scholarly journals Extraction, isolation, characterization, semi-synthesis and antiplasmodial activity of Justicia adathoda leaves

2016 ◽  
Vol 11 (4) ◽  
pp. 878 ◽  
Author(s):  
Sivaperumal Gopalan ◽  
Kannnan Kulanthai ◽  
Gnanavel Sadashivam ◽  
Perumal Pachiappan ◽  
Sowmiya Rajamani ◽  
...  

<p>There is a need to investigate the new sources of antimalarial drugs which are more effective against Plasmodium falciparum. The present study was undertaken to evaluate the in vitro antiplasmodial activity of vasicinone, vasicine and 9-oxo-1, 2, 3, 9-tetrahydropyrrolo [2,1-b]quinazolin-3-yl acetate (VA-1). Vasicinone and vasicine were extracted from the leaves of Justicia adhatoda. The novel compound VA-1 was synthesized from alkaloid the alkaloid vasicine, which was isolated from the ethanol extract of J. adhatoda leaves. Vasicine (IC<sub>50</sub> = 89.8 µg/mL) and vasicinone (IC<sub>50</sub> = 38.9 µg/mL) showed moderate antiplasmodial activity whereas the compound VA-1 ( IC<sub>50</sub>  = 06.0 µg/mL) showed excellent antiplasmodial activity when compared with standard drug chloroquine (IC<sub>50</sub>  = 12.6 µg/mL). The results achieved suggest that both isolated and semi-synthetic compounds may serve as a lead compound to antiplasmodial activity. Further, the compound VA-1 is for the first time reported for antiplasmodial activity with IC<sub>50</sub> value.</p><p><strong>Video Clip:</strong></p><p><a href="https://youtube.com/v/dcQUBU6PuVw">Antiplasmodia activity procedure</a>: 7 min 13 sec</p>

2018 ◽  
Vol 13 (10) ◽  
pp. 1934578X1801301
Author(s):  
Partha P Dutta ◽  
Manobjyoti Bordoloi ◽  
Sonali Roy ◽  
Bardwi Narzary ◽  
Kabita Gogoi ◽  
...  

Gnetum gnemon L. (Gnetaceae) is used traditionally for treating malaria related fever by indigenous people of North East India. In our preliminary study, the ethanol extract of G. gnemon leaves showed promising antiplamodial activity against Plasmodium falciparum chloroquine sensitive (3D7) strain in vitro with an IC50 value of 29.4 μg/mL. Therefore, it was further investigated, and by following a bioassay guided approach, 2,3-dihydroxypropyl icosanoate (1), oleic acid (2) and ursolic acid (3) were isolated for the first time from this plant. Compound 3 showed highest antiplasmodial activity with IC50 values of 4.0 and 6.0 μg/mL against chloroquine sensitive (3D7) and resistant (Dd2) strains of P. falciparum, respectively. The antiplasmodial activity of 1 (IC50 9.5 and 11.4 μg/mL) and 2 (IC50 17.6 and 21.1 μg/mL) was moderate. The isolated constituents showed low cytotoxicity against rat skeletal muscle (L6) and human cervical cancer (HeLa) cells. This is the first report on the antimalarial potential of G. gnemon and the isolated compounds may be responsible for its activity. The findings of the study are in line with the ethnopharmacological claim and can be possible leads for future studies.


Author(s):  
Ekta Shirbhate ◽  
Preeti Patel ◽  
Vijay K Patel ◽  
Ravichandran Veerasamy ◽  
Prabodh C Sharma ◽  
...  

: The novel coronavirus disease-19 (COVID-19), a global pandemic that emerged from Wuhan, China has today travelled all around the world, so far 216 countries or territories with 21,732,472 people infected and 770,866 deaths globally (as per WHO COVID-19 update dated August 18, 2020). Continuous efforts are being made to repurpose the existing drugs and develop vaccines for combating this infection. Despite, to date, no certified antiviral treatment or vaccine prevails. Although, few candidates have displayed their efficacy in in vitro studies and are being repurposed for COVID-19 treatment. This article summarizes synthetic and semi-synthetic compounds displaying potent activity in their clinical experiences or studies against COVID-19 and also focuses on mode of action of drugs being repositioned against COVID-19.


2020 ◽  
Vol 6 (2) ◽  
pp. 155-169
Author(s):  
Neeraj Panihar ◽  
Neeru Vasudeva ◽  
Sunil Sharma ◽  
Babu Lal Jangir

Background: Fagopyrum esculentum Moench. is a herb consumed as food and has medicinal value. It is a rich source of bioactive nutrients which cure and prevent many ailments. Traditionally, it is used to treat hypertension, diabetes, constipation, cancer etc. Methods and Objective: Present work illustrates morphological, microscopic and physicochemical parameters of Fagopyrum esculentum seeds as per WHO guidelines, in vitro antioxidant activity; assessed by DPPH scavenging method, hydrogen peroxide scavenging assay and β-carotene linoleic acid bleaching method and study of lipid lowering potential of the ethyl acetate and ethanol extract of seeds on normal diet fed Wistar rats. Results: Morphological studies delineated the triangular shape, dark brown colour, 8 mm length and 6 mm width of the seed. The microscopic examination of the transverse section of seed depicted features like testa or pericarp (seed coat), the endosperm, embryo and sclerenchyma cells. Study of physiochemical parameters exhibited 0.3±0.02% of foreign matter and 1.44±0.51% crude fibre content. Total ash, acid insoluble ash and water soluble ash value were 6.7±1.7%, 1.9±0.23% and 3.9± 0.31% respectively. Alcohol soluble and water soluble extractive value came out to be 65.02± 3.21 mg/g and 12.7±1.24 mg/g respectively. Foaming index was less than 100, swelling index was found to be 0.5±0.01 ml/g. Loss on drying was 4.02±1.27%. Phytochemical screening of ethyl acetate and ethanol extract revealed the presence of alkaloids, carbohydrates, phenolic compounds, phytosterols and flavonoids. Trace amount of heavy metals (arsenic, cadmium, lead, mercury) were determined by atomic absorption spectrophotometer. Pesticide residue analysis confirmed the presence of nontoxic pesticides like dimethipin, hymexazol, phenothrin-2, methoprene, triadimenol, prohydrojasmon- 1, jasmolin ii, triademinol, jasmolin i, prohydrojasmone i, cyromazine in both the extracts by gc-ms spectrometer. The ethyl acetate and ethanol extract has shown significant in-vitro antioxidant activities demonstrated by the DPPH method (IC50 = 94.37±2.51 and 216.04±4.39 μg/ml respectively), hydrogen peroxide scavenging assay (IC50 = 83.72±3.72 and 193.47±5.05 µg/ml respectively) and β-carotene bleaching method (IC50 = 100.67±4.01 and 205.39±2.89 µg/ml respectively). Lipid lowering study performed on Wistar rats demonstrated a significant (p<0.001) decrease in serum Total Cholesterol (TC), Triglyceride (TG) and increase in High Density Lipoprotein (HDL) level as compared to normal group. Both the extracts have shown a non significant difference in the level of TG as compared to standard drug atorvastatin, depicting that the efficacy of extracts is at par with that of standard drug atorvastatin. Conclusion: Pharmacognostical study of the plant can be a very good tool for identification as well as authentication of a herb. Moreover, these parameters may be helpful in the development of monograph of the plant. Pharmacological activity confirmed Fagopyrum esculentum Moench. seed to be a good antioxidant and have lipid lowering potential.


Author(s):  
YASSER HUSSEIN EISSA MOHAMMED ◽  
DEEPIKA HS ◽  
FARES HEZAM AL-OSTOOT ◽  
ZABIULLA ◽  
ANILAKUMAR ◽  
...  

Objective: The objective of the study was to in vitro evaluate of hypolipidemic effect of extracts of medicinal Dracaena cinnabari Balf. f. resin. Methods: About 800 g of dry powder of the resin of dracaena cinnabar was taken in a Soxhlet apparatus and subjected for sequential extraction of solvents from non-polar to polar end (hexane, benzene, diethyl ether, dichloromethane, chloroform, ethyl acetate, acetone, ethanol, methanol, and water); the extract samples were kept at 4°C for further assays. All the extracts were subjected to glucose uptake assay. Results: The ethanol extract showed significant (p<0.05) hypolipidemic effect by decreasing the activity of enzyme such as significant reduction in the pancreatic lipase enzyme, malic dehydrogenase enzyme, and glucose-6-phosphate dehydrogenase enzyme with IC50~13, ~13, and ~14, respectively. This results were similar to the standard drug atorvastatin with IC50~12, ~16, and ~17, respectively. Ethanol extract exhibited significant atherogenic index and percentage protection against hyperlipidemia. The potential biological activity of ethanol extract may be attributed to the highest polarity which needs further investigation.


2020 ◽  
Vol 23 ◽  
pp. 54-62
Author(s):  
O.O. Amujoyegbe ◽  
M. Idu ◽  
J.M. Agbedahunsi ◽  
G.N. Bazuaye

Sickle cell disorder is a genetic ailment with enormous social and economic burden for patients and caregivers. The most promising management apart from being expensive particularly for poor African people, faces some major incompatibility problems. The patients consequently rely on herbal therapy which could be prepared in single or combination forms to manage the painful episodes and its complications. This present study aimed to formulate polyherbal combination and evaluate three purposively selected plants previously reported for their antisickling activities. The polyherbal products were formulated using both aqueous and 70% ethanol extracts into different combinational ratio with the best in 1:1:1 and evaluated for its antisickling activity. The antisickling activity involved both the inhibitory and reversal effects at varying concentrations from 1.0 mg/ml to 6.0 mg/ml using ciklavit as the positive control. The best inhibitory activity was found in ethanol extract of Piper guineense, Gongronema latifolium and Cymbopogon citratus (PGC) with 70.09 ± 0.67% when compared with the positive control (59.25 ± 0.05%) at 4.0 mg/mg while the reversal ability was 67.87 ± 1.23%. The aqueous extracts of the combinations had activity above 50% with the exception of PGC (2:3:1) which is a little less than 50% (46.67 ± 0.98%) while the highest was 60.02 ± 0.87%. The polyherbal ethanol extract had better effects than the aqueous extract and the standard drug used in this study.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Rosangela A. Falcao ◽  
Patricia L. A. do Nascimento ◽  
Silvana A. de Souza ◽  
Telma M. G. da Silva ◽  
Aline C. de Queiroz ◽  
...  

Hyptis pectinata, popularly known in Brazil as “sambacaitá” or “canudinho,” is an aromatic shrub largely grown in the northeast of Brazil. The leaves and bark are used in an infusion for the treatment of throat and skin inflammations, bacterial infections, pain, and cancer. Analogues of rosmarinic acid and flavonoids were obtained from the leaves ofHyptis pectinataand consisted of two new compounds, sambacaitaric acid (1) and 3-O-methyl-sambacaitaric acid (2), and nine known compounds, rosmarinic acid (3), 3-O-methyl-rosmarinic acid (4), ethyl caffeate (5), nepetoidin A (6), nepetoidin B (7), cirsiliol (8), circimaritin (9), 7-O-methylluteolin (10), and genkwanin (11). The structures of these compounds were determined by spectroscopic methods. Compounds1–5, and7were evaluatedin vitroagainst the promastigote form ofL. braziliensis, and the ethanol extract. The hexane, ethyl acetate, and methanol-water fractions were also evaluated. The EtOH extract, the hexane extract, EtOAc, MeOH:H2O fractions; and compounds1,2and4exhibited antileishmanial activity, and compound1was as potent as pentamidine. In contrast, compounds3,5, and7did not present activity against the promastigote form ofL. braziliensisbelow 100 µM. To our knowledge, compounds1and2are being described for the first time.


2021 ◽  
Vol 20 (1) ◽  
pp. 105-111
Author(s):  
Olorunfemi Abraham Eseyin ◽  
Iweh Emmanuel Etim ◽  
Emmanuel E. Attih ◽  
Ekarika Johnson ◽  
Aniefiok Sunday Udobre ◽  
...  

Purpose: To evaluate the antiplasmodial effects of eleven plants (Bombax buonopozense, Carica papaya, Anthocleista djalonensis, Milicia excelsa, Heterotis rotundifolia, Homalim letestui, Starchystarpheta cayennnensis, Ocimum gratissimum, Cleistopholis patens, Chromolaena odorata and Hippocratea africana) reportedly used in the treatment of malaria in Akwa Ibom State of Nigeria. Methods: Phytochemical analysis was done by standard methods, while in vitro antiplasmodial evaluation was carried out using Plasmodium falciparum chloroquine-sensitive and chloroquineresistant strains using lactate dehydrogenase (pLDH) assay.  Cytotoxicity test was undertaken by MTT assay on LLC-MK2 cells and the concentration killing 50 % of the cells (CC50) was calculated.Antioxidant activity of the ethanol extract was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Results: Milicia excelsa, Heterotis rotundifolia and Chromolaena odorata had moderate antiplasmodial activity. Ocimum gratissimum and Hippocratea africana were weakly active. Milicia excelsa showed a considerable level of cytotoxicity, while Bombax buonopozense exhibited moderate cytotoxicity. Bombax buonopozense (95.3 %) and Ocimum gratissimum (92.0 %) exhibited high DPPH scavengingeffect comparable to Vitamin C (98.7 %). There was a significant correlation (p < 0.05) between DPPH inhibition and the total phenolic contents of the eleven plants studied (r2 = 0.6616), between DPPH inhibition and flavonoids (r2 = 0.3553), between antiplasmodial activity and saponin content (r2= 0.3992), and between the two antiplasmodial evaluation assay methods (r2 = 0.614).Conclusion: The results of this work provide some justification for the use of Milicia excelsa, Heterotis rotundifolia, Chromolaena odorata, Ocimum gratissimum and Hippocratea africana in the treatment of malaria. Keywords: Antiplasmodial, Antioxidant, Cytotoxicity, Phytochemicals, Antimalaria


2016 ◽  
Vol 11 (2) ◽  
pp. 389 ◽  
Author(s):  
Kerem Canli ◽  
Ergin Murat Altuner ◽  
Ilgaz Akata ◽  
Yavuz Turkmen ◽  
Ugur Uzek

<p class="Abstract">The aim of this study was to investigate the antimicrobial activity of <em>Lycoperdon lividium</em> against 17 bacterial and 1 fungal strains and analyse the composition of ethanol extracts by GC/MS. The in vitro antimicrobial activity of <em>L. lividium</em> extracts having 15 mg/mL concentration was assessed against a wide range of strains by disk diffusion method. The ethanol extract of <em>L. lividium</em> had antimicrobial activity against several microorganism tested, but it was active especially against <em>S. carnosus</em>. The results obtained herein indicate that <em>L. lividium</em> contains several active metabolites.</p><p class="Abstract">Video clip</p><p><a href="https://youtube.com/v/ymWOQBeNN84">Disk diffusion test</a>: 7 min 11 sec</p>


2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Harish C. Upadhyay ◽  
Brijesh S. Sisodia ◽  
Harveer S. Cheema ◽  
Jyoti Agrawal ◽  
Anirban Pal ◽  
...  

The roots, leaves and stems of Christia vespertilionis were separately and successively extracted with methanol and aqueous-methanol (1:4, v/v) and were evaluated in vitro for their antiplasmodial potential against Plasmodium falciparum NF-54. The aqueous-methanolic stem (AS) extract was the most active (IC50 7.5 μg/mL) followed by the methanolic leaf (ML) extract (IC50 32.0 μg/mL). The in vivo antimalarial activity of the combined plant extract of C. vespertilionis was also assessed in P. berghei infected mice, which showed 87.8% suppression of parasitaemia as compared with complete suppression by chloroquine on day 8. Finally, detailed chemical investigation of C. vespertilionis resulted in the isolation and characterization of fifteen compounds (1–15), of which two (1 and 4) are being reported for the first time from nature. The novel compound 1 possesses potent antiplasmodial activity (IC50 = 9.0 μg/mL).


2018 ◽  
pp. 16
Author(s):  
Olorunshola Dave Omodamiro ◽  
Chinedu Nwankwo

Chrysophyllum albidum G. is generally regarded as a plant with many ethno-medicinal uses. The study was aimed at evaluating the in vitro antioxidant, diuretic, and hypoglycemic properties of the ethanol extract of leaves of C. albidum Male Wistar albino rats weighing between 150g and 200g were used for the experiment. The DPPH scavenging activity was determined using DPPH assay, inhibition of lipid peroxidation was carried out using the reactions of peroxides with thiobarbituric acid, while nitric oxide was conducted based on the Greiss reaction. Diuretic activity was carried out using the method of Lipschitz with slight modifications. Alloxan (140 mg/kg) was used to induce diabetes in the rats. The extract showed a concentration-dependent increase in DPPH radical scavenging activity, anti-lipid peroxidation activity, and nitric oxide inhibition activity maximal at 200 mg/ml (84.99±7.97, 79.82±6.10, 69.99±2.22 respectively) and this was significant (p<0.05) when compared with that of 100 mg/ml of vitamin C (97.68±0.84, 99.05±0.24 and 98.15±0.29 respectively) which served as the control. The extract also significantly (p<0.05) increased; urine volume, urinary sodium, and urinary chloride particularly at 2000 mg/kg (1.55±0.07, 109.60±0.57, and 106.00±1.41 respectively) when compared with the standard drug (1.85±0.07, 115.20±0.57, and 112.85±0.49 respectively). The increase in potassium excretion was also significant (p<0.05) particularly at 2000 mg/kg (13.70±0.28) but less than those of sodium (109.60±0.57) and chloride (106.00±1.41) at the same concentration. There was no significant (p<0.05) increase in urinary bicarbonate the maximum being at 250 mg/kg (22.55±0.78). The extract caused a non-significant (p<0.05) decrease in the fasting blood glucose level of the rats. It was concluded that the leaves of C. albidum could be used as a source of natural antioxidant boosters and also a diuretic.


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