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Objective:To explore the value of adrenocorticotrophic hormone (ACTH) stimulation in adrenal vein sampling (AVS) with its effect on the sampling success rate and lateralization determination.Methods:The clinical data of 54 patients with primary aldosteronism (PA) who underwent AVS in Nanjing Drum Tower Hospital from July 2018 to June 2020 were collected retrospectively. Blood samples from bilateral adrenal veins were collected simultaneously at baseline and after ACTH stimulation. The selectivity index (SI), lateralization index (LI), and relative aldosterone secretion index (RASI) were examined.Results:The concentration of serum cortisol level in left and right adrenal vein and peripheral vein increased significantly after ACTH stimulation ( P<0.001). SI of left adrenal vein increased from 18.00 (2.29, 20.29) to 34.76 (12.10, 46.86) , and the SI of right adrenal vein increased from 26.61(5.24, 31.85) to 28.40 (27.65, 56.05, P<0.001). The bilateral vein sampling success rate increased from 80%(43/54) to 93%(50/54). LI decreased from 2.85(1.78, 6.20) at baseline to 2.45(1.40, 6.10) after ACTH stimulation without significant difference( P>0.05). Eleven patients who identified unilateral secretion at baseline demonstrated bilateral after ACTH stimulation, and the RASI of these patients decreased from 0.50 (0.38, 1.25 ) to 0.37 (0.22, 0.84, P=0.019). Conclusion:ACTH stimulation significantly increased SI and the AVS success rate in patients with PA: ACTH stimulation decreased the relative aldosterone secretion in the dominant side of some patients with aldosterone producing adenoma, thus reduced the proportion of identified unilateral PA.
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A series of new aminomethyl derivatives of methyl-substituted asymmetrical curcumin mono-carbonyl was synthesizedand evaluated for their anticancer potential by means of cytotoxicity and selectivity determination against MCF-7,WiDr, Hela, A549, PLC/PRF/5, and Chang Liver cells lines using the methyl thiazolyl tetrazolium proliferation assaymethod. All the synthesized compounds (3a–f) exhibited high cytotoxic against WiDr cells lines, but only 3a–e hadhigh cytotoxic against MCF-7 cells lines, and only 3b showed high cytotoxic against HeLa, A549, and PLC/PRF/5 celllines. However, 3b and 3c exhibited high cytotoxic against Chang Liver (normal liver) cells lines. Further evaluationsshowed that compounds 3d, 3e, and 3f exhibited a potent and selective cytotoxic agent (IC50 = 5.70, 5.55, and 2.97µM) against WiDr (colorectal carcinoma) cells lines with selectivity index (SI) = 4.43, 2.69, and 2.04, respectively.The compounds performed better cytotoxic activity than curcumin and 5-fluorouracil (IC50 = 8.29 and >100 µM andSI = 1.28 and <1). So, compounds 3d, 3e, and 3f were potential as an anticancer agent for colorectal carcinoma andshould be further studied for investigating their mechanism of action and their effectivity in preclinical studies usingan animal model..
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Objective: To evaluate the antimicrobial, antioxidant, cytotoxicity and anticancer activity of fractions from Jatropha zeyheri roots and to explore the phytochemical profile of the most biologically active fraction. Methods: Fractions from Jatropha zeyheri ethyl acetate extract were investigated for antimicrobial activity against a plethora of pathogenic microorganisms of different origins. The cytotoxicity studies of fractions were evaluated in vitro using tetrazolium-based calorimetric assay against human dermal fibroblast, colon adenocarcinoma (Caco-2), breast cancer (MCF-7) and lung cancer (A547) cell lines. The anti-oxidant activity of fractions was determined in vitro against 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and chelation of iron (Fe
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Objective: To evaluate the antimicrobial, antioxidant, cytotoxicity and anticancer activity of fractions from Jatropha zeyheri roots and to explore the phytochemical profile of the most biologically active fraction. Methods: Fractions from Jatropha zeyheri ethyl acetate extract were investigated for antimicrobial activity against a plethora of pathogenic microorganisms of different origins. The cytotoxicity studies of fractions were evaluated in vitro using tetrazolium-based calorimetric assay against human dermal fibroblast, colon adenocarcinoma (Caco-2), breast cancer (MCF-7) and lung cancer (A547) cell lines. The anti-oxidant activity of fractions was determined in vitro against 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and chelation of iron (Fe2+). Gas chromatography mass spectrometry analysis was performed to detect phytochemical constituents in fraction with potent biological activity. Results: Fraction 2 of Jatropha zeyheri roots exhibited the lowest minimum inhibitory concentration of 40 μg/mL against Klebsiella pneumoniae and 80 μg/mL against Candida albicans, Staphylococcus aureus and Mycoplasma hominis. The fractions revealed some varying degrees of cytotoxicity against human dermal fibroblasts yielding LC50 values ranging from 28.96 to 166.52 μg/mL. Fraction 3 exhibited the highest selectivity index value of 2.08 against Klebsiella pneumoniae. Moreover, fraction 2 selectively inhibited the growth of Caco-2 with LC50 of 8.83 μg/mL, compared to other cancerous cell lines. Fraction 2 of Jatropha zeyheri further exhibited IC50 of 19.66, 22.63 and 1.82 μg/mL against DPPH, ABTS and Fe2+, respectively. Gas chromatography mass spectrometry analysis revealed the presence of cyclotetracosane (10.08%), 9-hexacosene (9.40%), hexadecanoic acid (3.90%), (Z)-9-octadecenamide (3.63%), octacosane (2.27%), 11-n-decylheneicosane (2.23%), ethyl vallesiachotamate (2.17%), heneicosanoic acid (2.10%), and octadecanoic acid (2.08%) in fraction 2 of Jatropha zeyheri. Conclusions: These identified compounds, particularly cyclotetracosane (hydrocarbon), may well explain the biological activity of fraction 2 of Jatropha zeyheri, which possesses higher biological activity than other fractions. These compounds can be further investigated for use in treating various bacterial and fungal opportunistic infections associated with HIV-AIDS and related cancers.
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Tragia brevipes and Tetradenia riparia have been widely used in traditional medicine. T. brevipes relief stomach pain and in treatment of rheumatism while T. riparia; heal chest pains, stomach-ache, malaria and act as antioxidant. However, scanty data exist on their potential anticancer activity. The total phenolic content was determined and anti-proliferative activity of the Methanol-Dichloromethane extract from the leaves evaluated against cancerous cell lines. The total phenolic content of the plants extract was determined using an UV visual spectrophotometer at 765 nm. The 3- (4-5-dimethyl-2-thiazoly)-2, 5-diphenyltetrazolium bromide (MTT) cell proliferation bioassay was used to test for anti-proliferative activity on Hela (cervical), DU145 (prostrate) and HCC (breast) cancer cell lines and Vero (normal) cell. T. brevipes and T. riparia had a phenolic concentration of 30.44 and 20.25 µg/ml, respectively. Both plants showed anti-proliferative activity on cancer cells with the most inhibited being DU145 with an IC50 of 29.67 ± 4.60 µg/ml for T. brevipes and 11.45 ± 0.87 µg/ml for T. riparia. The standard 5 Fluorouracil had an IC50 of 5.04 ± 4.12 µg/ml on DU145. T. riparia had the highest antiproliferative activity of 65.54 ± 16.85 µg/ml on Hela cells and 62.84 ± 1.10 µg/ml on HCC. T. brevipes had an IC50 of 661.11 ± 15. 12 µg/ml on Hela cells and 703.09 ± 18.35 µg/ml on HCC. Extracts from both plants were highly selective on DU145 cancer cells with a selectivity index (SI) of 21.62 for T. brevipes and 7.88 for T. riparia. Methanol-Dichloromethane extracts from T. brevipes and T. riparia exert anti-proliferative activity, however, the active compound (s) and the mechanisms of anti-proliferative action need to be investigated further.
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ResumenLas plantas carnívoras del género Utricularia, capturan un amplio ámbito de organismos acuáticos. La mayoría se desarrollan en ambientes con carencias de nutrientes y tienen la capacidad de cambiar las condiciones de su microambiente. El objetivo de la presente investigación fue estudiar la selectividad, en la captura de zooplancton por Utricularia foliosa en la Ciénaga de Paredes; entre febrero y noviembre 2014. Se determinó si existe selección en los recursos alimentarios de la planta con el índice de Czekanowski y el grado de selección, a través de los índices de Savage e Ivlev. Se estableció la relación existente entre los patrones de captura y selección del zooplancton, con variables físicoquímicas y la disponibilidad de nutrientes en la Ciénaga. En nuestros resultados, el índice de Czekanowski evidenció selección, en los recursos alimentarios de la planta, durante todo el pulso de inundación, con valores entre 0.28 y 0.41. Se encontró selección positiva significativa, con el índice de Savage, para los géneros Lecane sp., Alona sp., Ceriodaphnia sp., y Bosmina sp. (p < 0.05). Se obtuvieron resultados similares, con el índice de Ivlev. La intensidad en la selección de los géneros varió entre periodos hidrológicos y por periodos de aguas altas y bajas. Se identificó que los cambios en la concentración de amoniaco y nitrato, además de la variación en la conductividad eléctrica de la ciénaga influencian la captura que realiza U. foliosa. Este es el primer trabajo que permite dar un acercamiento al entendimiento de la selección de recursos alimentarios dentro de la especie a través de índices de selectividad y uno de los pocos para el género.
Abstract:Utricularia is a genus of carnivorous plants that capture a wide range of aquatic organisms. Most of these plants grow in environments with nutrients deficiency and have the ability to change the conditions of their microenvironment. The aim of this research was to study the selectivity in the zooplankton capture by Utricularia foliosa in the Ciénaga de Paredes. Our study was undertaken between February and November, 2014. We tried to determine if there is selection in the plant's food resources by the Czekanowski's index, and the selection degree by the Savage and Ivlev's indexes. Additionally, we studied the possible relation between the patterns of zooplankton capture and selection, with physicochemical variables in the swamp. The Czekanowski's index showed a food selection in plant resources throughout the flood pulse, with values between 0.28 and 0.41. We also found a significant positive selection with Savage's index for Lecane sp., Alona sp., Ceriodaphnia sp., and Bosmina sp. (p < 0.05); similar results were obtained with Ivlev's index. The intensity in the selection of each captured genus varied significantly between hydrological periods and between high and low water levels in the swamp. It was possible to identify some changes in the ammonia and nitrate concentration and some variability in the electric conductivity of the swamp, which influenced the captures made by U. foliosa. This is the first paper that allows an approach to understand the selection of food resources for the species, using a selectivity index, and one of the few for the genus. Rev. Biol. Trop. 64 (3): 1297-1310. Epub 2016 September 01.
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Animals , Zooplankton/classification , Lamiales/physiology , Seasons , Temperature , Zooplankton/physiology , Cluster Analysis , Colombia , Statistics, Nonparametric , Rivers/chemistry , Food PreferencesABSTRACT
Hydrazones are nowadays considered to be good candidates for various pharmaceutical applications. Here, we have synthesized two series of hydrazones: salicylhydrazones (GS1-4) and p-tosylhydrazones (GT1-4) from S- (+)-carvone and three aryketones with good yields (57-91%). Molecules were characterized by elemental analyses; TLC, NMR 1H, NMR 13C and MS. Submitted, in vitro, to their antiparasitic testing on Trypanosoma brucei brucei, and toxicity on Artemia salina Leach, all compounds except GT2 showed significant antitrypanosomal activity IC50 ranging from 1 to 34 micromolar (μM). Among them, 2-acetynaphthalene salicylhydrazone GS4 (IC50 = 1.97 ± 0.42 μM) and 7-methoxy-1-tetralone p-tosylhydrazone GT3 (IC50 =7.98 ± 1.65 μM) exhibited good trypanocidal activity and the other are moderates on parasite; when the compounds GS1, GT3 and GT4 presented toxic activity on larvae. In agreement to their selectivity index, which is greater than 1 (SI > 1), products turn out quite selective on the parasite: a series of salicylhydrazones revealed more selective (SI ≥ 11), especially GS4 (SI = 157) than the series of p-tosylhydrazones showed 1 ≤ SI ≤ 22. The synthesized compounds clearly displayed significant selective pharmaceutical activities on the parasite tested. Compounds developing could open promising route to news drug-candidates.
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It is well known that proteins present in the primary urine are reabsorbed in the renal proximal tubules, and that this reabsorption is mediated via the megalincubilin complex and the neonatal Fcgamma receptor. However, the reabsorption is also thought to be influenced by an electrostatic interaction between protein molecules and the microvilli of the renal proximal tubules. By analyzing the charge diversity of urinary IgG, we showed that this reabsorption process occurs in a cationic charge-preferential manner. The charge-selective molecular sieving function of the glomerular capillary walls has long been a target of research since Brenner et al. demonstrated the existence of this function by a differential clearance study by using the anionic dextran sulfate polymer. However, conclusive evidence was not obtained when the study was performed using differential clearance of serum proteins. We noted that immunoglobulin (Ig) A and IgG have similar molecular sizes but distinct molecular isoelectric points. Therefore, we studied the differential clearance of these serum proteins (clearance IgA/ clearance IgG) in podocyte diseases and glomerulonephritis. In addition, we studied this differential clearance in patients with Dent disease rather than in normal subjects because the glomerular sieving function is considered to be normal in subjects with Dent disease. Our results clearly showed that the charge-selective barrier is operational in Dent disease, impaired in podocyte disease, and lacking in glomerulonephritis.
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Humans , Blood Proteins , Capillaries , Child Health , Dent Disease , Dextran Sulfate , Glomerulonephritis , Immunoglobulin A , Immunoglobulin G , Immunoglobulins , Isoelectric Point , Microvilli , Nephritis , Podocytes , Polymers , ProteinuriaABSTRACT
Aim: Antiplasmodial potential of traditional medicinal plant Thlaspi arvense against Plasmodium falciparum in vitro has been evaluated. Cytotoxicity of plant extract against HeLa cell lines and normal fibroblasts has also been observed. Place and Duration of the Study: Department of Zoology, Panjab University, Chandigarh, India, between May 2013 to April 2014. Materials and Methods: Ethanolic whole plant extract of Thlaspi arvense (EWETA) was analyzed for its phytochemical constituents. In vitro cytotoxicity was determined colorimetrically by MTT assay. WHO protocol, based on assessment of schizont maturation inhibition, was employed for the evaluation of in vitro antiplasmodial activity of plant extract. Results: Phytochemical screening of EWETA revealed the presence of diterpenes, triterpenes, steroids, anthraquinones and phytosterols. EWETA was observed to inhibit schizont maturation of both chloroquine-sensitive (MRC-2) and resistant (RKL-9) strains of P. falciparum with IC50<5μg/ml and =5μg/ml respectively. The extract was revealed to be safe against both HeLa cells and normal fibroblasts with CC50>1000μg/ml. Selectivity index for Thlaspi arvense was calculated to be >200 and =200 both for chloroquine sensitive and chloroquine-resistant strains of P. falciparum with both HeLa and normal fibroblasts. Conclusion: Plant extract possesses considerable in vitro antimalarial activity with high selectivity index (SI>10) pointing field pennycress to be an active antimalarial. Hence, present study provides scientific evidence for traditional usage of the plant as an antipyretic agent.
Subject(s)
Antimalarials/pharmacology , Humans , India , Malaria, Falciparum/drug therapy , Medicine, Traditional , Microbial Sensitivity Tests , Microbial Viability/drug effects , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/toxicity , Plasmodium falciparum/drug effects , ThlaspiABSTRACT
Infusions of Aspidosperma nitidum (Apocynaceae) wood bark are used to treat fever and malaria in the Amazon Region. Several species of this family are known to possess indole alkaloids and other classes of secondary metabolites, whereas terpenoids, an inositol and the indole alkaloids harmane-3 acid and braznitidumine have been described in A. nitidum . In the present study, extracts from the wood bark, leaves and branches of this species were prepared for assays against malaria parasites and cytotoxicity testing using human hepatoma and normal monkey kidney cells. The wood bark extracts were active against Plasmodium falciparum and showed a low cytotoxicity in vitro, whereas the leaf and branch extracts and the pure alkaloid braznitidumine were inactive. A crude methanol extract was subjected to acid-base fractionation aimed at obtaining alkaloid-rich fractions, which were active at low concentrations against P. falciparum and in mice infected with and sensitive Plasmodium berghei parasites. Our data validate the antimalarial usefulness of A. nitidum wood bark, a remedy that can most likely help to control malaria. However, the molecules responsible for this antimalarial activity have not yet been identified. Considering their high selectivity index, the alkaloid-rich fractions from the plant bark might be useful in the development of new antimalarials.
Subject(s)
Animals , Humans , Mice , Antimalarials/pharmacology , Aspidosperma/chemistry , Plant Bark/chemistry , Plant Extracts/pharmacology , Plasmodium berghei/drug effects , Plasmodium falciparum/drug effects , Antimalarials/isolation & purification , Malaria/drug therapy , Malaria/parasitology , Parasitic Sensitivity Tests , Plant Extracts/isolation & purificationABSTRACT
This work is focused on the synthesis and characterization of a series of N(4)- substituted thiosemicarbazones and the evaluation of their in-vitro anti-trypanosomal activity and toxicity. A series of thiosemicarbazones (1-4) and N(4)-phenyl-3-thiosemicarbazones (5-8) have been synthesized on R-(-)carvone, acetophenone, 4’-methylacetophenone and benzophenone by condensation reaction with good yields. All compounds were characterized by spectrometrical analysis methods infrared IR, nuclear magnetic resonance NMR (1H &13C) and mass spectrometry MS, confirming their structures respectively, and were evaluated for their invitro parasitic activity against the bloodstream form of the strain 427 of Trypanosoma brucei brucei using the “LILIT, Alamar Blue” method (Baltzet al., 1985; Hirumi et al., 1994; Räz et al.,1997). Their toxicity against brine shrimp larvae (Artemia salina Leach) was studied, according to the method of Michael et al. (1956) resumed byVanhaecke et al. (1981) and bySleet and Brendel (1983). Some of them have exhibited a strong trypanocidal activity, especially compounds 8, 3, 1 and 4 with their half-inhibitory concentrations (IC50) values equal to 8.48, 8.73, 39.71 and 67.17 micro-molar (μM) respectively. Except compounds 1 and 4whose half-lethal concentration (LC50) values were20.58 and 33.72 μM respectively and then toxics, all synthesized compounds showed negligible toxicity against Artemia salinaL. (LC50> 280 μM) and good selectivity (S) (SI “index” ≤1).
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Background and objectives: In integrated vector management programmes, major emphasis is given on the application of biocontrol agents. In the present study, the hemipteran water bug, Laccotrephes griseus (Hemiptera: Nepidae) was evaluated to establish its functional response against the immature Culex quinquefasciatus Say in the laboratory. Methods: Adult water bugs (L. griseus) were collected from different ponds in Bankura, West Bengal, India. Predation rate was determined in semi-field conditions. Functional response, regression equation analysis and rate of predation were also determined in the presence of an alternative prey. Results: The long-term predation experiment (up to 30 days) revealed that L. griseus is a very good predator of mosquito larvae. The functional curve analysis of L. griseus exhibited a Type II functional response. Their handling times and coefficient of attack rates were 29.37 min and 2.17 respectively. Regression equations showed that consumption rate was directly proportional to prey and predator densities and inversely proportional to the search area. The selectivity index, niche width and food breadth were also determined. Interpretation and conclusion: The present study revealed that L. griseus can consume a good number of mosquito larvae in the laboratory conditions. The long-term bioassay also indicates their predatory response against mosquito larvae in the semi-field conditions. The result of selectivity index, niche width and food breadth were also highest for Cx. quinquefasciatus. In these respects, the water bugs L. griseus are indicative of their release in the aquatic habitat where Cx. quinquefasciatus is the most dominant mosquito species.