In vitro anti-venom potential of various Jatropha extracts on neutralizing cytotoxic effect induced by phospholipase A2 of crude venom from Indian cobra (Naja naja)

Canthium parviflorum is used in the traditional therapy to treat snakebite victims. In the present study, partially purified methanol root extract of C. parviflorum was used for the neutralization of Eachis carinatus and Naja naja venom. The extract inhibited in vitro phosphomonoesterase, phosphodiesterase, acetylcholinesterase, hyaluronidase, protease, phospholipase A2 and 5’nucleotidase activities of both venoms. One of the promising band exhibited neutralization of all the in vitro enzyme activities and was further subjected to GC-MS analysis which revealed the presence of eight active phytocompounds. These phytochemicals might be responsible for in vitro enzyme neutralization. Methanol extract possesses potent active phytochemicals against the site specific toxins and hydrolytic enzymes analyzed.Video Clip of Methodology:<a href="https://youtube.com/v/oSLdFcfaJxU">Phospholipase A2 assay</a>: 1 min 36 sec

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The in vitro study of anti-leishmanial effect of Naja naja oxiana snake venom on Leishmania major

Infectious Disorders - Drug Targets ◽

10.2174/1871526520666200106121839 ◽

2020 ◽

Vol 20 ◽

Cited By ~ 1

Author(s):

Nastaran Fallahi ◽

Delavar Shahbazzadeh ◽

Fatemeh Maleki ◽

Marjaneh Aghdasi ◽

Fatemeh Tabatabaie ◽

...

Keyword(s):

Leishmania Major ◽

In Vitro Study ◽

Resistance Rate ◽

Standard Strain ◽

Crude Venom ◽

Naja Naja ◽

Ic50 Value ◽

Late Apoptosis ◽

First Time

Background: Although a majority of patients with cutaneous leishmaniasis (CL) are healed with Glucantime chemotherapy, the increased drug resistance rate following its consumption is a concern. In this study , Naja naja oxiana crude venom of cobra snakes was used for the first time as an assembled combination of bioactive pharmaceutical components on Leishmania major (L. major) standard strain . Objective: To evaluate the efficacy of the Naja naja oxiana crude venom of Iranian cobra snakes on Leishmania major standard strain in vitro. Methods: Five concentrations (1.25, 2.5, 5, 10 and 20 µg/mL) of venom were added to Leishmania major cultures at 24, 48 and 72 h. The viability of the parasites and venom toxicity were assessed by MTT test. The apoptosis was determined by flowcytometry, while IC50 was determined by counting parasites compared to that of glucantime. Each test was conducted in triplicate. Results: After exposure the venom at 2.5 µg/mL for 72 h, IC50 value was 0.36 µg/mL and 14.12 µg/mL for promastigotes and amastigotes, respectively. MTT valuation clarified 1.01% promastigotes viability. Furthermore, the results indicated that the venom of Naja naja oxiana induced early and late apoptosis in parasites. Conclusions: The venom of Naja naja oxiana revealed remarkable anti-leishmanial effects as a novel anti-parasitic alternative. Thus the bioactive and effective fractions of this venom may be considered as anti-leishmanial candidates in future studies.

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Mechanism of Inhibitory Action on Platelet Activation of a Phospholipase A2 Isolated from Lachesis muta (Bushmaster) Snake Venom

Thrombosis and Haemostasis ◽

10.1055/s-0038-1665414 ◽

1997 ◽

Vol 78 (05) ◽

pp. 1372-1380 ◽

Cited By ~ 56

Author(s):

André L Fuly ◽

Olga L T Machado ◽

Elias W Alves ◽

Célia R Carlinis

Keyword(s):

Platelet Aggregation ◽

Enzymatic Activity ◽

Phospholipase A2 ◽

Inhibitory Activity ◽

Thermal Inactivation ◽

Anticoagulant Activity ◽

Gel Filtration ◽

Apparent Molecular Weight ◽

Crude Venom ◽

Lachesis Muta

SummaryCrude venom from Lachesis muta exhibited procoagulant, proteolytic and phospholipase A2 activities. A phospholipase A2, denoted LM-PLA2 was purified from L. muta venom to homogeneity, through a combination of chromatographic steps involving gel-filtration on Sephacryl S-200 HR and reverse phase chromatography on a C2/C18 column. LM-PLA2 presented a single polypeptide chain with an isoelectric point at pH 4.7 and apparent molecular weight of 17 kDa. Partial aminoacid sequence indicated a high degree of homology for LM-PLA2 with other PLA2 from different sources.LM-PLA2 displayed a potent enzymatic activity as measured by indirect hemolysis of red blood cells but it was neither lethal when injected i.p. into mice nor did it present anticoagulant activity. Furthermore, LM-PLA2 displayed a moderate inhibitory activity on the aggregation of rabbit platelets induced by low levels of ADP, thrombin and arachidonate. In contrast, platelet aggregation induced by high doses of collagen was strongly inhibited by LM-PLA2 as well as ATP-release. Treatment of the protein with p-bromophenacyl bromide or 2-mercapto-ethanol, as well as thermal inactivation studies, suggested that the platelet inhibitory effect of LM-PLA2 is dependent on its enzymatic activity. Thus, the platelet inhibitory activity of LM-PLA2 was shown to be dependent on the hydrolysis of plasma phospholipids and/or lipoproteins, most probably those rich in phosphatidylcholine. Surprisingly, lyso-phosphatidylcholine released by LM-PLA2 from plasma was shown to preferentially inhibited collagen-induced platelet aggregation, in contrast to other PLA2s, whose plasma hydrolytic products indistinctly affect platelet’s response to several agonists.

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In vitro Cytotoxic Effect of Extracts from Styela plicata

Journal of the Korean Society of Food Science and Nutrition ◽

10.3746/jkfn.2007.36.9.1099 ◽

2007 ◽

Vol 36 (9) ◽

pp. 1099-1105 ◽

Cited By ~ 2

Author(s):

Bo-Bae Lee ◽

Mi-Ran Cha ◽

Hae-Ryong Park ◽

Seung-Cheol Lee

Keyword(s):

Cytotoxic Effect ◽

Styela Plicata

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Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

Current Computer - Aided Drug Design ◽

10.2174/1573409916666201224153414 ◽

2020 ◽

Vol 16 ◽

Author(s):

Anjali P.B ◽

Jawahar N. ◽

Jubie S. ◽

Neetu Yadav ◽

Selvaraj A. ◽

...

Keyword(s):

Drug Release ◽

Phospholipase A2 ◽

Release Kinetics ◽

Entrapment Efficiency ◽

Structural Analog ◽

Fickian Diffusion ◽

Release Kinetic ◽

Nanostructured Lipid Carrier ◽

Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

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Detoxifying Action of Aqueous Extracts of Mucuna pruriens Seed and Mimosa pudica Root Against Venoms of Naja nigricollis and Bitis arietans

Recent Patents on Biotechnology ◽

10.2174/1872208313666191025110019 ◽

2020 ◽

Vol 14 (2) ◽

pp. 134-144 ◽

Cited By ~ 1

Author(s):

Matthew P. Ameh ◽

Mamman Mohammed ◽

Yusuf P. Ofemile ◽

Magaji G. Mohammed ◽

Ada Gabriel ◽

...

Keyword(s):

Phospholipase A2 ◽

Plant Extracts ◽

Fibrinolytic Activity ◽

Neglected Tropical Diseases ◽

World Health ◽

Mucuna Pruriens ◽

Phytochemical Analysis ◽

Mimosa Pudica ◽

Health Organization

Background: The World Health Organization included snakebite envenomation among Neglected Tropical Diseases in 2017. The importance of natural products from plants is enormous, given that most prescribed drugs originate from plants. Among this is Mucuna pruriens and Mimosa pudica, with many registered patents asserting their health benefits. Objective: This study investigated the in vitro neutralizing effects of Mucuna pruriens seed and Mimosa pudica root extracts on venoms of Naja nigricollis and Bitis arietans. Methods: In mice, the LD50 and phytochemical analysis of M. pruriens and M. pudica plant extracts were carried out prior to the evaluation of their haemolytic and fibrinolytic effect. Their effects on the activities of phospholipase A2 (PLA2) were also assessed. Results: At a concentration of 50 mg/ml, both plant extracts were found to neutralize the fibrinolytic activity of N. nigricollis, but 400 mg/ml was required to neutralize the fibrinolytic activity of B. arietans. In haemolytic studies, 50 mg/ml concentration of M. pruriens extract suppressed haemolysis caused by N. nigricollis venom by 70% but at the same concentration, M. pudica extract reduced haemolysis by 49.4%. M. pruriens, at 50 mg/ml concentration, only inhibited phospholipase A2 activity by 7.7% but higher concentrations up to 400mg/ml had no effect against the venom of N. nigricollis; at 200 mg/ml. M. pudica extract inhibited PLA2 activity by 23%. Conclusion: The results suggest that M. pruriens and M. pudica may be considered as promising antivenom agents for people living in a snake-bite prone environment.

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