scholarly journals Mangifera indica Extracts as Novel PKM2 Inhibitors for Treatment of Triple Negative Breast Cancer

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Azhar Rasul ◽  
Ammara Riaz ◽  
Wei Wei ◽  
Iqra Sarfraz ◽  
Mudassir Hassan ◽  
...  

Pyruvate kinase (PK), a key enzyme that determines glycolytic activity, has been known to support the metabolic phenotype of tumor cells, and specific pyruvate kinase isoform M2 (PKM2) has been reported to fulfill divergent biosynthetic and energetic requirements of cancerous cells. PKM2 is overexpressed in several cancer types and is an emerging drug target for cancer during recent years. Therefore, this study was carried out to identify PKM2 inhibitors from natural products for cancer treatment. Based on the objectives of this study, firstly, plant extract library was established. In order to purify protein for the establishment of enzymatic assay system, pET-28a-HmPKM2 plasmid was transformed to E. coli BL21 (DE3) cells for protein expression and purification. After the validation of enzymatic assay system, plant extract library was screened for the identification of inhibitors of PKM2 protein. Out of 51 plant extracts screened, four extracts Mangifera indica (leaf, seed, and bark) and Bombex ceiba bark extracts were found to be inhibitors of PKM2. In the current study, M. indica (leaf, seed, and bark) extracts were further evaluated dose dependently against PKM2. These extracts showed different degrees of concentration-dependent inhibition against PKM2 at 90-360 μg/ml concentrations. We have also investigated the anticancer potential of these extracts against MDA-MB231 cells and generated dose-response curves for the evaluation of IC50 values. M. indica (bark and seed) extracts significantly halted the growth of MDA-MB231 cells with IC50 values of 108 μg/ml and 33 μg/ml, respectively. Literature-based phytochemical analysis of M. indica was carried out, and M. indica-derived 94 compounds were docked against three binding sites of PKM2 for the identification of PKM2 inhibitors. The results of in silico based screening have unveiled various PKM2 modulators; however, further studies are recommended to validate their PKM2 inhibitory potential via in vitro biochemical assay. The results of this study provide novel findings for possible mechanism of action of M. indica (bark and seed) extracts against TNBC via PKM2 inhibition suggesting that M. indica might be of therapeutic interest for the treatment of TNBC.

2018 ◽  
Vol 25 ◽  
pp. 27-37
Author(s):  
N Rashid ◽  
AA Paul ◽  
S Islam ◽  
SA Sajib ◽  
K Nasirujjaman ◽  
...  

Medicinal plant extract has long been used successfully in ‘unani’ or ‘ayurvedic’ medicine. Medicinal plant extract contains bioactive molecules and activity of these molecules may help to mitigate, eradicate or cure diseases. In the advent for the search for new medicinally important bioactive molecule, the current paper deals with the anti-oxidative, cytotoxic and phytochemical analysis of Scoparia dulcis leaf and root, Curculigo orchioides root, Pandanus fascicularis root and Baccaurea sapida leaf extract. Aqueous and methanolic extracts were made for each of the extracts where they posses significant antioxidative properties. High activities were seen in P. fascicularis and S. dulcis plant extract where IC50 values were 21.87 μg/ml and 173.36 μg/ml respectively. In toxicity test, only P. fascicularis extracts showed lethality in a dose-dependent manner where the LD50 value was 25.64 μg/ml. By the phytochemical analysis, it was found that each of these plant species possesses glycosides, protein, carbohydrates, alkaloid, flavonoid etc. which are pharmacologically active biomolecules. These important properties of those plants showed an indication that these plants can further be tested for the utilization in therapeutic purpose or in cosmetic industry.J. bio-sci. 25: 27-37, 2017


Author(s):  
Karunanithi M ◽  
David Raj C ◽  
Brindha P ◽  
Jegadeesan M ◽  
Kavimani S

Objective: The aim was to study the antiparkinson activity in the seed extracts of four species of Mucuna.Methods: The hydroalcoholic extracts of seeds of four species of Mucuna were evaluated for antiparkinson activity of after a preliminary phytochemical study. The activity was measured in rats by indirectly measuring the decrease in malondialdehyde level, decrease in tongue protrusion frequency, and reduction in vacuous chewing movement after administering reserpine at the dose of 1 mg/kg. The dose levels of four species of Mucuna seed extract were kept at 100, 200, and 300 mg/Kg.Results: Extracts exhibited potent antiparkinson activity and achieved statistically significant p values compared with control group. The study corroborates and compares all four species of Mucuna. Conclusion: Among the extracts, the highest percentage of antiparkinson activity was recorded for Mucuna pruriens.


Author(s):  
Kavitha S ◽  
Parthasarathi Perumal

 Objective: The present study was undertaken to assess the α-amylase inhibitory activity and antidiabetic experimental catfish model and antioxidant properties of Piper betle L. ethanolic (PBE) extract.Methods: The phytochemical analysis of PBE extract was performed. The PBE extract was tested for their inhibitory effect on the α-amylase assay, which compared to the control, acarbose. The absorbance was read at 540 nm using a spectrophotometer, and IC50 values were calculated. In this present investigation, diabetes mellitus was induced in catfish, Clarias gariepinus by epaxial musculature injection to glucose and standard drug, Metformin hydrochloride. After 24-h incubation, the treated fishes were dissected, and the blood, liver, tissue samples, and epaxial musculature regions were collected. In addition, the antioxidant properties of PBE were determined by 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical scavenging and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging (ABTS) assays.Results: The phytochemical screening of PBE revealed the presence of alkaloid, flavonoids, tannins, phenol, glycosides, sterols, saponins, and quinines. Furthermore, the values of (μg/ml) 3.038 and 7.672 α-amylase enzyme inhibition were excellent activity when compared to the acarbose. Moreover, elevated the glucose level (mg/dl) was estimated in blood 1.9±0.35, liver 0.5±0.25, tissue 0.2±0.25, and epaxial musculature 0.8±0.2 after 24-h incubation. The antioxidant effect of maximum activity was found in PBE; IC50 values (μg/ml) of DPPH and ABTS were 9.362 and 6.606, respectively.Conclusions: These studies might be responsible for the P. betle L. that was used as the new source of antidiabetic and antioxidant agents. 


Author(s):  
Media Fitri Isma Nugraha ◽  
Hessy Novita ◽  
Muh Alias Rajamuddin ◽  
Rossa Yunita ◽  
Wening Enggarini ◽  
...  

This study was aimed to identify the potential use of active compounds extracted from Staurogyne sp as an antibacterial agent to control disease-causing bacteria in fish. Staurogyne sp, an aquatic plant collected from Bantimurung, South Sulawesi were subjected to allelochemical compound. Plant extracts were tested to five bacteria including four types of bacterial pathogen, such as Aeromonas hydrophilla, Edwardsiella ictaluri, Streptococcus agalactiae, and Flavobacterium columnare, and one bacterial sensing quoroum, Chromobacterium violaceum. Based on phytochemical analysis, Staurogyne’s extracts derived from both stem and root contained flavonoids, phenols, and antioxidants compounds with the concentration of 0.018 mgQE/g, 0.3471 mgGAE/g, and  1004,391 IC50 µg/mL, respectively. In addition, Staurogyne plant extracts derived from both their stem and root has also produced both saponins and glycosides compounds. Plant extracts derived from Staurogyne’s leaves revealed three major chemical compounds such as flavonoids (0.77 mgQE/g), phenol (0.0629 mgGAE/g), and glycosides (+). However, no antioxidants and saponin compounds were detected.  Applying plant extracts as an antibacterial on five disease-causing bacteria causing diseases in aquaculture, such as Aeromonas Hydrophilla, Edwardsiella ictaluri, Streptococcus agalactiae, Flavobacterium columnare, and Chromobacterium violaceum bacterials revealed that at concentration of 0.1 g the Staurogyne sp extracts did not influence all the bacterials growth. However, by application of plant extract at concentration of 0.2 g on the growth media,three out of 5 tested bacterials (Aeromonas hydrophilla, Edwardsiella ictaluri, and Streptococcus agalactiae) showed intermediate inhibition responses on bacterial growth. The growth of remaining two bacterials pathogen, Flavobacterium columnare and Chromobacterium violaceum at 0.2 g plant extract of Staurogyne sp was not affected. This study revealed that the use of active compound derived from Staurogyne sp would be potential to be used in inhibiting disease-causing bacterial in fish in future. However, optimum concentration of the plant extracts, in particular on the inhibition of the growth of disease-causing bacteria in fish is still needed to adjust.Key words: Antibacterial, aquatic plant, Staurogyne sp, fish disease


Author(s):  
Mukesh S Sikarwar ◽  
Chew Khai Szeek ◽  
Neeraj Paliwal

Background: Herbal medicine mostly contains wide range of chemical compounds responsible for medicinal therapeutic use. Costus woodsonii is commonly called as Red Button Ginger and synonyms of the botanical name are Costus spiralis, Alpinia spiralis and Costus pisonis. In Malay, it is known as Setawar Halia Merah. In Chinese, it is known as Hong Bi Qiao Jiang. Objective: This research was conducted to study the pharmacognostical, phytochemical, antioxidant and antimicrobial activity of C. woodsonii leaf extracts. Method: Macroscopy, microscopy, phytochemical analysis, thin layer chromatography, antioxidant activity and antimicrobial activity of C. woodsonii leaf were carried out. Total flavonoids were estimated in the leaf extract. The total phenolic content of C. woodsonii leaf was determined using Folin-Ciocalteu reagent. The antioxidant activity of leaf extract of C. woodsonii was determined by performing DPPH radical scavenging. The microbial activity was determined by Well diffusion test, MIC (Minimum Inhibitory Concentration) test and MBC (Minimum Bactericidal Concentration) test. Result and Discussion: C. woodsonii belongs to costaceae with elliptical green leaves. Till now are no extensive studies on C. woodsonii. Preliminary phytochemical analysis revealed the presence of flavonoid, steroid, fat, phenol, tannin and mucilage in leaf extract. Physicochemical studies further revealed the ash value of leaf as 8.7%. Among the three extractions, alcohol extractive values showed the highest as 13%. Loss on drying at 105 degree Celsius in leaf was found to be 12.67%. The plant extract showed total phenolic content of 7.941 mg GAE/g at concentration of 5µg/ml. As for flavonoids content, plant extract showed 21.7 mg RE/g at concentration of 200µg/ml and 43.4 mg RE/g at concentration of 400µg/ml. For antioxidant activity, the plant extract showed weak antioxidant activity in DPPH scavenging activity assay. For antimicrobial test, the leaf extract of C. woodsonii showed weak antimicrobial activity. Conclusion: From this study, it can conclude that C. woodsonii leaf extract possess weak antioxidant activity and weak antimicrobial activity which need to be further validated by using more antioxidant assays and antimicrobial tests.


2021 ◽  
Vol 8 (4) ◽  
Author(s):  
Hashini Imalsha Abeysuriya ◽  
Vajira P Bulugahapitiya ◽  
Loku Pullukkutige Jayatissa

Sri Lanka is a habitat of diverse fruit varieties; nevertheless 95% of them are underutilized by people due to unawareness of their nutritional values and health aspects, and hence become ‘minor fruits’. This study was aimed on revealing vitamin C, iron and antioxidant contents of 29 varieties of minor fruits (MFs) with the comparison of the same with three best commonly consumable fruits (CFs), namely Carica papaya, Mangifera indica and Psidium guajava. Ascorbic acid (Asc), dehydroascorbic acid (DAsc), vitamin C (TC), phenolic (TP), flavonoid (TF), iron (Fe) contents and antioxidant capacities (AOCs) of fruits were determined using standard methods. The results of mean Asc, DAsc, TC, TP, TF and Fe contents in 100 gm of MFs ranged from 3.1 to 121.5 mg, 1.2 to 70.7 mg, 6.6 to 136.1 mg, 24.9 to 1613.3 mg Gallic acid equivalent, 6.2 to 228.0 mg Quercetin equivalents and 0.2 to 4.9 mg respectively. DPPH and Ferric Reducing Antioxidant Power (FRAP) assays were used for AOCs and variation of IC50 values in a DPPH assay was 1.2 to 245.4 mg/ml whereas FRAP values ranged from 9.6 to 486.7 ?mol FeSO4/gm. Among the studied minor fruits, Melastoma malabathricum (Maha bovitiya/ Malabar melastome) is found as the best respect to all considered parameters. As a conclusion, it can be stated that, the Sri Lankan minor fruits are good alternatives to the common fruits as they are recognized as good source of vitamin C, iron and higher content of antioxidants. As an outcome, Sri Lankan minor fruits can be promoted as alternatives to common fruits and as source of revenue for national economy.


Author(s):  
Nerlis Paola Pajaro Castro ◽  
Clemente Granados Conde ◽  
Miladys Esther Torrenegra AlarcÓn ◽  
MarÍa Del Rosario Osorio Fortich ◽  
Enilson JÓse Pajaro Castro ◽  
...  

Introduction: For the food industry and trade, it is very important to obtain powders based on fruits or vegetables by means of drying techniques that allow them to preserve their nutritional, organoleptic properties and also extend the life time by offering new commercialization possibilities. Studies have made it possible to optimize drying techniques by obtaining water-free products in more than 80% with a high commercial value. To microencapsulate the mango pulp (Mangifera indica L) flounder variety by the Spray Drying method and to evaluate its potential antioxidant activity.Methodology: The fruits were collected in the municipality of Turbana - Bolívar (10º 16 '22 "N 75º 26' 38" W), Colombia. The pulps obtained from the healthy fruits were microencapsulated by the spray drying method. The obtained microcapsules were measured the particle size and the mineral content was determined. The antioxidant activity was determined by three methodologies: total phenols, DPPH • and ABTS • +.Results: The results obtained demonstrate that the microcapsules of the mango pulp (M. indica L) have a mineral content in the following order of importance Calcium> Phosphorus> Iron. The IC50 values for the DPPH • and ABTS • assay were found to be 110.54 ± 1.5 μg / mL and 65.33 ± 1.0 μg / mL respectively. The total phenol content was 73.11 ± 1.54 mg AG / 100 mg of microcapsules, which may be related to the antioxidant activity.Conclusion: The spray drying method was a suitable technique to microcapsulate the mango pulp (M.indica L), which were shown to possess antioxidant activity.


2016 ◽  
Vol 2 (1) ◽  
pp. 01-10 ◽  
Author(s):  
Anju Mathew ◽  
A Malar Retna

Scoparia dulcis Linn has been widely reported to have pharmacological uses arising from its wide spread uses. The different extracts were prepared by successive extraction with petroleum ether, chloroform, ethanol and water using soxhlet distillation method. Phytochemical analysis of plant extract revealed the presence of alkaloids, carbohydrates, glycoside, tannins, starch etc.Thin layer chromatography and Gas chromatography-mass spectrometric analysis revealed the presence of different components in the plant extract. Among the 50 components obtained, 10 important organic compounds were analyzed. All these compounds are found to be having some medicinal application.UV visible spectroscopic analysis of extract of Scoparia dulcis reported four chromatogram figures which showed prominent peaks having maximum absorption of 666 nm corresponded to wavelength of methylene blue and brilliant blue. FTIR spectroscopic analysis reveals the presence of important functional groups like-OH,-NO2,-SO3,-SH, -COOH, NH2, R-X etc. Antibacterial activity of petroleum ether, chloroform, and ethanol and water extracts of stems and leaves of Scoparia dulcis reveals that chloroform and ethanol extracts shows maximum resistance against Staphylococcus while ethanol and aqueous extracts showed maximum resistance against Klebsiela pneumonia.The exciting fact came out of the study is that water extract of Scoparia dulcis showed great potential to dissolve the Calcium oxalate crystals ie, the plant extract shows invitro antilithiatic activity for kidney stones. Thus Scoparia dulcis act as a source of different valuable organic compounds that are having medicinal applications and have a beneficial effect on kidney stone problem.


2014 ◽  
Vol 20 (1) ◽  
pp. 19-28 ◽  
Author(s):  
B. Jayalakshmi ◽  
K.A. Raveesha ◽  
K.N. Amruthesh

Antibacterial activity of aqueous and solvent extracts of E. cotinifolia leaves were tested against some human pathogenic bacteria viz. Escherichia coli, Klebsiella pneumonia, Bacillus subtilis, Bacillus cereus, Salmonella typhi, Enterobacter aerogenes and Staphylococcus aureus by agar cup diffusion and broth microdilution methods. Antioxidant properties were evaluated for different solvent extracts by diphenyl picryl hydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide methods and IC50 values were calculated and compared with the standard ascorbic acid and butylated hydroxyanisole. Among the aqueous and organic solvent extracts, methanol and ethyl acetate, showed significant activity against B. subtilis and E. aerogenes which recorded a maximum inhibition zone of 17.25 mm. Minimum inhibitory concentration of methanol and ethyl acetate extracts for different bacteria ranged from 0.3- 1.25 mg/mL. In DPPH method, IC50 values of chloroform, petroleum ether, ethyl acetate and methanol were found to be 15, 17, 18 and 19 mg/mL, respectively, lesser than the standard, ascorbic acid (25 mg/mL). Phytochemical analysis of aqueous, ethyl acetate and methanol extract showed the presence of flavonoids, terpenoids, tannins and steroids. Further work is in progress to isolate the active compound(s).


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