Inhibition of Amyloid β Aggregation Using Optimized Nano-Encapsulated Formulations of Plant Extracts with High Metal Chelator Activities

2020 ◽  
Vol 21 (8) ◽  
pp. 681-701
Author(s):  
Fatma Kazdal ◽  
Fatemeh Bahadori ◽  
Burak Celik ◽  
Abdulselam Ertas ◽  
Gulacti Topcu
Keyword(s):  
Plant Extracts ◽  
Amyloid Β ◽  
Toxic Metal ◽  
In Vivo Studies ◽  
Total Phenolic ◽  
Metal Chelator ◽  
Apo E ◽  
High Metal ◽  
Induced Aggregation

Background: The role of Fe+2, Cu+2 and Zn+2 in facilitating aggregation of Amyloid β (Aβ) and consequently, the progression of Alzheimer's disease (AD) is well established. Objective: Development of non-toxic metal chelators is an emerging era in the treatment of AD, in which complete success has not been fully achieved. The purpose of this study was to determine plant extracts with high metal chelator and to encapsulate them in nano-micellar systems with the ability to pass through the Blood Brain Barrier (BBB). Method: Extracts of 36 different Anatolian plants were prepared, total phenolic and flavonoid contents were determined, and the extracts with high content were examined for their Fe+2, Cu+2 and Zn+2 chelating activities. Apolipoprotein E4 (Apo E) decorated nano-formulations of active extracts were prepared using Poly (Lactide-co-Glycolide) (PLGA) (final product ApoEPLGA) to provide BBB penetrating property. Results: Verbascum flavidum aqueous extract was found as the most active sample, incubation of which, with Aβ before and after metal-induced aggregation, resulted in successful inhibition of aggregate formation, while re-solubilization of pre-formed aggregates was not effectively achieved. The same results were obtained using ApoEPLGA. Conclusion: An optimized metal chelator nano-formulation with BBB penetrating ability was prepared and presented for further in-vivo studies.

Phenolic Acids Exert Anticholinesterase and Cognition-Improving Effects

2018 ◽  
Vol 15 (6) ◽  
pp. 531-543 ◽  
Author(s):  
Dominik Szwajgier ◽  
Ewa Baranowska-Wojcik ◽  
Kamila Borowiec
Keyword(s):  
Phenolic Acids ◽  
Ex Vivo ◽  
Amyloid Β ◽  
Inhibitory Effect ◽  
In Vivo Studies ◽  
Amyloid Β Peptide ◽  
Beneficial Effects ◽  
Aβ Fibrils

Numerous authors have provided evidence regarding the beneficial effects of phenolic acids and their derivatives against Alzheimer's disease (AD). In this review, the role of phenolic acids as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is discussed, including the structure-activity relationship. In addition, the inhibitory effect of phenolic acids on the formation of amyloid β-peptide (Aβ) fibrils is presented. We also cover the in vitro, ex vivo, and in vivo studies concerning the prevention and treatment of the cognitive enhancement.

scholarly journals Efficacy of different fungicides and biopesticides for the management of lentil wilt (Fusarium oxysporum f. sp. lentis)

2021 ◽  
Vol 8 (01) ◽  
Author(s):  
KAMLESH RAM ◽  
RAMESH SINGH
Keyword(s):  
Seed Germination ◽  
Grain Yield ◽  
Plant Extracts ◽  
Seed Treatment ◽  
In Vivo Studies ◽  
Test Plant ◽  
Mycelia Growth ◽  
Wilt Incidence

In Vitro and In Vivo studies on the efficacy of fungicides and biopesticides. Among the fungicides, in Carbedazim to the most effective as they have inhibited the mycelia growth completely of the test fungus, and Benomyl, Topsin - M, Ridomil,Vitavax were found the next best in inhibiting the mycelial growth of the pathogen up to 92.11% to 83.46% respectively. Sadabahar was least effective plant extracts which causes 42 mm of radial growth and inhibited the growth of the only 19.23%. In Vivo condition the maximum seed germination (95.50% and 95.33%), minimum wilt incidence (5.16% and 3.65%) and highest grain yield (10.50 q/ha and 10.35 q/ha) was found seed treatment with Carbendazim (0.2%). Among the test plant extracts Tulsi was lested effective, which show the minimum seed germination (80.00% and 77.50%), maximum wilt incidence (15.70% and 14.10%), and lowest grain yield (3.92 q/ha and 4.17 q/ha).

scholarly journals Antioxidant Activities and Reduced Amyloid-β Toxicity of 7-Hydroxycalamenene Isolated from the Essential Oil of Zelkova serrata Heartwood

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Pei-Ling Yen ◽  
Sen-Sung Cheng ◽  
Chia-Cheng Wei ◽  
Huan-You Lin ◽  
Vivian Hsiu-Chuan Liao ◽  
...  
Keyword(s):  
Essential Oil ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Amyloid Β ◽  
Total Phenolic ◽  
C Elegans ◽  
In Vivo Assays ◽  
Zelkova Serrata

The in vitro and in vivo antioxidant activities and its potential to protect against amyloid-β toxicity of essential oils from Zelkova serrata (Thunb.) Makino were investigated in the model organism Caenorhabditis elegans. The results revealed that the essential oil of Z. serrata heartwood exhibited great radical scavenging activities and high total phenolic content. In vivo assays showed significant inhibition of oxidative damage in wild-type C. elegans under juglone-induced oxidative stress and heat shock. Based on results from both in vitro and in vivo assays, the major compound in essential oil of heartwood, (-)-(1 S, 4 S)-7-hydroxycalamenene (1 S, 4 S-7HC), may contribute significantly to the observed antioxidant activity. Further evidence showed that 1 S, 4 S-7HC significantly delayed the paralysis phenotype in amyloid beta-expressing transgenic C. elegans. These findings suggest that 1 S, 4 S-7HC from the essential oil of Z. serrata heartwood has potential as a source for antioxidant or Alzheimer's disease treatment.

Preliminary pharmacologic evaluation of crude whole plant extracts of Elephantopus scaber. Part I: in vivo studies

1992 ◽  
Vol 37 (1) ◽  
pp. 71-76 ◽  
Author(s):  
Anicleto Poli ◽  
Mauro Nicolau ◽  
Claudia Maria Oliveira Simões ◽  
Rosa Maria Ribeiro-do-Valle Nicolau ◽  
Marlene Zanin
Keyword(s):  
Plant Extracts ◽  
In Vivo Studies ◽  
Whole Plant ◽  
Elephantopus Scaber

Investigation of anti-Alzheimer’s activity of aqueous extract of areca nuts (Areca catechu L.): In vitro and in vivo studies

2021 ◽  
Vol 20 (4) ◽  
pp. 406-415
Author(s):  
Mahboubeh Bozorgi ◽  
◽  
Zahra Najafi ◽  
Sahar Omidpanah ◽  
Arash Sadri ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Neurodegenerative Disorder ◽  
Amyloid Β ◽  
In Vivo Studies ◽  
Memory Impairments ◽  
Age Related ◽  
Areca Catechu ◽  
Aβ Aggregation

Alzheimer’s disease (AD) is an age-related neurodegenerative disorder. Sever cognitive and memory impairments, huge increase in the prevalence of the disease, and lacking definite cure have absorbed worldwide efforts to develop therapeutic approaches. Since many drugs have failed in the clinical trials due to multifactorial nature of AD, symptomatic treatments are still in the center attention and now, nootropic medicinal plants have been found as versatile ameliorators to reverse memory disorders. In this work, anti-Alzheimer’s activity of aqueous extract of areca nuts (Areca catechu L.) was investigated via in vitro and in vivo studies. It depicted good amyloid β (Aβ) aggregation inhibitory activity, 82% at 100 µg/mL. In addition, it inhibited beta-secretase 1 (BACE1) with IC50 value of 19.03 µg/mL. Evaluation of neuroprotectivity of the aqueous extract of the plant against H2O2-induced cell death in PC12 neurons revealed 84.5% protection at 1 µg/mL. It should be noted that according to our results obtained from Morris Water Maze (MWM) test, the extract reversed scopolamine-induced memory deficit in rats at concentrations of 1.5 and 3 mg/kg.

scholarly journals In Vivo Studies with a New Antiaggregating Drug EMD 26644, A Mercapto-Oxazolyl-Carbon-Acid Derivative

1977 ◽  
Author(s):  
H. J. Krzywanek ◽  
U. Pietsch ◽  
K. Breddin
Keyword(s):  
Incubation Temperature ◽  
Shape Change ◽  
Inhibitory Effect ◽  
In Vivo Studies ◽  
Factor Vii ◽  
Thrombin Time ◽  
Antithrombotic Agent ◽  
Platelet Spreading ◽  
Induced Aggregation

The inhibitory effect of EMD 26644 on platelet function has been studied with the following methods: spontaneous aggregation (PAT III), ADP-, collagen-and epinephrire-induced aggregation, primary shape change of thrombocytes at 37°C incubation temperature and platelet spreading.Duke’s bleeding time, platelet count and some coagulation parameters like partial thromboplastin time, Quick’s test, fibrinogen, thrombin time and factor VII-assay as well as platelet spreading were unchanged throughout the test period.An aspirin like inhibitory effect on platelet aggregation and primary shape change was observed 48 – 72 hrs. after the ingestion of a single dose of 250 mg EMD, which lasted for 2–3 weeks. A prolonged antiaggregating effect was achieved by the continuous oral administration of 25 – 50 mg EMD for a period of 2 – 3 months. No potentiation of the antiaggregating effect was seen, if ASA was given in addition to EMD 26644.In comparison with aspirin the new compound seems to have some advantages: the same antiplatelet properties are achieved with a much lower dose and no side effects have been reported so far. Clinical studies will have to confirm whether EMD 26644 is an effective antithrombotic agent.

scholarly journals Prunella vulgaris L. Potentiates Answer to the Emergence of Dreaded Antibiotic Resistance

2021 ◽  
Author(s):  
Jitendra K. Patel ◽  
Chetan Kumar Joshi ◽  
Mukesh Kumar Sharma
Keyword(s):  
Petroleum Ether ◽  
Plant Extracts ◽  
Herbal Extract ◽  
In Vivo Studies ◽  
Human Beings ◽  
Prunella Vulgaris ◽  
Reduced Pressure ◽  
E Coli

Medicinal herbs that are in use for centuries to treat infections and other illnesses. Prunella vulgaris L. is traditionally used for its therapeutic attributes for the alleviation of various infectious diseases. The objective of this study on Prunella vulgaris was to reveal relevant pharmaceutical information to understand its beneficial medicinal uses for human beings. The methanolic and petroleum ether extracts after removal of the solvent under reduced pressure from the Prunella vulgaris plants were prepared and these extracts were analyzed in vitro for their activity against B. subtilis, E. coli, S. aureus and S. typhi (with ATCC numbers 6051, 25922, 23235 and 14028 respectively). Likewise, in vivo studies were conducted using the E. coli-induced peritonitis in laboratory rat models where the rats were given allopathic antibiotic ofloxacin and the results were compared with those rats who received plant extracts under controlled conditions. The results were analyzed for the efficacy of the plant extracts was compared with ofloxacin; the methanol extracts exhibited equally if not better results in clearing the pathogen from the system of animals. The petroleum ether extracts exhibited the least antimicrobial activity in comparison to those extracted in methanol isolates. In conclusion, the herbal extract demonstrated significant antibacterial activity both under in-vitro and in-vivo studies which is a major outcome of the study. During this study, all standards and norms were followed as per government animal authority.

scholarly journals Antischistosomal Activity of Origanum majorana, Ziziphus spina-christi, and Salvia fruticosa Plant Extracts on Hamster Infected with Schistosoma haematobium

2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Yousef Abdal Jalil Fadladdin
Keyword(s):  
Plant Extracts ◽  
Schistosoma Haematobium ◽  
Early Stage ◽  
World Health ◽  
In Vivo Studies ◽  
Salvia Fruticosa ◽  
Medical Plant ◽  
Origanum Majorana

World Health Organization (WHO) has approved only one treatment for schistosomiasis, praziquantel (PZQ), but some poor efficacy was noticed in patients during the early stage of infection. Therefore, researchers have intensified their efforts to research new alternative medicines to treat schistosomiasis. In the present study, in vitro as well as in vivo studies have been accomplished to evaluate the effect of Origanum majorana, Ziziphus spina-christi, and Salvia fruticosa extracts in a different concentration 500, 250, 125, 62.5, and 31.25 μg/ml on golden hamster infected by Egyptian strains of schistosome (Schistosoma haematobium). In vitro, the adult worms and schistosomula of S. haematobium were investigated in RPMI-1640 medium for 48 hrs. The results showed that the concentration 500, 250, and 125 μg/ml of Origanum majorana, and Ziziphus spina-christi caused dead of 100% of Egyptian Schistosoma strains of adult worm and schistosomula of S. haematobium within 6 to 12 hrs of incubation. On the other hand, the extract of Salvia fruticosa at concentrations 500, 250, and 125 μg/ml showed death 100% parasites after 12 to 24 hrs of incubation. Inclusion, Origanum majorana, and Ziziphus spina-christi showed effectiveness against Egyptian Schistosoma strains (S. haematobium), a slight decrease in Salvia fruticosa was observed. Therefore, these medical plant extracts may be used as a safe and effective treatment for schistosomiasis.

scholarly journals Structure–Activity Relationship Study of Newly Synthesized Iridium-III Complexes as Potential Series for Treating Thrombotic Diseases

2018 ◽  
Vol 19 (11) ◽  
pp. 3641 ◽  
Author(s):  
Chih-Hao Yang ◽  
Chih-Wei Hsia ◽  
Thanasekaran Jayakumar ◽  
Joen-Rong Sheu ◽  
Chih-Hsuan Hsia ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Chloride Ion ◽  
Adenosine Diphosphate ◽  
Structure Activity Relationship ◽  
In Vivo Studies ◽  
Activity Relationship ◽  
Structure Activity ◽  
Induced Aggregation

Platelets play a major role in hemostatic events and are associated with various pathological events, such as arterial thrombosis and atherosclerosis. Iridium (Ir) compounds are potential alternatives to platinum compounds, since they exert promising anticancer effects without cellular toxicity. Our recent studies found that Ir compounds show potent antiplatelet properties. In this study, we evaluated the in vitro antiplatelet, in vivo antithrombotic and structure–activity relationship (SAR) of newly synthesized Ir complexes, Ir-1, Ir-2 and Ir-4, in agonists-induced human platelets. Among the tested compounds, Ir-1 was active in inhibiting platelet aggregation induced by collagen; however, Ir-2 and Ir-4 had no effects even at their maximum concentrations of 50 μM against collagen and 500 μM against U46619-induced aggregation. Similarly, Ir-1 was potently inhibiting of adenosine triphosphate (ATP) release, calcium mobilization ([Ca2+]i) and P-selectin expression induced by collagen-induced without cytotoxicity. Likewise, Ir-1 expressively suppressed collagen-induced Akt, PKC, p38MAPKs and JNK phosphorylation. Interestingly, Ir-2 and Ir-4 had no effect on platelet function analyzer (PFA-100) collagen-adenosine diphosphate (C-ADP) and collagen-epinephrine (C-EPI) induced closure times in mice, but Ir-1 caused a significant increase when using C-ADP stimulation. Other in vivo studies revealed that Ir-1 significantly prolonged the platelet plug formation, increased tail bleeding times and reduced the mortality of adenosine diphosphate (ADP)-induced acute pulmonary thromboembolism in mice. Ir-1 has no substitution on its phenyl group, a water molecule (like cisplatin) can replace its chloride ion and, hence, the rate of hydrolysis might be tuned by the substituent on the ligand system. These features might have played a role for the observed effects of Ir-1. These results indicate that Ir-1 may be a lead compound to design new antiplatelet drugs for the treatment of thromboembolic diseases.

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