Safety,efficacy and toxicological evaluation of a novel,patented anti-diabetic extract of Trigonella Foenum-Graecum seed extract (Fenfuro)

Safety and anti-diabetic efficacy of a novel, proprietary Trigonella foenum-graecum seed extract [novel fenugreek extract (FE), Fenfuro?, CR0010810) enriched in furostanolic saponins (>60% w/w, HPLC) were assessed. Concerning safety, we undertook studies dealing with acute oral toxicity, 28-d sub-chronic toxicity and Ames’ bacterial reverse mutation assay that revealed no toxicity. Concerning efficacy, we examined beneficial effects of the extract on rats with type 2 diabetes (T2D). Male Sprague–Dawley rats received a high-fat diet for 2 weeks followed by streptozotocin (STZ, 35?mg/kg i.p.) to produce T2D. Seven days post-STZ, rats showing ≥300?mg/dl fasting plasma glucose level (PGL) were included in the study. FE (150- or 450- mg/kg p.o.) and glipizide (5?mg/kg p.o.) were administered once daily for 20?d and then twice daily for another 10?d (total 30?d). Blood samples were collected at 0, 10, 20 and 30?d of treatment and estimated for fasting plasma triglyceride (PTG), total cholesterol and insulin levels. After 30?d, FE and glipizide-treated diabetic animals were treated in combination with or without metformin (100?mg/kg) twice daily for another 10?d. FE did not influence body weight, feed and water intake. FE (150?mg/kg p.o.) reduced PTG levels in T2D rats by 22%, 24.6% and 29% at 10, 20 and 30?d of treatment, respectively, while glipizide (5?mg/kg p.o.) reduced the PTG levels by 57.4%, 46.2% and 39.4% at these time points. FE (450?mg/kg) treatment in STZ-induced diabetic rats produced significant hypoglycemic activity (approximately 31.5%) as compared to insulin (48.2% with 1 U/kg i.p.). FE (150?mg/kg p.o.) and metformin (100?mg/kg p.o.) combined produced significant reduction (20.7%) of PGL in T2D rats. No adverse effects were observed. We conclude after extensive in vitro and in vivo safety and efficacy studies that FE is safe and effective in treating T2D.     

Vegetable residue of fenugreek (Trigonella Foenum-Graecum), waste biomass for removal of Basic Violet 14 from wastewater: Kinetic,equilibrium, and reusability studies

The present work has focused on the utilization of vegetable residue of Fenugreek (VRF), sustainable and novel adsorbent for sequestration of Basic Violet 14 (BV 14) dye. Effect of various batch operating parameters on BV 14 adsorption has been studied in detail and optimum values were reported as pH of 7.2, adsorbent loading of 0.125 g, shaking time of 105 min and temperature of 323 K. VRF was characterized based on various techniques as FTIR, DLS, zeta potential, SEM-EDS, and BET analysis. Kinetic and equilibrium data have been well exemplified by pseudo 1^st order and Freundlich model, respectively. The maximum uptake capacity was reported to be significant as 177.78 mg/g. Mechanism of BV 14 adsorption on VRF was reported to involve steps as pore diffusion and film diffusion based on reported data fitting to Boyd model. Thermodynamic investigation affirmed adsorption as spontaneous, endothermic and physical in nature. Recovery of adsorbed BV 14 from VRF was conducted using ethanol as an elution media and regenerated VRF was applied for fresh BV 14 adsorption in five cycles. Recovery values were reported to be significant as 98.92% for first cycle and 84.41% for fifth cycle. Similarly, uptake capacity values were reported to be significant as 39.34 mg/g for first cycle and 32.47 mg/g for fifth cycle, which has proved the recovery potential and thus the applicability of VRF for subsequent cycles of BV 14 adsorption. Overall, the present work proved VRF as a promising adsorbent for successful remediation of BV 14 dye.     

Diosgenin and Dioscorea Microscopy

Abstract

On assaying different parts of Iberis amara L. (Cruciferae) for their fungitoxicity against Hel-minthosporium oryzae, flowers and seeds were found to possess strong toxicity. Seed extract was found to be fungicidal at the minimum inhibitory concentration (2%), remained active up to 35 days, and exhibited a broad range of activity and non-phytotoxicity. The fungitoxicity of the seeds was thermostable up to 120°C, remained active up to 9 months at room temperature but declined on autoclaving.     

Molluscicidal Properties of Agave Americana and Balanites Aegyptica

Abstract

Agave Americana and Balanites Aegyptica Were Evaluated For Molluscicidal Properties Against Eggs and Adults Of Three Species Of Freshwater Snails, Lndoplanorbis Exustus, Lymnaea Luteola and Gyrau-Lus Convexiusculus and For Haemolytic Activity With Sheep Red Blood Cells. Further Studies Were Then Performed With Extracts Of The Leaves Of A. Americana and The Fruits Of B. Aegyptica, and A. Americana Was Found To Be More Effective Against All Stages Of Snail Development.     

HPLC法测定金线莲中芦丁的含量

目的：建立金线莲中芦丁的含量测定方法。方法：采用高效液相色谱法。选用Lanbo-Kromasil-C18色谱柱（250 mm×4.6 mm,5μm）;以甲醇-0.2%磷酸溶液（40∶60）为流动相;检测波长：257 nm,流速：1.0 ml·min-1,柱温：30℃。结果：芦丁在进样量0.021~0.433μg范围内呈良好的线性关系（r=0.999 6）。平均加样回收率为96.65%（RSD=1.67%,n=9）。结论：本法简便、快速、专属性强、重复性好。     

Molluscicidal activity of Balanites aegyptiaca against Monacha cartusiana

Context: Balanites aegyptiaca (L.) Delile (Zygophyllaceae) is a tropical tree that has many folk uses in various countries. The bark extract is used for the control of the fresh water snails that act as intermediary host of Schistosoma.

Objective: Study the molluscicidal activity and chemical constituents of seed oil and seed glycosides of B. aegyptiaca against Monacha cartusiana and determine the structure-activity relationship.

Materials and methods: Two bioassay methods (residual film application and the leaf dipping technique) were used to evaluate the toxicity effect of the seed oil and glycosides, in concentrations of 1.000, 0.500, 0.250 and 0.125%. The seed oil was analysed by GC/MS. Acid hydrolysis and chromatographic separation were used to study the seed saponins.

Results: The bioassay of B. aegyptiaca against the land snail, M. cartusiana, indicated the activity of the seed oil and the high activity of the seed saponins. The seed glycosides gave 30.0, 53.3, 73.0 and 73.3% mortality for concentrations of 0.125, 0.250, 0.500 and 1.00%, respectively. The LC₅₀ values were 0.335 and 0.256%, respectively. The seed oil was analysed by GC/MS. Acid hydrolysis of the seed saponins gave a mixture of diosgenin, yamogenin and 3,5-spirostadiene.

Discussion and conclusion: To study the structure-activity relationship, a triterpenoidal saponin and a triterpenoidal saponins rich extract (of Zygophyllum coccenum) were proven to be inactive. Thus, the activity is associated with the steroidal, not triterpenoidal saponins. Moreover, a spirostane aglycone without sugar moiety, was found to be inactive and attained the activity by glycosidation.     

Molluscicidal activity of Balanites aegyptiaca against Monacha cartusiana

Context: Balanites aegyptiaca (L.) Delile (Zygophyllaceae) is a tropical tree that has many folk uses in various countries. The bark extract is used for the control of the fresh water snails that act as intermediary host of Schistosoma. Objective: Study the molluscicidal activity and chemical constituents of seed oil and seed glycosides of B. aegyptiaca against Monacha cartusiana and determine the structure-activity relationship. Materials and methods: Two bioassay methods (residual film application and the leaf dipping technique) were used to evaluate the toxicity effect of the seed oil and glycosides, in concentrations of 1.000, 0.500, 0.250 and 0.125%. The seed oil was analysed by GC/MS. Acid hydrolysis and chromatographic separation were used to study the seed saponins. Results: The bioassay of B. aegyptiaca against the land snail, M. cartusiana, indicated the activity of the seed oil and the high activity of the seed saponins. The seed glycosides gave 30.0, 53.3, 73.0 and 73.3% mortality for concentrations of 0.125, 0.250, 0.500 and 1.00%, respectively. The LC(50) values were 0.335 and 0.256%, respectively. The seed oil was analysed by GC/MS. Acid hydrolysis of the seed saponins gave a mixture of diosgenin, yamogenin and 3,5-spirostadiene. Discussion and conclusion: To study the structure-activity relationship, a triterpenoidal saponin and a triterpenoidal saponins rich extract (of Zygophyllum coccenum) were proven to be inactive. Thus, the activity is associated with the steroidal, not triterpenoidal saponins. Moreover, a spirostane aglycone without sugar moiety, was found to be inactive and attained the activity by glycosidation.     

胡芦巴研究新进展

胡芦巴（Trigonella foenum-graecum L.）又名苦豆（《饮膳正要》）、芦巴（《本草原始》）、胡巴（《本草求真》）、季豆（《东北药植志》）、小木夏、香豆子（《新疆中草药手册》）.为豆科蝶形花亚科葫芦巴属一年生草本.《本草纲目》中记载,“胡芦巴苦温纯阳亦能人肾补命门……”.《回回药方》残卷中也包含有胡芦巴.现用于治疗肾脏虚冷、小腹冷痛、小肠疝气、寒湿脚气等.在国外多用作强壮、催欲、催乳、止咳、抗淋病、抗痢疾、抗天花、降胆固醇、降血糖等药剂,也可作化妆品.     

薯蓣皂苷元的制备及其抗甲亢活性研究

目的 考查薯蓣皂苷元对甲亢大鼠的活性。方法 穿山龙饮片用含1.5 mol·L^-1硫酸的75%乙醇水溶液在沸水浴中回流提取4.5 h,再经柱层析法分离、精制纯化得薯蓣皂苷元提取物,并进行结构表征。采用优甲乐灌胃法制作大鼠甲亢模型,并将大鼠随机分成正常对照组、甲亢模型组、甲巯咪唑治疗组、薯蓣皂苷元治疗组(低、中、高剂量),分别于给药21 d后测定大鼠血清中T₃、T₄及TSH值。结果 薯蓣皂苷元提取制备工艺正确适当,所得薯蓣皂苷元提取物经氢谱、碳谱、质谱和高效液相色谱表征确定为薯蓣皂苷元。与甲亢模型组比较,薯蓣皂苷元治疗组(低、中、高)血清中T₃、T₄和TSH值均有不同程度改善。结论 薯蓣皂苷元制备工艺合理可行,得率较高。薯蓣皂苷元可使甲亢大鼠的各项甲状腺功能血清值恢复正常,还可增加其体质量,功效与甲巯咪唑相似,值得进一步研究。     

薯蓣皂苷元衍生物的抗肿瘤活性研究

目的研究薯蓣皂苷元衍生物在体外的抗肿瘤活性。方法采用MTT法对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2及人慢性髓原白血病细胞株K562进行体外抗肿瘤活性试验。结果薯蓣皂苷元衍生物对4个肿瘤细胞株A375、A549、K562、HepG-2具有不同程度的抗肿瘤活性。结论绝大部分薯蓣皂苷元衍生物对4个肿瘤细胞株有较好的抗肿瘤活性,IC50值都低于30μmol.L-1。化合物22对细胞株A375的IC50=4.48μmol.L-1,化合物9、10对细胞株K562的IC50分别为2.51、2.38μmol.L-1;显示其抗肿瘤活性与对照化合物1-(3β-薯蓣皂苷元)-3-苄基咪唑溴盐相当。     

刺梨SOD口服液的制备及临床应用

目的：介绍刺梨 ＳＯＤ口服液的制备和治疗失眠的效果。方法：将刺梨原汁与苍术煎煮液混合调配;通过检测 ＳＯＤ活力控制质量,并据此考察稳定性; 对３４例失眠患者进行临床疗效观察。结果：样品放置１８ｍｏ未见显著质量改变;治疗失眠有效率为８８．２％。结论：本制剂具安全、稳定、疗效确切的特性,     

HPLC法测定金刚藤片中薯蓣皂苷元的含量

目的：建立高效液相色谱法测定金刚藤片中薯蓣皂苷元的含量，以评价其制剂的质量。方法：色谱柱为十八烷基键合硅胶柱（Kromasil，5μm，150×4．6mm）；以乙腈-水（90：10）为流动相；流速1．0ml／min；柱温：35C；检测波长为203nm。结果：薯蓣皂苷元的进样量在0．22～6．40／1g范围线性关系良好（r=0．9997，n=6）。平均回收率为97．83％（RSD=1．11％，n=6）。10批金刚藤片样品中薯蓣皂苷元的含量为0.143～0．308mg／片。结论：该方法操作简便，测定结果准确，重现性好，可用于金刚藤片巾暮辅囊菩元的会量测定．     

薯蓣总皂苷水解物中提取薯蓣皂苷元工艺研究

摘 要 目的：优选一种能高效、安全地从薯蓣总皂苷水解物中提取薯蓣皂苷元的工艺。方法: 以薯蓣皂苷元得率为指标,通过单因素试验对回流提取法、索氏提取法、超声提取法3种提取方法以及甲醇、乙醇、乙酸乙酯、石油醚、环己烷5种提取溶剂进行考察,采用正交试验法优化所选提取方法,确定最佳提取条件。结果: 以石油醚为溶剂,采用超声提取法,最佳提取条件为：50倍料液比,频率40 kHz,每次提取20 min,共3次。结论:超声法提取具有工艺周期短、效率高、能耗低、安全等优点,适合用于薯蓣皂苷元提取。     

In vitro and in vivo antidiabetic potential of extracts and a furostanol saponin from Balanites aegyptiaca

Context: Balanites aegyptiaca Del. (Zygophyllaceae) fruits are well-known antidiabetic drug in Egyptian folk medicine. Nevertheless, its mechanism of action is still unclear.

Objectives: Searching for the possible mechanisms of action of the plant and identification of its bioactive compounds.

Materials and methods: A bio-guided protocol based on the evaluation of α‐glucosidase (AG) and aldose reductase (AR) inhibitory activities was adopted to isolate the biologically active compounds from the methanol extract (MeEx). An in vivo antidiabetic study was conducted for the active extract, fraction and compound using streptozotocin-induced diabetic male albino Wistar rats at two dose levels (100 and 200?mg/kg.b/wt) for 2 weeks.

Results: Three compounds were isolated and identified: a sterol, (1) stigmasterol-3-O-β-d-glucopyranoside; a pregnane glucoside, (2) pregn-5-ene-3β,16β,20(R)-trio1-3-O-β-d-glucopyranoside; a furostanol saponin, (3) 26-(O-β-d-glucopyranosyl)-22-O-methylfurost-5-ene-3β,26-diol-3-O-β-d-glucopyranosyl-(1 → 4)-[α-l-rhamnopyranosyl-(1 → 2)]-β-d-glucopyranoside. Only compound 3 possessed significant AG and AR inhibitory activities (IC₅₀?=?3.12?±?0.17 and 1.04?±?0.02?μg/mL, respectively), while compounds 1 and 2 were inactive. The in vivo antidiabetic study revealed that MeEx and furostanol saponin 3 possessed significant activities at a dose of 200?mg/kg through reducing the fasting plasma glucose level by 46.14% and 51.39%, respectively, as well as reducing the total cholesterol by 24.44% and 31.90%, respectively. Compound 3 also caused increment in insulin and C-peptide levels by 63.56% and 65%, respectively.

Discussion and conclusions: We presented a scientific base for using Balanites aegyptiaca, and shed the light on one of its saponins, as an antidiabetic agent in fasting and postprandial hyperglycaemia along with the improvement of diabetic complications.     

HPLC测定骨骼风痛胶囊中薯蓣皂苷元的含量

目的建立骨骼风痛胶囊中薯蓣皂苷元的含量测定方法。方法采用HPLC,色谱柱为Hypersil ODS2（4.6mm×250mm,5μm）;流动相为甲醇-水（93∶7）;检测波长203nm。结果薯蓣皂苷元在0.7728～3.8640μg内与峰面积呈良好的线性关系,回归方程为Y=443254X＋18856,r=0.9991;平均回收率为97.87%,RSD为1.71%。结论本法可用于骨骼风痛胶囊的质量控制。     

气相色谱法测定菝葜中薯蓣皂苷元含量

目的　建立菝葜中薯蓣皂苷元的含量测定方法。方法　程序升温气相色谱法 ,CPSil 5CB熔融石英毛细管柱 ,FID检测器。结果　薯蓣皂苷元在 0 2 0～ 5 0 μg范围内具有良好的线性关系 ,r=0 9998,测定方法平均回收率为 97 2 0 %。 结论　本方法有较高的灵敏度和回收率 ,可用于菝葜中薯蓣皂苷元的含量测定。