scholarly journals In Vitro Potential of the Acetone Leaf Extract and Fractions of Psychotria capensis (Eckl.) Vatke (Rubiaceae) to Combat Co-Infection of Tuberculosis and Helminthiasis

2022 ◽  
Vol 12 ◽  
Author(s):  
Abimbola O. Aro ◽  
Ibukun M. Famuyide ◽  
Ademola A. Oyagbemi ◽  
Prudence N. Kabongo-Kayoka ◽  
Lyndy J. McGaw

Tuberculosis (TB) is a disease of global importance that affects millions of people. Approximately a quarter of the world’s population is currently infected with M. tuberculosis, and about 10% of those infected will develop into active disease, particularly immune compromised individuals. Helminthiasis is of global health importance, affecting over 2 billion people mostly in resource-poor countries. Co-infection with tuberculosis (TB) and helminths (worms) is an emerging global public health concern with both affecting about one-third of the global population. Chronic infection with helminths can result in impaired immune responses to TB as well as enhancing failure to TB therapy and BCG vaccination. Antimycobacterial and anthelmintic activities of the acetone extract and fractions of Psychotria capensis were evaluated, including their in vitro safety. In addition, the anti-inflammatory and immunomodulatory effect of the fractions and crude extract of P. capensis were assessed. Antimycobacterial activity of the extract and fractions was tested against four non-tuberculous mycobacteria (Mycobacterium smegmatis, M. fortuitum, M. aurum, M. bovis BCG) and pathogenic M. tuberculosis H37Rv while the Egg Hatch Assay (EHA) was used for the anthelmintic test on eggs of Haemonchus contortus. Cytotoxicity was determined against Vero kidney cells while in vitro immune modulation via cytokine production was determined on activated macrophages. The minimum inhibitory concentration (MIC) values of the Psychotria capensis acetone extract and fractions ranged from 39 to 1,250 μg/ml with the crude extract and hexane fraction having the best MIC values (both 39 μg/ml). In the EHA, the inhibitory concentration (IC50) ranged from 160 to 630 μg/ml with the hexane fraction having the best activity. The hexane and chloroform fractions were relatively non-toxic with LC50 values of 290 and 248 μg/ml respectively, while the acetone crude extract (64 μg/ml) and n-butanol fraction (71 μg/ml) were moderately toxic. The SI values (LC50/MIC) ranged from 0.1 to 7.4 with the hexane fraction having the highest value against M. smegmatis (7.4). The hexane fraction had the best dual anthelmintic and antimycobacterial activity. This fraction had the best NO inhibitory activity and was the least cytotoxic, indicating that its activity was not due to general metabolic toxicity, with 96.54% cell viability. Pro-inflammatory cytokines such as IL-12p70 were upregulated while IL-10 expression was inhibited by the extracts. Compounds were detected using GC-MS analysis, and in both the crude acetone extract and the hexane fraction was the diterpene neophytadiene, which has anti-inflammatory and antimicrobial activity. Finding alternative or complementary approaches to dealing with TB infections by, amongst other things, reducing the incidence of helminth infestations may lessen the burden of TB, contributing to slowing the spread of multi-drug resistance.

Author(s):  
Dian Ayu Eka Pitaloka ◽  
Elin Yulinah Sukandar

Objective: The resurgence of tuberculosis (TB) caused by Mycobacterium TB (MTB) is associated with the rapid spread of multidrug-resistant,therefore, the development of new antimycobacterial agents is necessary. The aim of this study was to evaluate the antimycobacterial activity ofursolic acid (UA) when it using alone and combination with TB drugs.Methods: MTB H37Rv strain, streptomycin-rifampicin resistant strain, and isoniazid-ethambutol resistant strain were evaluated by susceptibility testusing a serial number of UA (25-150 µg/mL). Minimum inhibitory concentration (MIC) was read as minimum concentration of drugs that completelyinhibit visible growth of organism. Activities of drug combination of UA with TB drug were determined in Lowenstein-Jensen media by calculatingthe fractional inhibitory concentration index.Results: The results showed that MIC of UA was 50 µg/mL against three different strains of MTB. The combination of UA and TB drugs displayedsynergistic interaction, and no antagonism result from the combination was observed for strains of MTB.Conclusion: These results indicate that UA may serve as a promising lead compound for future antimycobacterial drug development.Keywords: Ursolic acid, Tuberculosis, Drug combination, Susceptibility test


2015 ◽  
Vol 13 (1) ◽  
pp. 69-73
Author(s):  
Md Abul Khair ◽  
Mohammed Ibrahim ◽  
Qamrul Ahsan ◽  
Md Ruhul Kuddus ◽  
Ridwan Bin Rashid ◽  
...  

The methanol extract of the whole plant of Blumea lacera (Burn.f.) DC. (BLME) has been subjected to preliminary screenings for phytoconstituents and antipyretic, analgesic and anti-inflammatory activities. Antipyretic activity was assessed by the yeast-induced hyperthermia in mice. The analgesic property was evaluated by formalin-induced writhing test. Acetyl salicylic acid (ASA) was used as standard for in-vitro anti-inflammatory activity test. In yeast-induced pyrexia, the crude extract demonstrated a significant (p=0.05) reduction in body temperature of mice after elevation by the administration of yeast. These effects were pronounced at the 2nd and 3rd h of post-treatment with the extract. BLME exhibited a dose-dependent analgesic activity with 39.13% and 56.52% protection at 200-and 400-mg/kg, b.w., respectively as compared to 76.09% revealed by the standard diclofenac sodium. In the anti-inflammatory test, the crude extract at 400 ?g/ml displayed 62.40% inhibition of protein denaturation whereas standard acetyl salicylic acid exhibited 76.74% inhibition. Results of the preliminary phytochemical screenings demonstrated the presence of alkaloids, flavonoids and triterpenoids in the extract. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21863 Dhaka Univ. J. Pharm. Sci. 13(1): 69-73, 2014 (June)


2018 ◽  
Vol 315 (2) ◽  
pp. G231-G240 ◽  
Author(s):  
Thomas K. Hoang ◽  
Baokun He ◽  
Ting Wang ◽  
Dat Q. Tran ◽  
J. Marc Rhoads ◽  
...  

Lactobacillus reuteri DSM 17938 (LR 17938) has been shown to reduce the incidence and severity of necrotizing enterocolitis (NEC). It is unclear if preventing NEC by LR 17938 is mediated by Toll-like receptor 2 (TLR2), which is known to mediate proinflammatory responses to bacterial cell wall components. NEC was induced in newborn TLR2−/− or wild-type (WT) mice by the combination of gavage-feeding cow milk-based formula and exposure to hypoxia and cold stress. Treatment groups were administered formula supplemented with LR 17938 or placebo (deMan-Rogosa-Sharpe media). We observed that LR 17938 significantly reduced the incidence of NEC and reduced the percentage of activated effector CD4+T cells, while increasing Foxp3+ regulatory T cells in the intestinal mucosa of WT mice with NEC, but not in TLR2−/− mice. Dendritic cell (DC) activation by LR 17938 was mediated by TLR2. The percentage of tolerogenic DC in the intestine of WT mice was increased by LR 17938 treatment during NEC, a finding not observed in TLR2−/− mice. Furthermore, gut levels of proinflammatory cytokines IL-1β and IFN-γ were decreased after treatment with LR 17938 in WT mice but not in TLR2−/− mice. In conclusion, the combined in vivo and in vitro findings suggest that TLR2 receptors are involved in DC recognition and DC-priming of T cells to protect against NEC after oral administration of LR 17938. Our studies further clarify a major mechanism of probiotic LR 17938 action in preventing NEC by showing that neonatal immune modulation of LR 17938 is mediated by a mechanism requiring TLR2. NEW & NOTEWORTHY Lactobacillus reuteri DSM 17938 (LR 17938) has been shown to protect against necrotizing enterocolitis (NEC) in neonates and in neonatal animal models. The role of Toll-like receptor 2 (TLR2) as a sensor for gram-positive probiotics, activating downstream anti-inflammatory responses is unclear. Our current studies examined TLR2 −/− mice subjected to experimental NEC and demonstrated that the anti-inflammatory effects of LR 17938 are mediated via a mechanism requiring TLR2.


Author(s):  
Sucheta Singh ◽  
Surjeet Verma ◽  
Dharmendra Kumar Yadav ◽  
Anant Kumar ◽  
Rekha Tyagi ◽  
...  

Introduction: Endophyte is considered as a source of natural bioactive secondary metabolites that provides an array of bioactive lead compounds. The present study was aimed to determine the antimicrobial and anti-inflammatory potential of fungal endophytes isolated from Catharanthus roseus. Methods: A total of seven fungal endophytes crude extract were screened against bacterial pathogens. Of these, Curvularia geniculata CATDLF7 crude extract exhibited the most potent inhibitory activity against bacterial pathogen. Hence, CATDLF7 crude extract was subjected to the chromatographic separation. This purification leads to the isolation of six pure compounds (1PS - 6PS). Of these, 3PS was found to be a major constituent and most effective against clinical isolates of methicillin resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) values ranging from 100 to 200 μg/ml. Based on the spectroscopic data, 3PS was characterized as α,β-dehydrocurvularin. This compound also showed synergistic interaction with norfloxacin, and reduced its MIC up to 32-folds with fractional inhibitory concentration index (FICI) of 0.09. Results: To understand the possible antibacterial mechanism of action, α,β-dehydrocurvularin alone (100 μg/ml) exhibited efflux pump inhibitory potential by 0.84 fold decreasing in ethidium bromide (EtBr) fluorescence. In addition, α,β-dehydrocurvularin inhibited inflammatory cytokines TNF-α and IL-6 production which is further validated by molecular docking score -4.921 and -5.641 respectively for understanding orientation and binding affinity. Conclusion: Overall the results highlighted to identifying bioactive compound α,β-dehydrocurvularin which could be used as an antimicrobial and anti-inflammatory agents.


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Tamires Rocha Falcão ◽  
Aurigena Antunes de Araújo ◽  
Luiz Alberto Lira Soares ◽  
Iuri Brilhante de Farias ◽  
Wliana Alves Viturino da Silva ◽  
...  

Background.Libidibia ferrea(L. ferrea)is found throughout the northeastern region of Brazil, where it has been used in folk medicine with beneficial effects on many inflammatory disorders.Purpose. This study investigated the phytochemical composition of the crude extract and fractions ofL. ferreafruit and evaluated its anti-inflammatory and antinociceptive activitiesin vivoand effect on cell viabilityin vitro.Methods. Characterization of polyphenols present in crude extract (CE), hydroalcoholic fractions of 20-80% ethanol (CE20, CE40, CE60, and CE80), aqueous fraction (AqF), and ethyl acetate (EAF) fractions ofL. ferreafruit was performed by chromatographic analysis.Anti-inflammatory activity was evaluated by using a carrageenan-induced peritonitis model submitted to a leukocyte migration assay and myeloperoxidase activity (MPO) analysis. Total glutathione and malondialdehyde (MDA) levels were assessed to evaluate the oxidative stress level. Antinociceptive activity was evaluated by acetic acid-induced abdominal writhing and hot plate test.In vitrocell viability was determined by using MTT assay in a mouse embryonic fibroblast cell line (3T3 cells).Results. Chromatography revealed the presence of ellagic acid content in EAF (3.06), CE (2.96), and CE40 (2.89). Gallic acid was found in EAF (12.03), CE 20 (4.43), and CE (3.99).L. ferreacrude extract and all fractions significantly reduced leukocyte migration and MPO activity (p<0.001).L. ferreaantioxidant effect was observed through high levels of total glutathione and reduction of MDA levels (p<0.001). Acetic acid-induced nociception was significantly inhibited after administration ofL. ferreacrude extract and all fractions (p<0.001). Crude extract and all fractions significantly increased the viability of the 3T3 cell line (p<0.05).Conclusions. The appropriate extraction procedure preserves the chemical components ofL. ferreafruit, such as gallic acid and ellargic acid. Crude extract and fractions ofL. ferreafruit exhibited anti-inflammatory, antioxidant, antinociceptive activitiesin vivoand enhanced cell viabilityin vitro.


2010 ◽  
Vol 56 (6) ◽  
pp. 487-494 ◽  
Author(s):  
Duncan Webster ◽  
Timothy D.G. Lee ◽  
Jill Moore ◽  
Tracy Manning ◽  
Dennis Kunimoto ◽  
...  

Multidrug-resistant Mycobacterium tuberculosis strains have rapidly become a global health concern. North American First Nations communities have used traditional medicines for generations to treat many pulmonary infections. In this study, we evaluated the antimycobacterial activity of 5 medicinal plants traditionally used as general therapeutics for pulmonary illnesses and specifically as treatments for tuberculosis. Aqueous extracts of Aralia nudicaulis , Symplocarpus foetidus , Heracleum maximum , Juniperus communis, and Acorus calamus were screened for antimycobacterial activity against Bacillus Calmette–Guérin, Mycobacterium avium, and M. tuberculosis H37Ra using the colorimetric microplate resazurin assay. Extracts of Acorus calamus and H. maximum root demonstrated significant antimycobacterial activity comparable to that of the rifampin control (2 µg/mL). Evaluation of the cytotoxicity of these 2 extracts using the MTT assay also showed that the extracts were less toxic to 3 human cell lines than was the DMSO positive control. This study demonstrates that aqueous extracts of the roots of H. maximum and Acorus calamus possess strong in vitro antimycobacterial activity, validates traditional knowledge, and provides potential for the development of urgently needed novel antituberculous therapeutics.


Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1059
Author(s):  
Marianna Pauletto ◽  
Mery Giantin ◽  
Roberta Tolosi ◽  
Irene Bassan ◽  
Andrea Barbarossa ◽  
...  

Aflatoxin B1 (AFB1) toxicity in livestock and human beings is a major economic and health concern. Natural polyphenolic substances with antioxidant properties have proven to be effective in ameliorating AFB1-induced toxicity. Here we assessed the potential anti-AFB1 activity of curcumin (pure curcumin, C, and curcumin from Curcuma longa, CL) in a bovine fetal hepatocyte-derived cell line (BFH12). First, we measured viability of cells exposed to AFB1 in presence or absence of curcumin treatment. Then, we explored all the transcriptional changes occurring in AFB1-exposed cells cotreated with curcumin. Results demonstrated that curcumin is effective in reducing AFB1-induced toxicity, decreasing cells mortality by approximately 30%. C and CL induced similar transcriptional changes in BFH12 exposed to AFB1, yet C treatment resulted in a larger number of significant genes compared to CL. The mitigating effects of curcuminoids towards AFB1 toxicity were mainly related to molecular pathways associated with antioxidant and anti-inflammatory response, cancer, and drug metabolism. Investigating mRNA changes induced by curcumin in cattle BFH12 cells exposed to AFB1 will help us to better characterize possible tools to reduce its consequences in this susceptible and economically important food-producing species.


Planta Medica ◽  
2020 ◽  
Author(s):  
Raymond Muganga ◽  
Joanne Bero ◽  
Joëlle Quetin-Leclercq ◽  
Luc Angenot ◽  
Monique Tits ◽  
...  

AbstractThis study aims at determining the in vitro antitrypanosomal, antileishmanial, antioxidant, and anti-inflammatory-like activities of Terminalia mollis root crude extracts. The antitrypanosomal and antileishmanial activities on Trypanosoma brucei brucei (strain 427) and promastigotes of Leishmania mexicana mexicana (MHOM/BZ/84/BEL46) were evaluated in vitro. The methanolic root bark extract and standards were profiled by HPLC-PDA, and the majority of compounds identified using literature data. The in vitro antioxidant and anti-inflammatory-like activities were determined by evaluating the effect of crude extracts on reactive oxygen species produced by phorbol 12-myristate 13-acetate-stimulated equine neutrophils using lucigenin-enhanced chemiluminescence and on purified equine myeloperoxidase activity measured by specific immunological extraction followed by enzymatic detection. The methanolic, aqueous crude extract, and aqueous crude extract free of tannins exhibited good growth inhibition on Trypanosoma brucei brucei (IC50 3.72, 6.05, and 4.45 µg/mL respectively) but were inactive against Leishmania mexicana mexicana (IC50 > 100 µg/mL). Suramin (IC50 0.11 µg/mL) and amphotericin (IC50 0.11 µg/mL) were used as standard respectively for the antitrypanosomal and antileishmanial activity. Very interesting antioxidant and anti-inflammatory-like activities were observed with 50% hydroethanolic, aqueous crude extracts, and aqueous crude extract free of tannins as well as with pure punicalagin, gallic, and ellagic acid (IC50 0.38 – 10.51 µg/mL for 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid), chemiluminescence, and specific immunological extraction followed by enzymatic detection assays. The study results support traditional medicinal use of the plant for the treatment of parasitical disorders and revealed for the first time the antitrypanosomal potential, anti-inflammatory-like, and antioxidant activity of Terminalia mollis root.


Author(s):  
Novie E. Mauliku ◽  
Hendro W. ◽  
Suharyo Hadi Saputro ◽  
Tri N. Kristina

Objective: This study aimed to evaluate the antitubercular activity of extracts and compounds isolated of Morinda citrofolia Linn (noni) against Mycobacterium tuberculosis strains (H37Rv) with a dose of 10 mg/ml, 20 mg/ml, 30 mg/ml and 40 mg/ml. Methods: The noni fruits was extracted using 96% ethanol. A crude ethanol extract of noni tested by phytochemical fractionation to obtain flavonoids, alkaloids, scopoletin, and anthraquinone. Extract and active compounds of noni testing antibacterial activity against tuberculosis (H37RV) bacterial with a dose of 10 mg / ml, 20 mg / ml, 30 mg / ml and 40 mg / ml. This study was performed in vitro with laboratory-based experimental study. Statistical analysis was performed by analysis of variance.Results: Compounds of noni shown to have antitubercular activity in inhibiting the growth of MDR TB bacteria at various doses compared to controls (p = 0.00). The mean number of bacterial colonies on the MDR TB crude ethanol extract (59.0± 60.51), alkaloids (64.8 ± 49.36), anthraquinone (69.5 ± 50.40), flavonoids (72.9 ± 58.7), scopoletin (95.9 ± 33.3) and negative controls (189.3 ± 35.19). Crude extract, alkaloids, anthraquinones, and flavonoid have highly bactericidal inhibition than scopoletin and negative control. The exhibited minimum inhibitory concentration (MIC) against M. Tuberculosis on the compound of the noni fruit is at a dose of 40 mg / ml Conclusion: All compounds and extract of noni fruits represents a potent active anti-TB against M. tuberculosis strains. An crude extract of  noni was the most active compound against M. tuberculosis strains (H37RV). 


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