1.In vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.
Sachin JAIN ; Praveen SHARMA ; Santosh GHULE ; Ankit JAIN ; Nitesh JAIN
Chinese Journal of Natural Medicines (English Ed.) 2013;11(5):472-476
AIM:
To study the in vivo anti-inflammatory activity of Tabernaemontana divaricata leaf extract on male albino mice.
METHODS:
Aqueous decoction and methanol leaf extracts were tested for their ability to reduce croton oil-induced edema in the mouse ear after topical application. The methanol leaf extract dose-dependently inhibited the croton oil-induced ear edema in mice (ID50 <500 μg·cm(-2)). A bioassay-guided liquid-liquid fractionation of this methanol extract gave four active fractions: water insoluble (F1), hexane (F2), ethyl acetate (F3) and water (F4).
RESULTS:
The hexane fraction showed a very high activity (42.1% inhibition at 0.7 μg·cm(-2)) as compared to the control. The other fractions were less active (F1: 56.1% at 506.2 μg·cm(-2); F3: 57.3% at 289.3 μg·cm(-2); and F4: 31.9% for 203.8 μg·cm(-2)) while indomethacin gave 48.8% of inhibition at 90 μg·cm(-2). The activity of F1 and F3 may be at least in part explained by the presence of anti-inflammatory flavonoids, while the activity was not correlated to the tannin contents. No compounds were detected in the most active F2 fraction.
CONCLUSIONS
The results give a rational support to the traditional use of T. divaricata in tropical India as anti-inflammatory agent.
Animals
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Anti-Inflammatory Agents
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administration & dosage
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Edema
;
drug therapy
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Humans
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Male
;
Mice
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Plant Extracts
;
administration & dosage
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Plant Leaves
;
chemistry
;
Tabernaemontana
;
chemistry
2.Efficacy of Ulinastatin and Sulforaphane Alone or in Combination in Rat Model of Streptozotocin Diabetes Induced Vascular Dementia
Poonam SHARMA ; Prachi KAUSHIK ; Swati JAIN ; Brij Mohan SHARMA ; Rajendra AWASTHI ; Giriraj Thirupathirao KULKARNI ; Bhupesh SHARMA
Clinical Psychopharmacology and Neuroscience 2021;19(3):470-489
Objective:
Vascular Dementia (VaD), is associated with metabolic conditions. Diabetes is a major risk factor for the development of VaD. This study investigates the efficacy of ulinastatin (UTI) and sulforaphane (SUL) in streptozotocin (STZ)-diabetes induced vascular endothelium dysfunction and related dementia.
Methods:
Single dose STZ (50 mg/kg i.p.) was administered to Albino Wistar rats (male, 200−250 g). Morris water maze and attentional set shifting tests were used to assess the spatial learning, memory, reversal learning, and executive functioning in animals. Body weight, serum glucose, serum nitriteitrate, vascular endothelial function, aortic superoxide anion, brains’ oxidative markers (thiobarbituric acid reactive species-TBARS, reduced glutathione-GSH, superoxide dismutase-SOD, and catalase-CAT), inflammatory markers (IL-6, IL-10, TNF-, and myeloperoxidase-MPO), acetylcholinesterase activity-AChE, blood brain barrier (BBB) permeability and histopathological changes were also assessed. UTI (10,000 U/kg) and SUL (25 mg/kg) were used alone as well as in combination, as the treatment drugs. Donepezil (0.5 mg/kg) was used as a positive control.
Results:
STZ-administered rats showed reduction in body weight, learning, memory, reversal learning, executive functioning, impairment in endothelial function, BBB permeability, increase in serum glucose, brains’ oxidative stress, inflammation, AChE-activity, BBB permeability and histopathological changes. Administration of UTI and SUL alone as well as in combination, significantly and dose dependently attenuated the STZ-diabetes-induced impairments in the behavioral, endothelial, and biochemical parameters.
Conclusion
STZ administration caused diabetes and VaD which was attenuated by the administration of UTI and SUL.Therefore, these agents may be studied further for the assessment of their full potential in diabetes induced VaD.
3.Efficacy of Ulinastatin and Sulforaphane Alone or in Combination in Rat Model of Streptozotocin Diabetes Induced Vascular Dementia
Poonam SHARMA ; Prachi KAUSHIK ; Swati JAIN ; Brij Mohan SHARMA ; Rajendra AWASTHI ; Giriraj Thirupathirao KULKARNI ; Bhupesh SHARMA
Clinical Psychopharmacology and Neuroscience 2021;19(3):470-489
Objective:
Vascular Dementia (VaD), is associated with metabolic conditions. Diabetes is a major risk factor for the development of VaD. This study investigates the efficacy of ulinastatin (UTI) and sulforaphane (SUL) in streptozotocin (STZ)-diabetes induced vascular endothelium dysfunction and related dementia.
Methods:
Single dose STZ (50 mg/kg i.p.) was administered to Albino Wistar rats (male, 200−250 g). Morris water maze and attentional set shifting tests were used to assess the spatial learning, memory, reversal learning, and executive functioning in animals. Body weight, serum glucose, serum nitriteitrate, vascular endothelial function, aortic superoxide anion, brains’ oxidative markers (thiobarbituric acid reactive species-TBARS, reduced glutathione-GSH, superoxide dismutase-SOD, and catalase-CAT), inflammatory markers (IL-6, IL-10, TNF-, and myeloperoxidase-MPO), acetylcholinesterase activity-AChE, blood brain barrier (BBB) permeability and histopathological changes were also assessed. UTI (10,000 U/kg) and SUL (25 mg/kg) were used alone as well as in combination, as the treatment drugs. Donepezil (0.5 mg/kg) was used as a positive control.
Results:
STZ-administered rats showed reduction in body weight, learning, memory, reversal learning, executive functioning, impairment in endothelial function, BBB permeability, increase in serum glucose, brains’ oxidative stress, inflammation, AChE-activity, BBB permeability and histopathological changes. Administration of UTI and SUL alone as well as in combination, significantly and dose dependently attenuated the STZ-diabetes-induced impairments in the behavioral, endothelial, and biochemical parameters.
Conclusion
STZ administration caused diabetes and VaD which was attenuated by the administration of UTI and SUL.Therefore, these agents may be studied further for the assessment of their full potential in diabetes induced VaD.
4.Synthesis of New VO(II), Co(II), Ni(II) and Cu(II) Complexes with Isatin-3-Chloro-4-Floroaniline and 2-Pyridinecarboxylidene-4-Aminoantipyrine and their Antimicrobial Studies.
Anand P MISHRA ; Rudra MISHRA ; Rajendra JAIN ; Santosh GUPTA
Mycobiology 2012;40(1):20-26
The complexes of tailor made ligands with life essential metal ions may be an emerging area to answer the problems of multi drug resistance. The coordination complexes of VO(II), Co(II), Ni(II) and Cu(II) with the Schiff bases derived from isatin with 3-chloro-4-floroaniline and 2-pyridinecarboxaldehyde with 4-aminoantipyrine have been synthesized by conventional as well as microwave methods. These compounds have been characterized by elemental analysis, molar conductance, electronic spectra, FT-IR, FAB mass and magnetic susceptibility measurements. FAB mass data show degradation of complexes. Both the ligands behave as bidentate and tridentate coordinating through O and N donor. The complexes exhibit coordination number 4, 5 or 6. The Schiff base and metal complexes show a good activity against the bacteria; Staphylococcus aureus, Escherichia coli and Streptococcus fecalis and fungi Aspergillus niger, Trichoderma polysporum, Candida albicans and Aspergillus flavus. The antimicrobial results also indicate that the metal complexes are better antimicrobial agents as compared to the Schiff bases. The minimum inhibitory concentrations of the metal complexes were found in the range 10~40 microg/mL.
Ampyrone
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Anti-Infective Agents
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Aspergillus flavus
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Aspergillus niger
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Candida albicans
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Coordination Complexes
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Drug Resistance
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Electronics
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Electrons
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Escherichia coli
;
Fungi
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Humans
;
Ions
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Isatin
;
Ligands
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Magnetics
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Magnets
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Microbial Sensitivity Tests
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Microwaves
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Molar
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Pyridines
;
Schiff Bases
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Staphylococcus aureus
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Streptococcus
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Tissue Donors
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Trichoderma
5.Inhibition of ADP-induced platelet aggregation and involvement of non-cellular blood chemical mediators are responsible for the antithrombotic potential of the fruits of Lagenaria siceraria.
Mithun Singh RAJPUT ; Neelam BALEKAR ; Dinesh Kumar JAIN
Chinese Journal of Natural Medicines (English Ed.) 2014;12(8):599-606
AIM:
The fruits of Lagenaria siceraria (Molina) Standl. (Cucurbitaceae), a commonly used vegetable, are reported to possess various medicinal properties. In previous studies, the fibrinolytic potential of an ethanolic extract of fruits of Lagenaria siceraria was investigated in comparison with kaempferol isolated from it. The aim of the present study was to explore its mechanistic antithrombotic potential and antiplatelet activity using a wide dose range in different in vitro and in vivo models, and to quantify the total phenolic, flavonoid, and kaempferol contents using a colorimetric method.
METHOD:
The antithrombotic potential was investigated using tail bleeding time in mice, a plasma recalcification assay, and pulmonary thromboembolism in mice. The antiplatelet activity was studied using an in vitro model to investigate IC50 value.
RESULTS:
A significant amount of total phenols, flavonoids, and kaempferol was quantified in L. siceraria ethanolic extract. An ethanolic extract of the fruits of L. siceraria showed a significant increase in tail bleeding time and plasma recalcification time, significant protection against ADP induced pulmonary thromboembolism in mice, and also inhibited the platelet aggregation induced by ADP in vitro. The study suggested that the fruits of L. siceraria exhibit significant antithrombotic potential due to inhibition of ADP-mediated platelet aggregation and the involvement of various non-cellular chemical mediators of blood.
CONCLUSION
This finding may be helpful in treating the serious consequences of the thrombus formed in blood vessels which include atherothrombotic diseases, such as myocardial or cerebral infarction. So, further investigation should be done for revealing exact mechanism of action behind these types of activities.
Adenosine Diphosphate
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Animals
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Calcium
;
blood
;
Cucurbitaceae
;
chemistry
;
Female
;
Fibrinolytic Agents
;
analysis
;
pharmacology
;
therapeutic use
;
Fruit
;
Goats
;
Kaempferols
;
analysis
;
pharmacology
;
therapeutic use
;
Male
;
Mice
;
Phytotherapy
;
Plant Extracts
;
chemistry
;
pharmacology
;
therapeutic use
;
Platelet Aggregation
;
drug effects
;
Platelet Aggregation Inhibitors
;
analysis
;
pharmacology
;
therapeutic use
;
Polyphenols
;
analysis
;
pharmacology
;
therapeutic use
;
Pulmonary Embolism
;
blood
;
chemically induced
;
drug therapy
;
Rats, Wistar
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Thrombosis
;
prevention & control