终影响。优化后的方法按照ICH指南进行了验证。结果:hplc固定相为60f254铝板,硅胶包覆。AQbD优化条件为流动相比例为甲苯:乙酸乙酯:甲醇:氨(5:4:2:2 .2),显色距离80 mm,带宽6mm,腔室饱和时间10 min。该方法在rf = 0.41±0.05时产生分辨率高、紧凑的条带。该方法具有较高的准确度、精密度、鲁棒性和回收率。开发的中药贴剂中Rottlerin的含量为134.8 ng/band。结论:简而言之,目前的研究不可否认地证明了一种基于QbD的方法开发方法,可以推断出在其他草药提取物或上市配方中估计它。
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引用次数: 0
Abrogation of Acute Inflammation in ICR Mice with Topical Administration of Philippine Stingless Bee (Tetragonula biroi Friese) Honey 局部给予菲律宾无刺蜂(Tetragonula biroi Friese)蜂蜜消除ICR小鼠急性炎症
IF 0.7 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.5530/pres.15.2.028
M. J. Desamero, Mikaela Bernadette Andres Rabino, Maria Angelica Rimas Tayao, M. Ang, J. Bariuan, Roxanne P. Gapasin, T. M. Collantes, M. M. R. Rondina, C. Fernandez-Colorado, C. Cervancia, M. Estacio
Background: Honey, a sweet sugar-rich bee-derived product, has been widely recognized in the realm of Ayurveda and Pharmacognosy for the treatment of various inflammatory conditions including inflammatory bowel disease, asthma, arthritis, and gastric ulcer. However, the anti-inflammatory effect of Philippine honey obtained from local stingless bees remains unexplored and poorly investigated. Hence, this study delved on the anti-inflammatory potential of topically applied Philippine stingless bee honey (PSH) using the λ-Carrageenan-induced mouse model of paw edema. Materials and Methods: A total of 30, male ICR mice of six weeks of age were randomly divided into the following groups ( n =10 per group) as follows: Distilled water, 1% Diclofenac sodium, and Honey-treated group. All treatments were administered immediately after Carrageenan injection and then every 8 hr during the 24-hr test duration. Results: Repeated topical application of PSH significantly attenuated the gross hind paw swelling observed at the onset of the 6 hr post-induction ( pi ) until the 24 hr pi with Carrageenan in contrast to the Distilled water-treated group. This corresponded histologically to a marked reduction in dermal thickness, dermal edema, and leukocytic infiltration. Whereas, at the cytokine level, this correlated to significant suppression of the circulating blood levels of pro-inflammatory cytokines, TNF-α, IL-1β, and IL-6. Conclusion: Based on these results, honey from the Philippine stingless bees shows convincing anti-inflammatory activity which is partly mediated through the regulation of the expression of inflammation-associated cytokines.
背景:蜂蜜是一种甜的富含糖的蜜蜂衍生产品,在阿育吠陀和生药学领域被广泛认可用于治疗各种炎症性疾病,包括炎症性肠病、哮喘、关节炎和胃溃疡。然而,从当地无刺蜜蜂获得的菲律宾蜂蜜的抗炎作用仍未被探索和调查。因此,本研究通过λ-卡拉胶诱导的小鼠足跖水肿模型,深入研究了局部应用菲律宾无刺蜜蜂蜂蜜(PSH)的抗炎潜力。材料与方法:选取6周龄雄性ICR小鼠30只,随机分为蒸馏水组、1%双氯芬酸钠组和蜂蜜处理组,每组10只。所有治疗均在卡拉胶注射后立即进行,然后在24小时的试验期间每8小时进行一次。结果:与蒸馏水处理组相比,在诱导后6小时(pi)开始至24小时(pi)时,用卡拉胶反复局部应用PSH显著减轻了观察到的总后爪肿胀。这在组织学上对应于真皮厚度、真皮水肿和白细胞浸润的显著减少。然而,在细胞因子水平上,这与循环血液中促炎细胞因子、TNF-α、IL-1β和IL-6水平的显著抑制相关。结论:基于这些结果,菲律宾无刺蜂蜂蜜显示出令人信服的抗炎活性,部分是通过调节炎症相关细胞因子的表达来介导的。
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引用次数: 0
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