scholarly journals Antibacterial and bacteriostatic potential of coelomic fluid and body paste of Pheretima posthuma (Vaillant, 1868) (Clitellata, Megascolecidae) against ampicillin resistant clinical bacterial isolates

2023 ◽  
Vol 83 ◽  
Author(s):  
M. Hussain ◽  
I. Liaqat ◽  
N. M. Ali ◽  
N. Arshad ◽  
U. Hanif ◽  
...  
Keyword(s):  
Growth Curves ◽  
Clinical Isolates ◽  
Coelomic Fluid ◽  
Drug Manufacturing ◽  
Pharmaceutical Industries ◽  
Bioactive Potential ◽  
Novel Drug ◽  
Dose Dependent ◽  
Different Doses ◽  
Positive Controls

Abstract Pheretima posthuma (Vaillant, 1868), a native earthworm of Pakistan and Southeast Asia, has wide utilization in vermicomposting and bioremediation process. In this study, P. posthuma coelomic fluid (PCF) and body paste (PBP) was evaluated as antibacterial agent against ampicillin (AMP) resistant five Gram positive and four Gram negative clinical isolates. The antibacterial effect of different doses (i.e. 25-100 µg/ml) of PCF and PBP along with AMP and azithromycin (AZM) (negative and positive controls, respectively) were observed through disc diffusion and micro-dilution methods. All nine clinical isolates were noticed as AMP resistant and AZM sensitive. Antibacterial effects of PCF and PBP were dose dependent and zone of inhibitions (ZI) against all clinical isolates were between 23.4 ± 0.92 to 0 ± 00 mm. The sensitivity profile of PCF and PBP against clinical isolates was noticed as 44.44 and 55.56%, respectively. Both PCF and PBP showed bacteriostatic (BTS) action against S. aureus, S. pyogenes, K. pneumonia, N. gonorrhoeae. Moreover, the cumulative BTS potential of PCF and PBP against all isolates was 66.67 and 55.56%, respectively. The MICs of PCF and PBP were ranged from 50-200 µg/ml against selected isolates. The bacterial growth curves indicated that PCF and PBP inhibited the growth of all isolates at their specific MIC concentrations. However, PBP has better antibacterial potential compared to PCF against selected isolates. Therefore, it is concluded that both PCF and PBP of P. posthuma possess antibacterial and BTS potential against ampicillin resistant clinical isolates. This organism might be considered as a second choice of antibacterial agents and can further be utilized in pharmaceutical industries for novel drug manufacturing by prospecting bioactive potential agents.

Melatonin actions in the heart; more than a hormone

2018 ◽  
Vol 1 (1) ◽  
pp. 21-26 ◽  
Author(s):  
Darío Acuña-Castroviejo ◽  
Maria T Noguiera-Navarro ◽  
Russel J Reiter ◽  
Germaine Escames
Keyword(s):  
Cell Membranes ◽  
Myocardial Cell ◽  
Rat Tissues ◽  
Dependent Manner ◽  
Broad Distribution ◽  
Multiple Organs ◽  
High Doses ◽  
Extrapineal Melatonin ◽  
Dose Dependent ◽  
Different Doses

Due to the broad distribution of extrapineal melatonin in multiple organs and tissues, we analyzed the presence and subcellular distribution of the indoleamine in the heart of rats. Groups of sham-operated and pinealectomized rats were sacrificed at different times along the day, and the melatonin content in myocardial cell membranes, cytosol, nuclei and mitochondria, were measured. Other groups of control animals were treated with different doses of melatonin to monitor its intracellular distribution. The results show that melatonin levels in the cell membrane, cytosol, nucleus, and mitochondria vary along the day, without showing a circadian rhythm. Pinealectomized animals trend to show higher values than sham-operated rats. Exogenous administration of melatonin yields its accumulation in a dose-dependent manner in all subcellular compartments analyzed, with maximal concentrations found in cell membranes at doses of 200 mg/kg bw melatonin. Interestingly, at dose of 40 mg/kg b.w, maximal concentration of melatonin was reached in the nucleus and mitochondrion. The results confirm previous data in other rat tissues including liver and brain, and support that melatonin is not uniformly distributed in the cell, whereas high doses of melatonin may be required for therapeutic purposes.

scholarly journals Ketamine—50 years in use: from anesthesia to rapid antidepressant effects and neurobiological mechanisms

2021 ◽  
Vol 73 (2) ◽  
pp. 323-345
Author(s):  
Samuel Kohtala
Keyword(s):  
Traumatic Stress ◽  
Molecular Mechanisms ◽  
Post Traumatic Stress ◽  
Active Metabolites ◽  
The Past ◽  
Antidepressant Effects ◽  
Post Traumatic ◽  
Pharmacologically Active ◽  
Dose Dependent ◽  
Different Doses

AbstractOver the past 50 years, ketamine has solidified its position in both human and veterinary medicine as an important anesthetic with many uses. More recently, ketamine has been studied and used for several new indications, ranging from chronic pain to drug addiction and post-traumatic stress disorder. The discovery of the rapid-acting antidepressant effects of ketamine has resulted in a surge of interest towards understanding the precise mechanisms driving its effects. Indeed, ketamine may have had the largest impact for advancements in the research and treatment of psychiatric disorders in the past few decades. While intense research efforts have been aimed towards uncovering the molecular targets underlying ketamine’s effects in treating depression, the underlying neurobiological mechanisms remain elusive. These efforts are made more difficult by ketamine’s complex dose-dependent effects on molecular mechanisms, multiple pharmacologically active metabolites, and a mechanism of action associated with the facilitation of synaptic plasticity. This review aims to provide a brief overview of the different uses of ketamine, with an emphasis on examining ketamine’s rapid antidepressant effects spanning molecular, cellular, and network levels. Another focus of the review is to offer a perspective on studies related to the different doses of ketamine used in antidepressant research. Finally, the review discusses some of the latest hypotheses concerning ketamine’s action.

scholarly journals Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Anton Lindberg ◽  
Ryosuke Arakawa ◽  
Tsuyoshi Nogami ◽  
Sangram Nag ◽  
Magnus Schou ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Specific Binding ◽  
Occipital Cortex ◽  
Intrinsic Activity ◽  
High Affinity ◽  
G Protein Coupled ◽  
Dose Dependent ◽  
The Brain ◽  
Agonist Affinity States ◽  
Different Doses

Abstract Background Over the last decade, a few radioligands have been developed for PET imaging of brain 5-HT1B receptors. The 5-HT1B receptor is a G-protein-coupled receptor (GPCR) that exists in two different agonist affinity states. An agonist ligand is expected to be more sensitive towards competition from another agonist, such as endogenous 5-HT, than an antagonist ligand. It is of interest to know whether the intrinsic activity of a PET radioligand for the 5-HT1B receptor impacts on its ability to detect changes in endogenous synaptic 5-HT density. Three high-affinity 11C-labeled 5-HT1B PET radioligands with differing intrinsic activity were applied to PET measurements in cynomolgus monkey to evaluate their sensitivity to be displaced within the brain by endogenous 5-HT. For these experiments, fenfluramine was pre-administered at two different doses (1.0 and 5.0 mg/kg, i.v.) to induce synaptic 5-HT release. Results A dose-dependent response to fenfluramine was detected for all three radioligands. At the highest dose of fenfluramine (5.0 mg/kg, i.v.), reductions in specific binding in the occipital cortex increased with radioligand agonist efficacy, reaching 61% for [11C]3. The most antagonistic radioligand showed the lowest reduction in specific binding. Conclusions Three 5-HT1B PET radioligands were identified with differing intrinsic activity that could be used in imaging high- and low-affinity states of 5-HT1B receptors using PET. From this limited study, radioligand sensitivity to endogenous 5-HT appears to depend on agonist efficacy. More extensive studies are required to substantiate this suggestion.

scholarly journals Effect of erythritol and xylitol on Streptococcus pyogenes causing peritonsillar abscesses

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Siiri Kõljalg ◽  
Risto Vaikjärv ◽  
Imbi Smidt ◽  
Tiiu Rööp ◽  
Anirikh Chakrabarti ◽  
...  
Keyword(s):  
Streptococcus Pyogenes ◽  
Bacterial Growth ◽  
Growth Curves ◽  
Culture Collection ◽  
Exponential Phase ◽  
Clinical Isolates ◽  
Growth Inhibitors ◽  
Throat Culture ◽  
Potent Growth

AbstractPolyols are effective against caries-causing streptococci but the effect on oropharynx-derived pyogenic streptococci is not well characterised. We aimed to study the effect of erythritol (ERY) and xylitol (XYL) against Streptococcus pyogenes isolated from peritonsillar abscesses (PTA). We used 31 clinical isolates and 5 throat culture collection strains. Inhibition of bacterial growth by polyols at 2.5%, 5% and 10% concentrations was studied and the results were scored. Amylase levels in PTA pus were compared to polyol effectivity scores (PES). Growth curves of four S. pyogenes isolates were analysed. Our study showed that XYL was more effective than ERY inhibiting 71–97% and 48–84% of isolates, respectively, depending of concentrations. 48% of clinical and all throat strains were inhibited by polyols in all concentrations (PES 3). PES was negative or zero in 26% of the isolates in the presence of ERY and in 19% of XYL. ERY enhanced the growth of S. pyogenes isolated from pus with high amylase levels. Polyols in all concentrations inhibited the growth in exponential phase. In conclusion, ERY and XYL are potent growth inhibitors of S. pyogenes isolated from PTA. Therefore, ERY and XYL may have potential in preventing PTA in the patients with frequent tonsillitis episodes.

scholarly journals CTRP9 protects against MIA-induced inflammation and knee cartilage damage by deactivating the MAPK/NF-κB pathway in rats with osteoarthritis

2020 ◽  
Vol 15 (1) ◽  
pp. 971-980
Author(s):  
Shicheng Zheng ◽  
Jing Ren ◽  
Sihai Gong ◽  
Feng Qiao ◽  
Jinlong He
Keyword(s):  
Synovial Fluid ◽  
Nuclear Factor Kappa B ◽  
Cartilage Damage ◽  
Cartilage Tissue ◽  
Enzyme Linked Immunosorbent Assay ◽  
Nuclear Factor ◽  
Knee Cartilage ◽  
Monosodium Iodoacetate ◽  
Dose Dependent ◽  
Different Doses

AbstractC1q/TNF-related protein 9 (CTRP9), the closest paralog of adiponectin, has been reported to protect against inflammation-related diseases. However, its role in regulating osteoarthritis (OA) has not been fully elucidated. First, a rat model of OA was generated. Furthermore, rats with OA were injected with different doses of recombinant CTRP9 protein (rCTRP9), and the knee cartilage damage was evaluated. Finally, the phosphorylation of p38 and the secretion of matrix metalloproteinases (MMPs) were detected by Western blotting and enzyme-linked immunosorbent assay. Results revealed that CTRP9 was highly expressed in adipose tissue, followed by skeletal muscle and cartilage tissue, and less expressed in liver, kidney and lung. Moreover, the expression of CTRP9 significantly decreased in the monosodium iodoacetate (MIA) group in the knee cartilage and knee synovial fluid, and the contents of interleukin-1β (IL-1β) and IL-6 significantly increased in knee synovial fluid. In addition, rCTRP9 alleviated MIA-induced inflammation, oxidative stress and knee cartilage damage in a dose-dependent way. In addition, rCTRP9 could attenuate the expression of p38MAPK and p-p38 and suppress the expression of nuclear factor-kappa B (NF-κB), p65 and MMPs. Collectively, the results of the present study suggested that CTRP9 alleviates the inflammation of MIA-induced OA through deactivating p38MAPK and NF-κB signaling pathways in rats.

Histopathological changes in the liver and kidney tissues of Wistar albino rat exposed to fenitrothion

2008 ◽  
Vol 24 (9) ◽  
pp. 581-586 ◽  
Author(s):  
S Afshar ◽  
AA Farshid ◽  
R Heidari ◽  
M Ilkhanipour
Keyword(s):  
Control Group ◽  
Histopathological Changes ◽  
Albino Rat ◽  
Hydropic Degeneration ◽  
Leukocytic Infiltration ◽  
Male Wistar Rats ◽  
Liver And Kidney ◽  
Dose Dependent ◽  
Significant Injury ◽  
Different Doses

The aim of this study was to investigate the dose-related effects of fenitrothion (FNT) on the liver and kidney. The study was conducted on 8-week-old male Wistar rats that were divided into four groups (three experimental groups and one control group) and were treated orally with different doses (25, 50, 100 mg/kg) of FNT for 28 consecutive days. After treatment, the rats were anesthetized with ether and liver and kidney samples were taken for histological studies. The results showed that the histopathological changes in the liver were mainly represented by parenchymatous degeneration of hepatocytes with mild necrosis, leukocytic infiltration in the portal area, severe congestion, and hemorrhage. These changes were dose dependent. Marked tubular dilation, hydropic degeneration in tubular epithelium, moderate congestion, and hemorrhage in the cortical and medulla part of the kidney were recorded. Histopathologic examination of the liver and kidney indicated a significant injury only in rats receiving 100 mg/kg FNT.

scholarly journals Pyrrolizidine Alkaloid-Induced Hepatotoxicity Associated with the Formation of Reactive Metabolite-Derived Pyrrole–Protein Adducts

Toxins ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 723
Author(s):  
Jiang Ma ◽  
Mi Li ◽  
Na Li ◽  
Wood Yee Chan ◽  
Ge Lin
Keyword(s):  
Natural Products ◽  
Pyrrolizidine Alkaloids ◽  
Pyrrolizidine Alkaloid ◽  
Protein Adducts ◽  
Dependent Manner ◽  
Histological Changes ◽  
Histological Results ◽  
Dose Dependent ◽  
Different Doses ◽  
Alt Activity

Pyrrolizidine alkaloids (PAs) with 1,2-unsaturated necine base are hepatotoxic phytotoxins. Acute PA intoxication is initiated by the formation of adducts between PA-derived reactive pyrrolic metabolites with cellular proteins. The present study aimed to investigate the correlation between the formation of hepatic pyrrole–protein adducts and occurrence of PA-induced liver injury (PA-ILI), and to further explore the use of such adducts for rapidly screening the hepatotoxic potency of natural products which contain PAs. Aqueous extracts of Crotalaria sessiliflora (containing one PA: monocrotaline) and Gynura japonica (containing two PAs: senecionine and seneciphylline) were orally administered to rats at different doses for 24 h to investigate PA-ILI. Serum alanine aminotransferase (ALT) activity, hepatic glutathione (GSH) level, and liver histological changes of the treated rats were evaluated to assess the severity of PA-ILI. The levels of pyrrole–protein adducts formed in the rats’ livers were determined by a well-established spectrophotometric method. The biological and histological results showed a dose-dependent hepatotoxicity with significantly different toxic severity among groups of rats treated with herbal extracts containing different PAs. Both serum ALT activity and the amount of hepatic pyrrole–protein adducts increased in a dose-dependent manner. Moreover, the elevation of ALT activity correlated well with the formation of hepatic pyrrole–protein adducts, regardless of the structures of different PAs. The findings revealed that the formation of hepatic pyrrole–protein adducts—which directly correlated with the elevation of serum ALT activity—was a common insult leading to PA-ILI, suggesting a potential for using pyrrole–protein adducts to screen hepatotoxicity and rank PA-containing natural products, which generally contain multiple PAs with different structures.

scholarly journals Genotoxic and Histopathological Effects of Chlorpyrifos on African Catfish, C. gariepinus and Ameliorative Potentials of Ackee Apple, blighia sapida Seed

2018 ◽  
Vol 6 (1) ◽  
pp. 1 ◽  
Author(s):  
Oluyinka Iyiolai ◽  
A. A. Adeagbo ◽  
W. S. Weliange ◽  
S. I. Abdulkareem ◽  
Anifowoshe T. Abass ◽  
...  
Keyword(s):  
Chronic Exposure ◽  
Clarias Gariepinus ◽  
Aquatic Organisms ◽  
Acute Exposure ◽  
Histopathological Analysis ◽  
African Catfish ◽  
Dependent Manner ◽  
Dose Dependent ◽  
Histopathological Effects ◽  
Positive Controls

Chlorpyrifos (CPF) is a very toxic pesticide commonly used for controlling agriculturally important pests. The present study investigates DNA damaging effects of CPF on Clarias gariepinus was assessed using genetic assays. Fish were exposed to varying concentrations of CPF (100ppm, 200ppm and 300ppm) at 96 hours (acute exposure). LC50 of the pesticide was found to be 120ppm and one-tenth of the LC50 (12ppm) was taken for the chronic exposure. Distilled water and colchicine were used as negative and positive controls respectively. After 28 days of chronic exposure, fish were fed with inclusion of B. sapida seed (powder) for 14 days. Liver and gills of the fish were removed following 96h exposure, days 7, 14 and 28 of the chronic exposure as well as after the period of amelioration (14 days) for CA assay and histopathological analysis. The results of CA assay showed statistically significant (p ˂ 0.05) increase in CA in a dose-dependent manner for all the exposed groups after acute exposure and time dependent after chronic exposure. Also, this study showed that CPF can potentially induce genotoxic and histopathological changes in fish and other aquatic organisms.

scholarly journals In vivo antiplasmodial evaluation of methanol mesocarp extract of Citrillus lanatus in Plasmodium berghei berghei infected mice

2021 ◽  
Vol 10 (2) ◽  
pp. 84-88
Author(s):  
EO Ettebong ◽  
◽  
GB Inyang ◽  
AIL Bassey ◽  
JA Udobang ◽  
...  
Keyword(s):  
Plasmodium Berghei ◽  
Survival Times ◽  
Natural Medicine ◽  
The Mean ◽  
Dose Dependent ◽  
Positive Controls

Aim: The aim of this study was to evaluate the in vivo antiplasmodial activities of the methanol mesocarp extract of Citrillus lanatus in mice infected with Plasmodium berghei berghei. Materials and Methods: The extract (125, 250, and 500 mg/kg) was administered orally to mice and were assessed in suppressive, repository and curative tests using Chloroquine (5 mg/kg) and Pyrimethamine (1.2 mg/kg) as positive controls. Results: A dose-dependent, significant (p < 0.001) antiplasmodial effect was recorded in the suppressive test relative to control. The extract also demonstrated a dose-dependent, significant (p < 0.01 – 0.001) prophylactic and curative effects when compared to the controls. These antiplasmodial effects of the extract compared favourably with those of the standard drugs. The extract in addition, increased the mean survival times of the infected mice. Conclusions: The methanol mesocarp extract of C. lanatus possesses antiplasmodial activities, thereby corroborating its use in natural medicine in the treatment of malaria.

scholarly journals Biochemical profile and bioactive potential of wild folk medicinal plants of Zygophyllaceae from Balochistan, Pakistan

2020 ◽  
Author(s):  
Alia Ahmed ◽  
Amjad Hameed ◽  
Shazia Saeed
Keyword(s):  
Medicinal Plants ◽  
Total Phenolic ◽  
Arid Zones ◽  
Standard Drug ◽  
Aerial Parts ◽  
Fruit Samples ◽  
Pharmaceutical Industries ◽  
Inhibitory Potential ◽  
Bioactive Potential ◽  
Semi Arid

AbstractRecent focus is on analysis of biological activities of extracts from plant species. Zygophyllaceae is exceedingly important angiosperm family with many taxa being used in folk medicines widely dispersed in arid and semi-arid zones of Balochistan, Pakistan. Only a small proportion of them have been scientifically analyzed and many species are nearly facing extinction. Therefore present investigation explores the biochemical and bioactive potential of fourteen folk medicinal plants usually used for treatments of different ailments. Fresh aerial parts of nine taxa and two fruit samples were collected from plants growing in arid and semi-arid zones of Balochistan and analyzed for enzymatic, non-enzymatic and other biochemical activities. Higher phytochemical activities were detected in the aerial parts. Superoxide dismutase was detected maximum in Fagonia indica, (184.7±5.17 units/g), ascorbate peroxidase in Tribulus longipetalus subsp. longipetalus (947.5±12.5 Units/g), catalase and peroxidase was higher in Peganum harmala (555.0±5.0 and 2597.8±0.4 units/g respectively). Maximum esterase and alpha amylase activity was found in Zygophyllum fabago (14.3±0.44 and 140±18.8 mg/g respectively). Flavonoid content was high in T. longipetalus subsp. longipetalus (666.1±49 μg/ml). The highest total phenolic content and tannin was revealed in F. olivieri (72125±425 and 37050±1900 μM/g. respectively). Highest value of ascorbic acid was depicted in F. bruguieri var. rechingeri (448±1.5 μg/g). Total soluble Proteins and reducing sugars were detected higher in P. harmala (372.3±54 and 5.9±0.1 mg/g respectively). Maximum total antioxidant capacity (TAC) was depicted in Z. simplex (16.9±0.01 μM/g). Pigment analysis exhibited the high value of lycopene and total carotenoids in T. terrestris (7.44±0.2 and 35.5±0.0 mg/g respectively). Chlorophyll a, b and total chlorophyll content was found maximum in T. longipetalus subsp. pterophorus (549.1±9.9, 154.3±10 and 703.4±20.2 ug/g respectively). All taxa exhibited anti-inflammatory activity as well as anti-diabetic inhibitory potential. Seed extracts of Zygophyllum eurypterum (96%) exhibited highest inhibitory potential, along with twelve other taxa of Zygophyllaceae indicated (96-76%) activity when compared with the standard drug diclofenac sodium (79%). Seeds of T. longipetalus subsp. longipetalus (85%) exhibited the highest anti-diabetic activity; other eleven taxa also exhibited inhibitory activity of α-amylase ranging from (85-69%) compared with Metformin (67%) standard drug. Phytochemical screening revealed that selected taxa proved to be the potential source of natural antioxidants and could further be explored for in-vivo studies and utilized in pharmaceutical industries as potent therapeutic agents validating their ethno-pharmacological uses.

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