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In vitro antitrypanosomal and antileishmanial activity of plants used in Benin in traditional medicine and bio-guided fractionation of the most active extract
Abstract
The aim of the study was to evaluate the in vitro antitrypanosomal and antileishmanial activity of crude extracts of 10 plant species traditionally used in Benin to treat parasitic infections.
For each species, dichloromethane, methanol and aqueous extracts were tested. Their antitrypanosomal and antileishmanial activities were evaluated in vitro on Trypanosoma brucei brucei (strain 427) (Tbb) and on promastigotes of Leishmania mexicana mexicana (MHOM/BZ/84/BEL46) (Lmm).
The best growth inhibition was observed with the dichloromethane extracts of aerial parts of Acanthospermum hispidum DC. (Asteraceae) (IC(50)=14.5 μg/ml on Tbb and 11.1 μg/ml on Lmm), twigs of Keetia leucantha (K. Krause) Bridson (syn. Plectronia leucantha Krause) (IC(50)=5.8 μg/ml on Tbb), aerial parts of Byrsocarpus coccineus Schumach. & Thonn (syn. Rourea coccinea (Schumach. & Thonn.) Hook.f.) (IC(50)=14.7 μg/ml on Tbb) and aerial parts of Carpolobia lutea G.Don. (IC(50)=18.3 μg/ml on Tbb). All these extracts had a low cytotoxicity. It is not the case for the methanolic and water extracts of roots of Anchomanes difformis (Blume) Engl. (IC(50)=14.7 and 13.8 μg/ml on Tbb) which were toxic at the same concentration range on WI38, human cells. A bio-guided fractionation of the most active extract of Keetia leucantha allowed to identify oleanolic acid and ursolic acid as responsible for the observed activities.
Our study gives some justification for antiparasitic activity of some investigated plants.
... Each year, 500,000 cases of the visceral type are reported and 50,000 individuals die from the latter [4]. In Mexico, cases of leishmaniasis has been reported in 22 states, and it is considered endemic in the states of Coahuila, Nuevo León, Tamaulipas, Veracruz, Tabasco, Campeche, Yucatán, Quintana Roo, Chiapas, Oaxaca, Guerrero, Michoacán, Jalisco, Nayarit, San Luis Potosí, Morelos, Puebla, and Hidalgo, where it is commonly known as chiclero's ulcer [5][6][7][8]. For example, in one municipality of the state of Campeche, over a 2-year period, 76% of persons had skin lesions, and were diagnosed with cutaneous leishmaniasis. ...
... From the active hexane fraction (obtained by partition from active methanol extract) of the U. andrieuxii roots (syn. P. andrieuxii), the following compounds were isolated: cholestra-4,20,24trien-3-one or pentalinosterol (2); 24-methylcholest-4-24(28)-dien-3-one (3), cholest-4-en-3one (4),6,7-dihydroneridienone (5), and neridienone (6). All compounds (2)(3)(4)(5)(6) inhibited the growth of L. mexicana promastigotes, showing an IC 50 of <30 μM; pentostam was used as positive control (IC 50 = 346.1 μM). ...
... P. andrieuxii), the following compounds were isolated: cholestra-4,20,24trien-3-one or pentalinosterol (2); 24-methylcholest-4-24(28)-dien-3-one (3), cholest-4-en-3one (4),6,7-dihydroneridienone (5), and neridienone (6). All compounds (2)(3)(4)(5)(6) inhibited the growth of L. mexicana promastigotes, showing an IC 50 of <30 μM; pentostam was used as positive control (IC 50 = 346.1 μM). All of these compounds, together with cholest-5,20,24-trien-3β-ol (7), were active against L. mexicana amastigotes (IC 50 < 14.5 μg/mL) in the in vitro assay [49]. ...
... Each year, 500 000 cases of the visceral type are reported and 50 000 individuals died from the recidivans [4] . In Mexico, its presence has been reported in 22 states and it is considered endemic in the states of Coahuila, Nuevo León, Tamaulipas, Veracruz, Tabasco, Campeche, Yucatán, Quintana Roo, Chiapas, Oaxaca, Guerrero, Michoacán, Jalisco, Nayarit, San Luis Potosí, Morelos, Puebla and Hidalgo, where it is commonly known as chiclero's ulcer [5][6][7][8] . For example, in one municipality of the state of Campeche, over 2-year period, 76% of persons had skin lesions and were diagnosed with cutaneous leishmaniasis. ...
... From the active hexanic fraction (obtained by partition from active MeOH extract) of the U. andrieuxii roots (syn. P. andrieuxii), the following compounds were isolated: Cholestra-4,20,24-trien-3-one or pentalinosterol (2), 24-methylcholest-4-24(28)-dien-3-one (3), cholest-4-en-3-one (4), 6,7dihydroneridienone (5), and neridienone (6). All compounds (2)(3)(4)(5)(6) inhibited the growth of L. mexicana promastigotes, showing an IC 50 of <30 mM; Pentostam was used as positive control (IC 50 = 346.1 mM). ...
... P. andrieuxii), the following compounds were isolated: Cholestra-4,20,24-trien-3-one or pentalinosterol (2), 24-methylcholest-4-24(28)-dien-3-one (3), cholest-4-en-3-one (4), 6,7dihydroneridienone (5), and neridienone (6). All compounds (2)(3)(4)(5)(6) inhibited the growth of L. mexicana promastigotes, showing an IC 50 of <30 mM; Pentostam was used as positive control (IC 50 = 346.1 mM). All of these compounds, together with cholest-5,20,24-trien-3b-ol (7), were active against L. mexicana amastigotes (IC 50 < 14.5 mg/mL) in the in vitro assay [48] . ...
Leishmaniasis is considered as an emerging, uncontrolled disease and is endemic in 98 countries. Annually, about 2 million cases of cutaneous and 500000 cases of visceral-type leishmaniasis are recorded and 60000 persons died from the disease. In Mexico, cutaneous leishmaniasis is known as chiclero's ulcer and is reported in 22 states, it is considered as a health problem. For its treatment, pentavalent antimonial drugs are administered. These drugs cause severe side effects, are costly. Drug-resistant cases have been reported and have been developing for over 70 years. One alternative to the drugs that are currently available is to find active molecules in medicinal plants. Dihydrocorynantheine, corynantheine and corynantheidine are active against Leishmaniamajor, while harmane, pleiocarpin, buchtienin, luteolin and quercetin are active against Leishmania donovani. In Mexico, about 20 medicinal plants have been evaluated against Leishmania mexicana, among which the most active are Tridax procumbens, Lonchocarpus xuul and Pentalinon andrieuxii. From these plants, active compounds with IC50 ≤ 30 μg/mL or μM have been isolated, such as 3(S)-16,17-didehydrofalcarinol or Oxylipin, cholestra-4,20,24-trien-3-one or pentalinosterol, 24-methylcholest-4-24(28)-dien-3-one, cholest-4-en-3-one, 6,7-dihydroneridie-none, neridienone, cholest-5,20,24-trien-3β-ol, and isocordoin. Today, only pentalinonsterol has been synthesized and assayed in the visceral leishmaniasis experimental model using BALB/c mice infected with Leishmania donovani. Liposome formulation of this compound administered by intravenous route at 2.5 mg/kg showed a significant reduction of parasite load in mouse liver and spleen.
... Leaf and root preparations of the S. liberica Gérôme & Labroy are used in the treatment of hemorrhoids, pain, smallpox, chicken-pox, and measles, venereal diseases, malnutrition, paralysis, epilepsy, convulsions, and spasm, pulmonary troubles, and as vermifuge [9], as well as remedy for parasitic infections [7]. Preparations of the S. liberica are used in the treatment of ear and eye infections, inflammation (leaf juice), toothache (fruit juice together with fluid from snails), fever, headache, and cold (fume from burning leaves inhaled), cough, pain, inflammation, infections, convulsion, diarrhea, and as stimulating tonic (root decoction) [3]. ...
... Therefore, this study aimed to determinate the antimicrobial activity of ten plants from the Sansevieria genus commonly used in traditional medicine in order to validate scientifically their therapeutic properties. The use of these plants in folk medicinal remedies for treating various health problems has already been reported, and the plants have been tested in the treatment of hemorrhoids, pain, smallpox, chicken-pox, and measles, venereal diseases, malnutrition, paralysis, epilepsy, convulsions, and spasm, pulmonary troubles, and as vermifuge [9], as well as remedy for parasitic infections [7]. ...
Purpose: In study, an attempt has been made to evaluate the antibacterial activity of seventeen plants belonging to the Sansevieria genus against Acinetobacter baumannii complex isolate, resistant to gentamicin and ciprofloxacin (specimen 3680, UK NEQAS). The aim of the present study was to evaluate the antibacterial capacity and to validate scientifically the inhibitory activity of some plants belonging to the Sansevieria genus for microbial growth attributed to their popular use and to propose new sources of antimicrobial agents. Methodology. The leaves of Sansevieria plants, cultivated under glasshouse conditions, were sampled at M.M. Gryshko National Botanic Garden (NBG), National Academy of Science of Ukraine. Specifically, the leaves of Sansevieria francisii Chahin, S. caulescens N.E.Br., S. suffruticosa N.E.Br., S. roxburghiana Schult. & Schult.f., S. metallica Gérôme & Labroy, S. gracilis N.E.Br., S. hyacinthoides (L.) Druce, S. cylindrica Bojer ex Hook., S. canaliculata Carrière, S. aethiopica Thunb., S. kirkii Baker, S. trifasciata Prain, S. forskaliana (Schult. & Schult.f.) Hepper & J.R.I. Wood, S. fischeri (Baker) Marais, S. dooneri N.E.Br., S. intermedia N.E.Br., S. parva N.E.Br. were sampled for the study. Antimicrobial activity was determined using the agar disk diffusion technique. Scientific novelty. Results proved that extracts obtained from the leaves of S. dooneri and S. gracilis were particularly active against Acinetobacter baumannii complex isolate (diameters of inhibition zones were 14-20.5 mm). It was followed by the activities of extracts from the S. suffriticosa (15.4 ± 1.11 mm), S. fischeri (14.7 ± 1.1 mm), S. parva (14.2 ± 1.1 mm), S. canaliculate (13.8 ± 1.18 mm), S. trifasciata leaves (13.7 ± 1.3 mm). Finally, the ethanolic extracts of S. hyacinthoides and S. intermedia showed fewer antimicrobial activities (diameters of inhibition zones ranged between 7.5 to 10 mm). Conclusions. Hence, the ethanolic extracts derived from S. dooneri and S. gracilis exhibit a favorable antibacterial activity against Acinetobacter baumannii, indicating that these plants could be a good source of antibacterial agents to combat A. baumannii-mediated infections. Thus, the leaves of some plants belonging to the Sansevieria genus with antibacterial properties may offer alternative therapeutic agents against bacterial infections.
... Even though antitrypanosomal and antioxidant activities of A. hispidum have been reported [18,19], the corresponding cellular mechanisms of action in trypanosomes have not been investigated. e present study aimed to investigate the phytochemistry of the Ghanaian species of A. hispidum for its antitrypanosomal and antioxidant properties in T. brucei to provide key insights for AT drug discovery and development. ...
... Several phytochemicals such as terpenoids, alkaloids, glycosides, flavonoids, and saponins have been identified and characterized in A. hispidum [7]. e plant species have also been linked to a myriad of pharmacological and medicinal properties [7,18,19]. However, there is no reported investigation linking the phytochemistry of A. hispidum to its pharmacological effects against microbial infections with regard to cellular mechanisms of action. ...
African trypanosomiasis is a major neglected tropical disease with significant health and economic concerns in sub-Saharan Africa. In the absence of vaccines for African trypanosomiasis, there is a consideration for alternative sources of chemotherapy. Acanthospermum hispidum DC (A. hispidum) is a herbal species of the Asteraceae family that is endowed with rich phytochemicals with unknown mechanisms of antitrypanosomal effects. This study aimed to investigate the cellular mechanisms of antitrypanosomal and antioxidant activities of A. hispidum against Trypanosoma brucei (T. brucei), a causative protozoan species of African trypanosomiasis. Fractions were prepared from the whole plant of A. hispidum through solvent partitioning by employing solvents of varying polarities (hexane, HEX; dichloromethane, DCM; ethyl acetate, EA; aqueous, AQ). The in vitro efficacies and mechanisms of antitrypanosomal activities of A. hispidum were investigated using a panel of cell biological approaches. GC-MS analysis was used to identify the major compounds with a possible contribution to the trypanocidal effects of A. hispidum. A. hispidum fractions displayed significant antitrypanosomal activities in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (AH-HEX, EC50 = 2.4 μg/mL, SI = 35.1; AH-DCM, EC50 = 2.2 μg/mL, SI = 38.3; AH-EA, EC50 = 1.0 μg/mL, SI = 92.8; AH-AQ, EC50 = 2.0 μg/mL, SI = 43.8). Fluorescence microscopic analysis showed that at their EC50 values, the fractions of A. hispidum altered the cell morphology as well as the organization of the mitochondria, nucleus, and kinetoplast in T. brucei. At their maximum tested concentrations, the prepared fractions exhibited antioxidant absorbance intensities comparable to the reference antioxidant, Trolox, in contrast to the oxidant intensity of an animal antitrypanosomal drug, diminazene (Trolox, 0.11 A; diminazene, 0.65 A; AH-HEX, 0.20 A, AH-DCM, 0.20 A, AH-EA, 0.13 A, AH-AQ, 0.22 A). GC-MS analysis of the various fractions identified major compounds assignable to the group of alkaloids and esters or amides of aliphatic acids. The results provide useful pharmacological insights into the chemotherapeutic potential of A. hispidum toward drug discovery for African trypanosomiasis.
... Reference [2] reported that the aqueous root extract of SL is an effective antidiarrhoeal agent. e antisnake venom, sedative, asthma, diabetes, abdominal pains, anticancer, hepatoprotective, CNS depressant, anticonvulsant, analgesic, anti-inflammatory and anticonvulsant, antidiabetic, antileishmanial, and antiplasmodial activities of SL have been evaluated and reported by various research teams [5][6][7][8][9][10][11]. ...
... e in vitro antiplasmodial effect of SL investigated by [6] showed moderate activity due to dichloromethane extract compared to the menthol and aqueous extracts that showed little or no activity. e difference in activity between the study [7] led by a research team and the current study may be due to different modes of extraction and solvents used and assay methods used. ...
Background:
Sansevieria liberica Gerome and Labroy (Agavaceae) is a religious and ornamental perennial plant with highly valued medicinal usage in Nigeria. Sansevieria liberica is used in the management of malarial fever. The ease of development of resistance to available antimalarial drugs has resulted in increased clinical failure and mortality. The study investigated the antimalarial effects of Sansevieria liberica (SL) leaf extract in mice infected with Plasmodium berghei.
Materials and methods:
The ability of SL leaf extract to suppress the growth of malaria parasites in early (suppressive) and established (curative) infections was established using animal models. The mean survival time (MST) was determined. The antioxidant potential was established using two standard in vitro models. High-performance liquid chromatography (HPLC) and phytochemical analysis methods were used to create a chemoprofile fingerprint of SL hydroethanolic leaf extract.
Results:
At 200, 400, and 400·mg kg-1, SL produced 68.71, 70.74, and 75.09% parasite suppression in the suppressive model while the curative model gave a percentage of cure of 71.09, 72.60, and 62.09, respectively. The animals lived longer compared to both negative and positive controls but were not fully protected. The IC50 values of SL and vitamin C were calculated to be 3.599 µg mL-1 and 3.08 µg mL-1, respectively. The reducing power of vitamin C was significantly (P < 0.05) higher than that of SL extract. Some flavonoids were established as possible marker compounds for SL leaf extract. Discussion and Conclusions. The antimalarial assay results demonstrated that the use of SL in folk medicine may have scientific support.
... Fractions C6 and C7 achieved better IC 50 results, 0.26 ± 0.03 and 0.25 ± 0.01 mg/mL, approximating the result found for the positive control, metronidazole, which produced an IC 50 of 0.20 ± 0.02 mg/mL. These results of antitrypanosomal, antileishmanial and antiplasmodial activity corroborate with previous results described in the scientific literature, where different extracts of the aerial parts of A. hispidum demonstrated different levels of parasite inhibition [50][51][52]. ...
... The leaves of A. hispidum were extracted with the hexane, petroleum benzene, chloroform, ethyl acetate and acetone solvents, using a Soxhlet apparatus, and the crude extracts were tested for larvicidal and pupicidal potential and for toxicity against the adult mosquitoes in the test of smoke toxicity. Petroleum benzene extract was more effective as a larvicide and pupicide for all mosquito species, with the lowest values of LC 50 and LC 90 . The smoke toxicity test on adult mosquitoes showed 69% mortality in An. stephensi, 52% in Ae. aegypti and 56% in Cx. quinquefasciatus. ...
Background:
Acanthospermum hispidum DC is a medicinal plant present in America, Africa, Australia, India, Hawaii, and Brazil. In Brazil, the species is used in the treatment of gastrointestinal, respiratory disorders and has expectorant action. In the literature there are studies on the chemical composition of the species, with reports of the presence of alkaloids, flavonoids, hydrolyzable tannins, terpenes, and steroids. In addition, several studies have reported in vitro and in vivo studies that prove the biological properties of extracts and compounds isolated from different organs of the A. hispidum plant, including: hepatoprotectors, antioxidants, antimicrobials and antiparasitic.
Objective:
The objective of this review is to update the knowledge about the phytochemical, pharmacological and toxicity aspects of A. hispidum, to contribute to the recognition of the species and direct new studies.
Methods:
An extensive bibliographic search was conducted in different scientific databases.
Results:
The presence of different chemical constituents in A. hispidum have been identified, among them flavonoids, tannins, terpenes, and steroids. Additionally, antimicrobial and antiparasitic activities were mainly attributed to the species, and other activities not previously described were presented, such as anticholinesterase, antioxidant, hepatoprotective, and hypoglycemic, all based on results of in vitro and in vivo studies. Finally, no reports of toxic effects were found in the in vitro and in vivo tests. After analyzing the articles, it was evidenced that other experiments, with different models using animals, are essential to evaluate the possible mechanisms of action of the extracts and compounds isolated of A. hispidum.
Conclusion:
Therefore, this review may contribute to the recognition of the importance of A. hispidum and its potential as a medicinal plant and may also guide the conduct of future research regarding the constituents, biological activities, and toxicity of the species.
... Among the listed plants Anchomanes difformis (Blume) Engl (Araceae), Rhizophora racemosa G. Mey (Rhizophoraceae) and Ravenala madagascariensis Sonn (Strelitziaceae) feature prominently. A. difformis, R. racemosa and R. madagascariensis are plants with several reported therapeutic effects, and they are used in many parts of Africa for the traditional management of malaria, asthma, diabetes, antimicrobials [18][19][20][21][22][23]. ...
... The acute oral toxicity study was conducted using test guidelines on acute oral toxicity (test 423) according to the Organization for Economic Cooperation and Development and as described by Alanin [20,22,23,19,18]. ...
Aims: Anchomanes difformis (Blume) Eng (Araceae), Rhizophora racemosa G. Mey (Rhizophoraceae) and Ravenala madagascariensis Sonn (Strelitziaceae) are used in traditional medicine in Guinea for diabetes management. The aim of this work was to test the antidiabetic activity of these plants and to determine their toxicity. Original Research Article Camara et al.; EJMP, 31(18): 15-22, 2020; Article no.EJMP.62592 16 Material and Methods: Extemporaneous extracts based on these plants were tested for their acute toxicity, their effects in normoglycemic rats and rendered hyper glycemic by the oral route in comparison with the glibenclamide an antidiabetic agent. Swiss albino mice and Male Wistar rats were used respectively for acute oral toxicity and antidiabetic activity. Results: This study showed that the administration of the 2000 mg / kg dose of dry extracts in mice showed no acute toxicity and adverse effect. At a dose of 400 mg/kg these three plants showed significant hypoglycaemia effect. The average blood glucose levels ranged from 111.2 ± 6.2 to 84.6 ± 6.7 mg/dL (p<0.001) for A. difformis, 110.6 ± 6 to 93.2 mg/dL (p<0.05) for R. racemosa and 99.6 ± 14.4 to 82.3 mg/dL (p<0.05) for R. madagascariensis. Conclusion: The results obtained on the antidiabetic properties of these three plants corroborates their traditional uses in the management of type 2 diabetes in the Republic of Guinea.
... The strain MHOM/BZ/84/ BEL46 of Leishmania mexicana mexicana (Lmm) in promastigote forms (BRC-Leishmania) were cultivated in vitro in a semi-defined medium (SDM-79) (Sigma-Aldrich) [38], supplemented with 15 % heat-inactivated FBS and incubated at 28°C in a humidified atmosphere with 5 % CO 2 . The in vitro antitrypanosomal and antileishmanial activity of plant extracts were evaluated as previously described [40]. Three extracts were tested: methanol, aqueous, and aqueous crude extract free of tannins as well as ellagic acid, analytical standard grade (Alfa Aesar). ...
... Suramin (99 %) and amphotericin B (± 80 %) (Sigma-Aldrich) were used as positive controls for antitrypanosomal and antileishmanial activity respectively. Plant extracts, ellagic acid, and positive controls were prepared as described [40] and tested in triplicate. The results were expressed as the mean IC 50 (the concentration of a product that can reduce the level of parasitaemia to 50 %). ...
This 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.
... Some of the relevant antileishmanial activities were found in fractions from South African Asteraceae plants. Fractions and essential oils from this family, in which Artemisia species are included, were tested for their parasitic toxicity revealing IC 50 ranging from 0.01 to 14.4 µg/ml [57][58][59]60]. The alkaloid-rich fractions of Pavetta crassipes K. Schum (Rubiaceae) leaves revealed promising results against L. infantum IA (2.0 µg/mL), being also a potential source of active compounds [61]. ...
... Minor phenylpropanoids (31-36) and a phenylethanoid (37) were identified. Other aromatic compounds have also been described, as iridoids (38--41), a diarylheptanoid or curcumin (42) and its derivatives (43)(44)(45), hydrolyzable tannins (46)(47)(48)(49)(50). From the chemical family of quinones, several compounds were studied as benzoquinones (51)(52)(53), hydroquinones and derivatives (54)(55)(56)(57)(58)(59)(60)(61), naphthoquinones (62)(63)(64)(65) and isoflavanquinones (66)(67)(68). Flavonoids known as flavones (69-72), a coumarin (73), benzoic acid derivatives (74,75), steroids (76-84) and triacylglycerols (85, 86) have also been described. ...
Leishmaniasis is a vector-borne disease among the 10 most Neglected Tropical Diseases with diverse clinical manifestations caused by protozoan parasites of the Leishmania genus. Around 80% of leishmaniasis cases are found in the Old World affecting populations mainly in low and middle-income countries. Its control relies mostly on chemotherapy which still presents many drawbacks. Natural products may offer an inexhaustible source of chemical diversity with therapeutic potential. Despite the lack of knowledge on traditional products with activity against Leishmania parasites, many reports describe the search for natural extracts and compounds with antileishmanial properties against promastigote and amastigote parasite forms. This review summarizes the research of 74 publications of the last decade (2008–2018) focused on the identification of endemic plant-derived products that are active against Old World Leishmania parasites responsible for cutaneous and visceral leishmaniasis. The present review combines data on antileishmanial activity of 423 plants species, belonging to 94 different families, including a large range of crude extracts which lead to the isolation of 86 active compounds. Most studied plants came from Asia and most promising plant families for antileishmanial activity were Asteraceae and Lamiaceae. From the chemical point of view, terpenoids were the most frequently isolated natural products. These studies suggest that natural products isolated from Old World flora are a rich source of new chemical scaffolds for future leishmaniasis treatment as well as for other Neglected Tropical Diseases warranting further investigation.
... This need is reflected in the growing interest of many research groups in the search for new compounds with anti-T. brucei potential [98][99][100][101][102][103][104][105][106]. ...
... Preliminary results [101] demonstrated good antitrypanosomal activity of dichloromethane extracts of S. spinosa (IC 50 = 1 5 μg/mL), causing us to speculate that there are active components that are not EO constituents that should be evaluated more intensively. The better results observed with linalool (3) and (E)-nerolidol (110) reflect the need for further studies of these substances and for investigation of the potential of other oxygenated terpenes to identify alternatives for human African trypanosomiasis treatment. ...
The term neglected diseases refers to a group of infections caused by various classes of pathogens, including protozoa, viruses, bacteria, and helminths, most often affecting impoverished populations without adequate sanitation living in close contact with infectious vectors and domestic animals. The fact that these diseases were historically not considered priorities for pharmaceutical companies made the available treatments options obsolete, precarious, outdated, and in some cases nonexistent. The use of plants for medicinal, religious, and cosmetic purposes has a history dating back to the emergence of humanity. One of the principal fractions of chemical substances found in plants are essential oils (EOs). EOs consist of a mixture of volatile and hydrophobic secondary metabolites with marked odors, composed primarily of terpenes and phenylpropanoids. They have great commercial value and were widely used in traditional medicine, by phytotherapy practitioners, and in public health services for the treatment of several conditions, including neglected diseases. In addition to the recognized cytoprotective and antioxidative activities of many of these compounds, larvicidal, insecticidal, and antiparasitic activities have been associated with the induction of oxidative stress in parasites, increasing levels of nitric oxide in the infected host, reducing parasite resistance to reactive oxygen species, and increasing lipid peroxidation, ultimately leading to serious damage to cell membranes. The hydrophobicity of these compounds also allows them to cross the membranes of parasites as well as the blood-brain barrier, collaborating in combat at the second stage of several of these infections. Based on these considerations, the aim of this review was to present an update of the potential of EOs, their fractions, and their chemical constituents, against some neglected diseases, including American and African trypanosomiasis, leishmaniasis, and arboviruses, specially dengue.
... cruzi and T. b. rhodesiense), indicating poor selectivity against mammalian cells and probable cytotoxicity (Obbo et al. 2019). It was also reported by Bero et al. (2011), that extracts with trypanocidal activities, such as A. hispidum, Byrsocarpus coccineus, Carpolobia lutea and Keetia leucantha twigs with DCM extracts, all demonstrated low or no cytotoxicity. ...
Trypanosomiasis is a neglected tropical disease caused by various trypanosome species that affects both humans and livestock with catastrophic implications across the endemic areas. Plants have been used for many centuries to establish or bring back health, well-being, and as cure for several illnesses. We performed a systematic review using the PRISMA guidelines to compile the results of studies carried out in both in vitro and in vivo investigations, examined the effect of plant extracts on trypanosomosis treatment and risk of bias of the studies. Published articles were appraised and only those with the requisite inclusion criteria looking at the efficacy of different medicinal plant extracts used against trypanosomosis globally from 1990 to 2020 in ScienceDirect, PubMed, SpingerLink, Scopus and Web of Science were used for this systematic review. A total of 761 medicinal plant species were evaluated for antitypanosomal activity with Fabaceae and Euphorbiaceae families being frequently studied. After comparative analysis, two plant species, namely, Khaya senegalensis and Terminalia superba produced best antitrypanosomal activity both in vitro and in vivo. Leaves (74%) and stem barks (38%) were most used plant parts. Medicinal plant extracts demonstrated in vivo antirypanosomal efficacy either singularly or synergistically at dosages < 2000 mg/kg, that resulted in elimination of parasitaemia and reduction of trypanosomosis clinical symptoms. On the other hand, most of the extracts, had an in vitro antirypanosomal activity within minutes after application in a concentration-dependent manner. Bias analysis showed the lack of standardized experimental designs and failures in statistical tests. There is lack of studies for evaluation of efficacy of medicinal plant extracts against Trypanosoma equiperdum and T. vivax both in vitro and in vivo amongst pathogenic trypanosomes. Medicinal plant extracts have potential therapeutic activity against pathogenic trypanosomes infecting animals and humans as suggested by majority of in vitro studies but require verification of in vivo efficacy and toxicity studies which are lacking.
... Therefore, this study aimed to determine the antimicrobial activity of ten plants from the Sansevieria genus commonly used in traditional medicine to validate scientifically their therapeutic properties. The use of these plants in folk medicinal remedies for treating various health problems has already been reported, and the plants have been tested in the treatment of hemorrhoids, pain, smallpox, chicken-pox, and measles, venereal diseases, malnutrition, paralysis, epilepsy, convulsions, and spasm, pulmonary troubles, and as a vermifuge (Burkill, 1985), as well as a remedy for parasitic infections (Bero et al., 2011). ...
The collection of the Ninth International Scientific and Practical Conference “Medicinal Herbs: from past experience to new technologies” presents the results of the investigations of medicinal plants, especially their introduction, biology, breeding, physiology and phytochemistry, propagation and cultivation, pharmacy, use in agriculture and industry.
... The spectrum of composition and bioactive constituents of the aqueous-methanolic extract of A. syriaca leaf is presented in Figure 2 and Table 2, respectively. Bioactive constituents of A. syriaca were found to be ionic liquids with high content pyrimidine derivatives (2-thiazolamine,4-(3,4-dimethoxyphenyl)-5-methyl and 4H-Thiopyrano (4',3':4,5) furo (2,3-d) pyrimidine-3(6H)-amine,5,8-dihydro-4-imino-6,6-dimethyl) couple with a compound of nitrogen which is quinolone derivatives (N, N-diethyl-3ethoxy carbonylmethylamino-2-(4-chlorophenyl)-acrylamide) used for moderate antiplasmodial acitivity with cytotoxicity to hepatic and renal tissues [32,33]. These pyrimidine derivatives contents exhibit high potency of anti-viral, antioxidants, anticancer, antimicrobial, antiarrhythmic, antimalarial, antifolate immunosuppressive, antioxidants, antiparkinson and good analgesic activities as well as reduce the cytotoxicity of quinolone derivative due to protective activity [34,35]. ...
High mortality rate couple with the economic effect of deadly Plasmodium falciparum caused by malaria necessitated this study. Evaluation of bioactive constituents and antimalarial properties of the aqueous-methanolic extract of Asclepias syriaca (A. syriaca ) was investigated. Bioactive constituents were determined by GC-MS analytical detector. Albino rats were five in each group of six groups (A-E) in which group A was non-infected with P. falciparum (negative control). Groups B, C, D, E were infected with 1×10 ⁷ /ml P. falciparum without treated, treated with standard drugs of 20mg of chloroquine/kg, 100, 200 and 400mg of extracted A. syriaca /kg, respectively . Hematological and biochemical parameters of Plasmodium falciparum infected albino rats were determined. Aqueous-methanolic extract of A. syriaca leaf made up of high content of pyrimidine, quinolone and silane derivatives with synergetic properties with potency for therapeutic of malarial and viral infectious diseases. MCV, PLA, RBC, total protein and albumin were significantly elevated upon infected P. falciparum and gradually increases with dosage and time when treated with chloroquine and A.syriaca leaf extract but vice visa for the case WBC and creatinine. Parasitemia level significantly declined when administered with chloroquine and A, syriaca leaf extract for 36 hours. Hence serves as an effective medication in place of chloroquine due to its availability, avoidable and as a source of relevant medications to Plasmodium spp and viral infectious diseases.
... It is an important source of medicine for a wide range of diseases ( Arbonnier 2002;Isa et al. 2014;Plantz Africa 2017;World Agroforestry Centre 2018). It is also used to increase milk and crop production (Hoet et al. 2006(Hoet et al. , 2007Bero et al. 2011;Salifou et al. 2017). In Benin, many parts of the species such as fruits, leaves, roots, seeds, etc. are used to fulfill these different functions (Avakoudjo et al. 2020). ...
Strychnos spinosa Lam. is an important wild edible fruit tree (WEFT) that is increasingly threatened due to anthropogenic pressure. Despite its remarkable socio-economic potential, commercial plantations for the species are rare. Characterization of the genetic diversity and potential of WEFT is a prerequisite for domestication and genetic improvement. This study assessed the morphological diversity and differentiation among populations of S. spinosa across a climatic gradient (Sudano-Guinean vs Sudanian zones) in Benin, West Africa. Morphological data were collected on 81 trees and 810 fruits of S. spinosa from 7 populations in the two climatic zones using nine phenotypic descriptors. Descriptive statistics and multivariate analyses were used to describe and partition differences among trees and study populations. Results showed highly significant differences (P ≤ 0.001) among populations for all measured traits. The within-population variation accounted for the highest proportion (53–90%) of the total variation. Strong and positive correlations (r = 0.91–0.99; P < 0.05) were observed among trunk and fruit traits except for tree height and fruits’ seed weight suggesting that fruit traits (fruit mass, pulp mass, seed number, ratio) can be predicted from trunk traits (dbh). Cluster analysis distinguished three distinct groups of S. spinosa in Benin. Population from Bassila phytodistrict in the Sudano-Guinean zone showed superior phenotypic traits (e.g. tree diameter, fruit mass, and pulp mass) indicating a high potential for selection for domestication purposes. Our study revealed marked phenotypic diversity of S. spinosa in Benin and provides relevant information for domestication and harnessing of S. spinosa genetic resources.
... Consequently, leishmaniasis represents a potential threat to several areas 27 . The lack of effective vaccines, the problems with vector control and the development of drug resistance have also raised the incidence of this disease 5 . The most commonly used medications for leishmaniasis treatment are pentavalent antimonials, amphotericin B, paromomycin, and pentamidine, which have severe side effects, require high doses for long periods of time, and are administered parenterally 28 . ...
Leishmaniasis is a major vector-borne disease triggered by an obligate intracellular protozoan parasite of the genus Leishmania and transmitted by the bite of phlebotomine female sand flies. This parasite causes a wide range of human diseases, from localized self-healing cutaneous lesions to fatal visceral infections. The aim of this study was to investigate the cytotoxic, antiproliferative, and apoptotic effects of curcumin on Leishmania major promastigotes (MHOM/SA/84/JISH) and to assess these effects on the cell cycle of promastigotes. The MTT colorimetric assay was used to evaluate the cytotoxicity and proliferation of promastigotes. Additionally, flow cytometry was used to analyze the cell cycle. The Annexin V/propidium iodide staining technique followed by flow cytometry was used to study the cell death induced by curcumin. In this study curcumin showed a potent antileishmanial effect, exhibiting cytotoxicity against L. major promastigotes. At 80 μM, the survival in curcumin treated promastigotes reached 22%; however, the median lethal concentration of curcumin (LC50) was 35 μM. The drug exerted its cytotoxic effect by inducing apoptosis. Curcumin-induced cell death in promastigotes reached 82.5% at 80 μM concentration. In addition, curcumin delayed the cell cycle in the S-phase inhibiting cell proliferation. Thus, curcumin was shown to be effective against L. major promastigotes. Therefore, curcumin merits further research studies to demonstrate its efficacy in treating cutaneous leishmaniasis.
... When compared with amphotericin B, used currently in the treatment of Leishmaniasis, compounds 55 and 56 show great potential for future selective drug development against Leishmania. Keetia leucantha (synonym: Plectronia leucantha Krause) is a West African tree of the Rubiaceae, used to treat a variety of infections, including parasitic infections [139,140]. Ursolic acid (57) and oleanolic acid (58), along with other constituents were isolated from the leaves of this plant. An investigation of the antitrypanosomal activities of essential oil, the dichloromethane extract and isolated compounds on T. b. brucei bloodstream forms (Tbb BSF) and procyclic forms (Tbb PF) [131] showed that ursolic acid (57) and oleanolic acid (58) were the most bioactive tested compounds [131]. ...
Parasitic diseases continue represent a threat on a global scale, particularly among the poorest countries in the world. This is particularly because of the absence of vaccines, and in some cases, resistance against available drugs, currently being used for their treatment. In this review emphasis is laid on natural products and scaffolds from African medicinal plants (AMPs) for lead drug discovery and possible further development of drugs for the treatment of parasitic diseases. In the discussion, emphasis has been laid on alkaloids, terpenoids, quinones, flavonoids and narrower compound classes of compounds with micromolar range activities against Schistosoma, Trypanosoma and Leishmania species. Suggestions for future drug development from African medicinal plants have also been provided.
... The diversity of triterpenes is highly associated with their broad range of 112 pharmacological effects, and different studies have already shown that these compounds 113 present multispecies action against Leishmania sp. (Gnoatto et al., 2008; Bero et al., 2011; 114 Begum et al., 2014). Recently, it was demonstrated that ursolic acid (UA) displayed activity 115 against promastigote and amastigote forms of L. Passero et al., 2011; Begum et al., 2014; Yamamoto et al., 117 2014; Yamamoto et al., 2015), suggesting that UA presents multispectral action. ...
Leishmaniasis is an important neglected tropical disease, affecting more than 12 million people worldwide. The available treatments are not well tolerated and present diverse side effects in patients, justifying the search for new therapeutic compounds. In the present study, the therapeutic potential and toxicity of ursolic acid (UA), isolated from the leaves of Baccharis uncinella C. DC. (Asteraceae), were evaluated in experimental visceral leishmaniasis. To evaluate the therapeutic potential of UA, hamsters infected with L. (L.) infantum were treated daily during 15 days with 1.0 or 2.0 mg UA/kg body weight, or with 5.0 mg amphotericin B/kg body weight by intraperitoneal route. Fifteen days after the last dose, the parasitism of the spleen and liver was stimated and the main histopathological alterations were recorded. The proliferation of splenic mononuclear cells was evaluated and IFN-g, IL-4, and IL-10 gene expressions were analyzed in spleen fragments. The toxicity of UA and amphotericin B were evaluated in healthy golden hamsters by histological analysis and biochemical parameters. Animals treated with UA had less parasites in the spleen and liver when compared with the infected control group, and they also showed preservation of white and red pulps, which correlate with a high rate of proliferation of splenic mononuclear cells, IFN-g mRNA and iNOS production. Moreover, animals treated with UA did not present alterations in the levels of AST, ALT, creatinine and urea. Taken together, these findings indicate that UA is an interesting natural compound that should be considered for the development of prototype drugs against visceral leishmaniasis.
... The diversity of triterpenes is highly associated with their broad range of pharmacological effects, and different studies have already shown that these compounds present multispecies action against Leishmania sp. (Gnoatto et al., 2008;Bero et al., 2011;Begum et al., 2014). Recently, it was demonstrated that ursolic acid (UA) displayed activity against promastigote and amastigote forms of L. (L.) amazonensis, L. (V.) braziliensis, L. (L.) chagasi, and L. (L.) major (Passero et al., 2011;Begum et al., 2014;Yamamoto et al., 2014Yamamoto et al., , 2015, suggesting that UA presents multispectral action. ...
... While the previous reports of Ibrahim et al. [18], employed shorter time (1 h) for the studies, this investigation involved the cultivation of trypanosome in vitro for longer period of time (6 h) in order to allow for adequate drug-parasite interaction, thereby avoiding wrong or misleading interpretations. Our selection of the root extract for subsequent study was based on the classification according to Bero et al. [23] where extract with IC 50 < 20 μg/ ml and IC 50 > 100 μg/ml are considered very good and ineffective, respectively. Owing to this classification, result from the present study of the methanolic extract of S. occidentalis root with IC 50 of 18 μg/ml suggest that the extract have a good anti-trypanosomal activity. ...
Objective
The present study investigated the anti-Trypanosoma brucei brucei activity of methanolic extract of Senna occidentalis roots, leaves, stem bark, and seed in vitro and bioactive components of the most active plant part.
Materials and methods
Trypanosoma brucei brucei was identified by PCR, cultured in Dulbecco’s Modified Eagle Medium (DMEM) and incubated at 37 °C and 5% CO2. Subsequently, the cultured T. brucei brucei were incubated with 500 μg/ml concentration of different parts of S. occidentalis plant and the most potent fraction was identified and subjected to Gas Chromatography-Mass Spectrometry (GC-MS).
Results
Amplicons of the rRNA gene of T. brucei brucei detected had a size of 1200 bp. The anti-trypanosomal activities indicated that the root extract of the plant was the most active at 500 μg/ml with inhibitory activity of 88.89% and fractions (2 and 5) the most active with IC50 values of 1.49 and 1.16 μg/ml respectively.
Conclusion
Results from this study insinuates that phenolic and simple aliphatic compounds might play key role in the anti-trypanosomal activity of S. occidentalis roots.
... It was also reported that the species can be used to combat ticks and tsetse flies; to cure diarrhea, fever, and trembling; and to improve milk production of animals and particularly in oxen. This is consistent with the findings of several authors (Bero et al. 2011;Hoet et al. 2006;Hoet et al. 2007;Salifou et al. 2017). This importance of the species in the traditional medicine constitutes an asset to be exploited for healing locally. ...
Green monkey orange (Strychnos spinosa) is an important multipurpose tree in rural communities in sub-Saharan Africa, including Benin. The objectives of this study were to (i) examine the various indigenous uses of Strychnos spinosa, (ii) assess local perception of the major threats to Strychnos spinosa, and (iii) identify the conservation strategies adopted by local communities to ensure its sustainable use in Benin. A participatory rural appraisal study was undertaken across three climatic zones in Benin. Data were collected through structured questionnaires involving 733 informants from 22 ethnic and 7 sociolinguistic groups. Correspondence analysis (CA) showed that S. spinosa is most widely used in the Sudanian zone (20 uses). About 73% of the informants used Strychnos spinosa as food, and 68% used it for medicine. The most valued organs were fruits, leaves, bark, and seeds. The major threats to Strychnos spinosa were human activities rather than climatic factors. Religion and cultural values were the main strategies adopted by local communities to conserve the species. The value of Strychnos spinosa is well appreciated in Benin, and local knowledge depends on the particular climatic zone, ethnic group, study level, and gender.
... Free radicals also cause several diseases whose treatments are very expensive for the population. There is a need to search for new anti-trypanosomal, anti-plasmodial and antioxidant lead compounds with new mechanism of action from medicinal plants (Bero et al., 2011). ...
The uncontrolled use of antimicrobials leads to an increase in the resistance of bacteria which becomes a public health problem. To overcome this problem, our study aims to establish a link between chemical composition and antimicrobial activity and then evaluate cytotoxicity, of seven essential oils. Antimicrobial activity of essential oils was assessed by macrodilution and solid-medium diffusion method on agar, then cytotoxicity test was evaluated in vitro by MTT method. Results showed that essential oils of Cymbopogon schoenantus, Cymbopogon giganteus, Cymbopogon citratus and Citrus aurantifolia are the most bactericidal. Analysis of antimicrobial activity and chemical composition reveal that the essential oil of Eucalyptus camaldulensis, the least oxygenated (14.9%), is the least active. The other essential oils, which are more active, are all rich in oxygenated compound (28.4% to 87.0%). The cytotoxicity assessment shows that our essential oils are less cytotoxic than camptothecin.
... Transmission of Leishmania occurs when the female phlebotomine sand fly bite a human body causing Leishmaniasis that may be cutaneous, mucocutaneous or visceral (kala-azar), which may be manifested by skin lesions (ulcers), mucous membranes destruction in the mouth, nose and throat, irregular fever attacks, weight loss, spleen and liver enlargement, and anemia. Visceral Leishmaniasis may be fatal in some cases if left untreated [1]. Scrophulariaceae is one of the largest angiosperm families, distributed everywhere as ornamental or wild plants. ...
Phytochemical study of the ethanolic extract of Scrophularia syriaca Benth. was attained by chromatographic and spectroscopic procedures, which resulted in the isolation of eight compounds; 6-O-α-L- rhamnopyranosylcatalpol (1), scropolioside B (2), gmelinoside-L (3), 8-acetyl harpagide (4), scropolioside D (5), scropolioside D2 (6), quercetin (7) and kaempferol-3-O-rutinoside (8). Their antiprotozoal activity was evaluated against Trypanosoma brucei brucei (s427-WT), Trypanosoma brucei brucei (TbAT1-B48), Leishmania major and Leishmania mexicana. Compounds 2, 5, 7 and 8 exhibited mild to moderate activities against kinetoplastid parasites compared to pentamidine positive control, the mechanism of antiprotozoal activity was investigated using molecular docking studies on the potential target enzyme Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH).
... However, no available data were reported on antiprotozoal activity of M. oleifera leaves of North Africa against L. major, the major causative agent of cutaneous leishmaniasis. Several classical methods have been adopted for the extraction of antileishmanial compounds like polyphenols from natural sources using different organic solvents pure or in mixtures (Bero et al., 2011;Al-Sokari et al., 2015;Kefi et al., 2018;). Whereas, little is known about the ultrasound extraction of antileishmanial compounds from plants with biodegradable and environmentally friendly solvents such as aqueous ethanol mixture (Nitin and Karnik, 2011). ...
Leishmaniasis is a parasitic disease affecting millions of people in Africa, Asia, and South America. It is considered
as a major public health problem causing morbidity and mortality worldwide. Actually, the luck of vaccines and
effective and less expensive antileishmanial therapy, have oriented pharmacological researches on natural
antileishmanial drugs from medicinal plants. Hence, the purpose of this work is to optimize extraction parame�ters such as the percentage of aqueous ethanol mixture, the temperature and the time through the ultrasound
bath equipment using a Box–Behnken Design (BBD) for maximal antileishmanial activity extraction from
Moringa oleifera leaves. The cytotoxicity of the optimum extract was evaluated on RAW 264.7 macrophage cell
line. The synergism between M. oleifera optimal extract and amphotericin B was also investigated using
checkboard method. The optimum extract exhibiting the highest percent inhibition of Leishmania major
promastigotes (99.15 ± 0.34%) was obtained using 16%v/v ethanol, at 60 °C for 20 min. Interestingly, this extract
showed the best IC50 value of 6.87 ± 0.32 and 9.31 ± 0.72 μg/mL against promastigote and amastigote forms, re�spectively with no cytotoxicity on macrophage cells Raw 264.7 (SI = 17.53). Moreover, this extract showed a
synergistic effect with amphotericin B (FIC = 0.375). HPLC analysis showed that at least six phenolic compounds
were identified. Resorcinol, luteolin7-O-glucoside and syringic acid were the most active ones against L. major
with IC50 values 3.788 ± 0.48, 10.70 ± 0.59 and 13.41 ± 0.59 μg/mL, respectively. Rutin and ferulic acid were fur�ther identified and showed moderate antileishmanial activity with IC50 values 78.51 ± 1.09 and 89.34 ± 1.22
μg/mL, respectively. Kaempferol 3-O-rutinoside was less active with IC50 value 204.4 ± 1.63 μg/mL
... Compared to the activity of Tridax procumbens (Martin-Quintal et al., (2009) demonstrating no mammalian cell toxicity, and, basing on the reported strong corollary between activity and cytotoxicity of constituent compounds from three species in the family Asteraceae (Schmidt et al., 2009), the observed antiprotozoal activities of V. grantii extracts in our screen could have been enhanced to some extent by cytotoxicity. However, several other reports also corroborate the low antileishmanial activities of crude extracts, fractions and essential oils from species of this family (Asteraceae) such as Baccharis dracunculifolia (Filho et al., 2009), Acanthospermum hispidum (Bero et al., 2011), Vernonia amygdalina (Tadesse et al., 1993), Vanillosmopsis arborea (Colares et al., 2013), Pulicaria gnaphaloides (Asghari et al., 2014), but with no significant toxicities to mammalian cells. ...
Ethnopharmacological relevance:
Seven medicinal plants from Ugandan flora, namelyEntada abyssinica, Khaya anthotheca, Vernonia amygdalina, Baccharoides adoensis, Schkuhria pinnata, Entandropragma utile and Momordica foetida, were selected in this study They are used to treat conditions and infections ranging from inflammations, pains and fevers to viruses, bacteria, protozoans and parasites. Two of the plants, V. amygdalina, and M. foetida are also used as human food or relish, while others are important in ethnoveterinary practices and in zoopharmacognosy in the wild. The aim of this study was to evaluate thein vitro antiplasmodial, antitrypanosomal and antileishmanial activities, along with cytotoxicity of the multi-component extracts of these plants MATERIALS AND METHODS: Different parts of the plants were prepared and serially extracted with hexane, petroleum ether, dichloromethane, ethyl acetate, methanol and double distilled water. Solvent free extracts were assayed for in vitro inhibition against four reference parasite strains, Plasmodium falciparum (K1), Trypanosoma brucei rhodesiense (STIB 900), Trypanosoma cruzi (Talahuen C2C4) and Leishmania donovani (MHOM-ET-67/L82) using standard methods. Toxicity was assessed against L6 skeletal fibroblast and mouse peritoneal macrophage (J774) cells and selectivity indices (SIs) calculated for the most active extracts.
Results:
The strongest activities, demonstrating median inhibitory concentration (IC50) values ≤2μg/ml, were observed for the dichloromethane and petroleum ether extracts of K. anthotheca, B. adoensis and S. pinnata. Overall, IC50 values ranged from <1μg/ml to >90μg/ml. Out of 22 extracts demonstrating IC50s <20μg/ml, seven were against T. b. rhodesiense (IC50: 1.6 - 16.2μg/ml), six against T. cruzi (IC50: 2.1 to 18.57μg/ml), none against L. donovani (IC50: falling >3.3 and >10μg/ml), and nine against P. falciparum (IC50: 0.96μg/ml to 4.69μg/ml). Selectivity indices (SI) calculated for the most active extracts ranged from 1.00 to 94.24. However, the B. adoensis leaf dichloromethane extract (a) was equipotent (IC50 = 3.3μg/ml) against L. donovani and L6 cells respectively, indicating non-specific selection. Trypanosome and Plasmodium parasites were comparatively more sensitive to the test extracts.
Conclusions:
The benefits achieved from the seven tested plant species as traditional ethnomedicinal and ethnoveterinary therapies or in zoopharmacognosy against infections and conditions of animals in the wild are strongly supported by results of this study. The synergy of plant extracts, so achieved by concerted actions of the ligands, produces adequate perturbation of targets in the four parasite genera, resulting in the strong potencies exhibited by low IC50values. The total inhibitory effect, achieved as a sum of perturbations contributed by each participating compound in the extract, minimises toxic effects of the compounds as seen in the high SI's obtained with some extracts. Those extracts demonstrating SI ≥4 form promising candidates for further cell-based and system pharmacology studies.
... In vitro antiparasitic and cytotoxicity tests were performed according to Bero et al. 18,20 Stock solutions of compounds were prepared in DMSO at 20 mg/ml and further diluted with medium. ...
In the present study, a series of new esters of secochiliolide acid (SA), a diterpene isolated from Nardophyllum bryoides, were synthesized in good yield. All compounds were evaluated for their in vitro antiparasitic properties (on Plasmodium falciparum and Trypanosoma brucei brucei) and cytotoxicity (on WI38, normal mammalian cells). They displayed moderate antitrypanosomal activity with IC50 values between 2.55 and 18.14 μM, with selectivity indices > 10, and low antiplasmodial effects with IC50 >29 μM. The only exception was the n‐hexyl ester of SA, which showed a strong and selective antiplasmodial activity (IC50= 1.99 μM and selectivity index= 117.0). The in vivo antimalarial efficacy of this compound was then assessed according to the 4‐day suppressive test of Peters in mice. An intraperitoneal treatment at 50 mg/kg/d induced a slight parasiteamia reduction by 56% wich was statistically significant on day 4 post‐infection and an increase in the survival time.
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... El tratamiento actual para la fase aguda de esta parasitosis está circunscrito al Nifurtimox y al Benznidazol, medicamentos que presentan varios inconvenientes como lo son el tiempo prolongado del tratamiento, efectividad relativa, desarrollo de resistencia y toxicidad tisular y genética (Lopera et al. 2013). Con el fin de aminorar este tipo de reacciones a algunos fármacos preparados artificialmente, desde hace varios años se busca en las plantas componentes químicos con actividad antimicrobiana (Wink 2012, Bero et al. 2011, Gurib-Fakin et al. 2014, Valencia et al. 2011. Específicamente, se conocen varios estudios con plantas en busca de metabolitos activos contra parásitos de la Familia Trypanosomatidae tales como T. cruzi (Soeiro et al. 2009, Apt & Zulantay 2011. ...
Different parts of 67 plants from the Biological Reserve Alberto Manuel Brenes (REBAMB) of Costa Rica,were studied for the presence of active components against Trypanosoma cruzi. The hydroalcoholic extracts of fresh or dried materials, were analyzed, in principle, with pilot presumptive tests, and then more specific, for their potential activity against the parasite; the Silvio (ATCC-50799) strain was used in all analyzes. Plants with at least one of its parts with a IC50<100 ug / mL were: Beilschmedia pendula, Bocconia frutescens, Guarea rhopalocarpa, Hydrocotyle mexicana, Povedadaphne quadriporata, Piper auritum, Ruagea glabra and Xanthosoma undipes. Most of the fresh extracts showed activity against T. cruzi. The species B. frutescens had the major number of active parts and only 3 of all the extracts studied showed some degree of toxicity. The impact that these findings represent alternatives in terms of treatment of Chagas disease.
... All in vitro assays were done as previously reported [34,35]. Strychnogucine B was evaluated in eight serial three-fold dilution from a DMSO stock solution of 4 mM (final concentration ranges: 20-0.009 and 40-0.018 ...
Strychnogucine B is a bisindole alkaloid previously isolated from Strychnos icaja that possesses promising in vitro antiplasmodial properties. This compound was synthesized in four steps from (−)-strychnine. As no acute toxicity was observed at the highest tested cumulative dose of 60 mg/kg, its in vivo antimalarial activity was determined intraperitoneally at 30 mg/kg/d in a Plasmodium berghei murine model. In the Petersʼs 4-d suppressive test, this alkaloid suppressed the parasitaemia by almost 36% on day 5 and 60% on day 7 compared to vehicle-treated mice. In addition to this interesting antimalarial activity, it showed moderate in vitro antitrypanosomal activity but no in vivo activity in an acute Trypanosoma brucei model. It was also inactive in vitro on Leishmania mexicana promastigotes. This highlights its selective antimalarial efficacy and leads to further investigation to assess its potential as new antimalarial lead compound.
... This study reports the anti-Trypanosoma activity of three of the 10 plant species, C. cordifolia, N. laevis, and P. angolensis, for the first time. The anti-Trypanosoma activity of the remaining seven plant species have been reported in previous studies(Abedo et al., 2013;Bero, Hannaert, Chataigné, Hérent, & Quenti-Leclercq, 2011;Ganfon et al., 2012;Kimani, Gathumbi, Auma, Ngeranwa, & Masiga, 2013;Mann et al., 2011;Shuaibu et al., 2008). The possible mechanisms of action are however unknown.M. lucida was the only extract observed to induce significant apoptosis-like cell death in Trypanosoma parasites through the externalization of phosphotidyl serine. ...
Trypanosomiasis, leishmaniasis, and malaria are protozoan infections of public health importance with thousands of new cases recorded annually. Control of these infection(s) with existing chemotherapy is limited by drug toxicity, lengthy parenteral treatment, affordability, and/or the emergence of resistant strains. Medicinal plants on the other hand are used in the treatment of various infectious diseases although their chemical properties are not fully evaluated. In this study, we screened 112 crude extracts from 72 selected Ghanaian medicinal plants for anti‐Trypanosoma, anti‐Leishmania, and anti‐Plasmodium activities in vitro and investigated their mechanisms of action. Twenty‐three extracts from 20 plants showed significant antiprotozoan activity against at least 1 of 3 protozoan parasites screened with IC50 values less than 20 μg/ml. Eleven extracts showed high anti‐Trypanosoma activity with Bidens pilosa whole plant and Morinda lucida leaf extracts recording the highest activities. Their IC50 (selectivity index [SI]) values were 5.51 μg/ml (35.00) and 5.96 μg/ml (13.09), respectively. Nine extracts had high anti‐Leishmania activity with Annona senegalensis and Cassia alata leaf extracts as the most active. Their IC50 (SI) values were 10.8 μg/ml (1.50) and 10.1 μg/ml (0.37), respectively. Six extracts had high anti‐Plasmodium activity with the leaf and stem‐bark extracts of Terminalia ivorensis recording the highest activity. Their IC50 (SI) values were 7.26 μg/ml (129.36) and 17.45 μg/ml (17.17), respectively. Only M. lucida at 25 μg/ml induced significant apoptosis‐like cell death in Trypanosoma parasites. Anti‐Leishmania active extracts induced varying morphological changes in Leishmania parasites such as multiple nuclei and/or kinetoplast, incomplete flagella division, or nuclear fragmentation. Active extracts may be potential sources for developing new chemotherapy against these infections.
... Keetia leucantha (synonym: Plectronia leucantha Krause) is a West African tree of the Rubiaceae, used to treat a variety of infections, including parasitic infections [139,140]. Ursolic acid (57) and oleanolic acid (58), along with other constituents were isolated from the leaves of this plant. An investigation of the antitrypanosomal activities of essential oil, the dichloromethane extract and isolated compounds on T. b. brucei bloodstream forms (Tbb BSF) and procyclic forms (Tbb PF) [131] showed that ursolic acid (57) and oleanolic acid (58) were the most bioactive tested compounds [131]. ...
Parasitic diseases continue to represent a threat on a global scale, particularly among the poorest countries in the world. This is particularly because of the absence of vaccines, and in some cases, resistance against available drugs, currently being used for their treatment. In this review emphasis is laid on natural products and scaffolds from African medicinal plants (AMPs) for lead drug discovery and possible further development of drugs for the treatment of parasitic diseases. In the discussion, emphasis has been laid on alkaloids, terpenoids, quinones, flavonoids and narrower compound classes of compounds with micromolar range activities against Schistosoma, Trypanosoma and Leishmania species. In each subparagraph, emphasis is laid on the compound subclasses with most promising in vitro and/or in vivo activities of plant extracts and isolated compounds. Suggestions for future drug development from African medicinal plants have also been provided. This review covering 167 references, including 82 compounds, provides information published within two decades (1997–2017).
Graphical Abstract
... The in vitro anti-leishmanial effects of essential oils from the leaves (LEO), stems (SEO) and the aerial parts of H. tuberculatum (LSEO) were investigated on Leishmania mexicana mexicana (L.m.m.) as described by [28]. The solutions were prepared in DMSO at 20 mg/ml. ...
Background:
Plants used for traditional medicine produce diverse and complex secondary metabolites exhibiting various medicinal properties. The medicinal plant Haplophyllum tuberculatum is used by native people against malaria and parasitic infections.
Methods:
In this study and in order to contribute for the search of new natural drugs for leishmaniasis, the essential oils of H. tuberculatum leaves, stems and aerial parts (leaves+stems) collected in two different periods, 2013 and 2015, and their components by GC/FID and GC/MS analyses were investigated. Those collected in 2013 were also re-analyzed two years later. The extracted oils were screened in vitro for anti-leishmanial activity on Leishmania mexicana mexicana (L.m.m.) promastigotes and cytotoxicity on the Chinese Hamster Ovary (CHO) cell line. Limonene (1.5 - 8%), its isomers (R- (+)-limonene and S-(-)-limonene), linalool and octanol were also tested.
Results:
Results showed that the chemical composition varied according to the year of collection. Though major compounds remain almost the same, qualitative and quantitative variations in the composition of the EOs can be observed between the two years of collection, with some minor compounds identified only in one type of samples. Variation in the composition were also observed in the re-analyzed volatile oils, showing stability concerns. The essential oils and R-(+)-limonene showed moderate anti-leishmanial activity. Their IC50range from 6.48 to 50.28 μg/ml. Cytotoxicity assays for theses volatile extracts, R- (+)-limonene and S- (-)-limonene on CHO cells showed relatively potent cytotoxicity with a selectivity index <10. Their CC50range from 27.79 to 82.56 μg/ml.
Conclusions:
The findings of the present study demonstrated that H. tuberculatum might not be considered as a natural source for production of new anti-leishmanial agents without further analyzing its eventual in vivo toxicity as well as that of major pure compounds.
... About ten million people are affected by this parasite these days. It is estimated that globally, one in every twenty individuals is affected by this parasite (Bero et al., 2011). Therefore, different bioactive compounds of medicinal plants can be widely used as a therapeutic source against these parasites. ...
The study was done to check the antimicrobial and antiprotozoal activity of different parts of Ballota pseudodictamnus (L.) Benth. These activities were then compared with the heavy metals toxicity of different parts, which plants accumulate in different concentrations in different parts. In in-vitro antileishmanial results ethanolic extract, chloroform and ethyl acetate fractions in roots of Ballota pseudodictamnus (L.) Benth showed antileishmanial activity. The ethanol, n-butanol and ethyl acetate fraction in stem revealed inhibition of amastigote form of leishmania. The ethanolic extract, chloroform, and n-butanol fraction in leaves showed inhibition of leishmanial parasite. In heavy metals study, Chromium was above permissible value in all parts except in leaves. Nickel was above WHO limit in roots. Cadmium and lead were beyond permissible limits in entire plant parts. Results revealed that different parts of the plant have different inhibition properties. So each part of plant should be checked for antimicrobial and antiprotozoal assay separately. It is concluded that various metals accumulates with miscellaneous concentrations in different plant parts.
... Oleanolic and ursolic acids and 8 ETT, previously identified in the crude dichloromethane extract [11,17], were quantified in this extract ( Table 1). The total of both acids represents 16.9% of this extract, with a majority of ursolic acid (14.2%). ...
Background
Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts.
Results
These eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC–UV methods. They account for about 19% of this extract (16.9% for acids and 1.8% for esters). These compounds were also identified in trace in the twigs decoction by HPLC-HRMS. Results also showed that extracts and esters did not produce any haemolysis, and were devoid of any acute toxicity at a total cumulative dose of 800 and 150 mg/kg respectively. Moreover, esters given intraperitoneally at 50 mg/kg/day to Plasmodium berghei-infected mice showed a very significant (p < 0.01) parasitaemia inhibition (27.8 ± 5.4%) on day 4 post-infection compared to vehicle-treated mice.
Conclusions
These results bring out new information on the safety of K. leucantha use and on the identification of anti-malarial compounds from its dichloromethane extract. Its activity can be explained by the presence of triterpenic acids and esters which in vivo activity and safety were demonstrated for the first time.
... According to Bero et al. (2011), the in vitro antileishmanial activity of a given crude extract or compound must have an IC 50 value of ≤20 μg/ml to possess a promising activity, whereas IC 50 values between 21 and 50 μg/ml, 50 and 100 μg/ml are considered to have moderate and low activity, respectively and that with an IC 50 > 100 μg/ml is considered inactive. ...
Background: Malnutrition in women can be categorized as the macro-and micro-nutrient malnutrition. Many women, particularly those living in developing countries like Ethiopia, are underweight and/or stunted. Nutritional status of mothers in Ethiopia is currently a major public health concern. There are three key factors of maternal nutrition that could have an impact on human milk composition: current dietary intake, nutrient store, and alterations in nutrient utilization.
Objective: The aim of this research was to study the relation between maternal nutritional status and contents iron, zinc and vitamin A in breast milk of mothers in a rural community in Southern Ethiopia.
Methods: Community-based cross sectional study was conducted from April to May 2012. Maternal anthropometric status, plasma level of ferritin, iron, zinc and retinol and breast milk composition was assessed. Energy and nutrient intakes were calculated using 24h recall method.
Results: The prevalence of iron deficiency anemia (using hemoglobin concentration), zinc deficiency (using plasma zinc) and vitamin A deficiency (using plasma retinol) among lactating mothers of 6 to 12 months of postpartum in Boricha, SNNP, district were 36%, 100% and 7.3%, respectively. The median calorie and nutrient intake of the lactating mothers were below the Estimated Average Requirement. Dietary intake of vitamin A (beta-carotene) showed a significant positive correlation (p<0.05, r=0.24) with plasma retinol concentration of lactating mothers. The plasma concentration of retinol also showed a significant correlation (p<0.05, r=0.23) with that of breast milk retinol concentration.
Conclusion: Maternal malnutrition is a serious problem in the study area. Maternal plasma retinol status was positively related to maternal intake of vitamin A and breast milk retinol concentration.
Key Words: Breast milk composition, dietary intake, plasma nutrient level, Boricha.
... It has long been used in West Africa as a traditional treatment for dysentery, coughs, constipation, trypanosomiasis and peptic ulcer disease (Okpo et al. 2011;Okpo et al. 2012). It has compounds with various beneficial effects such as antimicrobial, antiplasmodial, antitrypanosomal, antileishmanial, antinociceptive and antiinflammatory activity (Bero et al. 2009;Bero et al. 2011;Eneojo at al, 2011;Adebayo et al. 2014). Important information has been documented by Soladoye et al. (2010) that A. difformis also contains anti-cancer compounds. ...
Rivai RR, Wardani FF, Zulkarnaen RN. 2017. The effect of NPK fertilizer and planting media on plant growth and saponin content of the medicinal plant Anchomanes difformis. Nusantara Bioscience 9: 141-145. Anchomanes difformis (Blume) Engl., belongs to the aroid family (Araceae) and has potential as a medicinal plant. A. difformis has not in the past been widely cultivated by farmers in Indonesia, so if it is to be grown as a crop for medicinally active compounds, we must first find how best to cultivate it. The objective of the research described here was to determine an effective planting media and optimum dosage of a standard NPK fertilizer for A. difformis plant growth in pots, and saponin content of its rhizomes. The research was conducted at the Treub Laboratory and Garden Nursery, Center for Plant Conservation Botanic Gardens, Indonesian Institute of Sciences (LIPI). A completely randomized design with three replications was used to test a factorial arrangement of two treatment factors, namely: planting media of three types; and dosage of a standard NPK fertilizer (15% N, 15% P2O5, 15% K2O) at four levels. Results showed that for plant growth of Anchomanes difformis, a mixed medium of soil/cocopeat (1:1) was the best of the three media evaluated, and the application of the NPK fertilizer at a dosage equivalent to 100 kg/ha was the optimum fertilizer level. There was no statistical interaction between the treatment factors. The rhizomes of A. difformis had their highest level of saponin content when planted in the mixed soil/cocopeat (1:1) medium, and with NPK fertilizers at a dose level of 100 kg/ha.
... Natural products are potential sources of new and selective agents for the treatment of important tropical diseases caused by protozoans and other parasites [28][29][30]. The most active extract, Artemisia inculta, contains polyphenolic compounds like flavonoids and triterpenoids (Table 3) which are believed to have the ability to inhibit trypanosomal and leishmanial infections without significant toxicity to mammalian cells [31][32][33]. Different Artemisia species have been reported to have in vitro and in vivo activity against various Leishmania species; Artemisia annua leaves extract was proved to have leishmanicidal activity against L. donovani which causes visceral leishmaniasis [34,35]. The second promising plant is Malva sylvestris, reported in this study to have antileishmanial activity for the first time; it is an edible plant and people in Palestine used it extensively. ...
Herbal and traditional medicine is commonly and widely used in Palestine. There has been no ethno pharmacological study to document the usefulness of traditional or medicinal plants from Palestine against leishmaniasis, a spectrum of severe parasitic diseases that occur worldwide and is caused by protozoa of the genus Leishmania. The aim of the present study was to collect and analyze some of the traditionally used medicinal plants from Palestine against Leishmania major parasites that cause cutaneous leishmaniasis. Plant materials were collected during spring and summer of the year 2011, identified and the voucher numbers were kept at Al-Quds University Gardens (AQUG). The whole plant (except roots), flowers, fruits or seeds were collected, washed with distilled water, air dried in the shade for 20 days and then powdered in an electric grinder. For each plant species, alcoholic and dimethyl sulfoxide extracts were tested in vitro against L. major promastigotes and their antileishmanial activities were evaluated by Alamar Blue bioassay. Twenty plant species belonging to14 families were examined for their in vitro anti-parasitic effect against L. major. Among the total crude extracts tested; five were found to have various levels of activities (20%), some extracts having significant antileishmanial activity with IC 50 values ranging from 8.83 to 100 µg/mL. The most active crude extracts were from the shoots of Artemisia inculta and Malva sylvestris with activity of 84.1%, IC 50 = 8.8 µg/mL. And 90.1%, IC 50 = 19.5 µg/mL respectively. The results demonstrate that the crude extracts of Artemisia inculta and Malva sylvestris showed promising antileishmanial activity, further and extensive studies should be carried out; particularly bio-guided fractionation to identify the active fraction and further chemical characterization of structure ABBREVIATIONS
... Recent studies on K. leucantha (K. Krause) Bridson, which is used in traditional medicine in Benin, found significant antiplasmodial, antitry panosomial and antileishmanial activity of leaf and twig extracts in in vitro conditions (Bero et al., 2009(Bero et al., , 2011. Most of the other Keetia species have not yet been tested pharmacologically, and it would be highly interesting to know if they show similar properties. ...
A new species of Rubiaceae from the Democratic Republic of Congo, Keetia namoyae O. Lachenaud & Q. Luke, is described and illustrated. The species resembles Keetia tenuifora (Hiern) Bridson and Keetia mannii (Hiern) Bridson, but difers from both in having alternate (not opposite) fowering twigs with stif appressed hairs, few-fowered inforescences, a longer corolla tube, and larger fruits. The species is only known from the type locality in Maniema Province, and is assessed to be "Critically Endangered" according to IUCN Red List Categories and Criteria.
... Reported biological activities of A. hispidum include abortifacient and teratogenic activity [15], antiviral, [16] antimicrobial, [17] antiplasmodial [18], antidiarrheoal [19], antitumour [20], antibacterial [21], anthelmintic [22], and antitrypsomal [23]. ...
Age related memory loss is a common occurrence in traditional medical practice and several medicinal plants have been used over the years for managing it. Acanthospermum hispidum DC (Asteraceae) is a medicinal plant that has been included in traditional preparations used in the management of memory loss. In clinical practice however, anticholinesterases have remained relevant in managing memory and cognition dysfunction associated both with old age and certain neurodegenerative diseases. In vitro anticholinesterase activity of extracts and fractions of A. hispidum was done using Ellman’s colorimetric and TLC bioautography assay with eserine as control. The ethyl acetate fraction of A. hispidum showed highest inhibition to acetylcholinesterase and butyrylcholinesterase (91.11% and 64.31%, respectively) in a concentration-dependent manner. A. hispidum presents a good prospect in the development of cholinesterase inhibitors for the management of memory-related disorders.
Keywords: Acanthospermum hispidum, Anticholinesterase, acetylcholinesterase, butyrylcholinesterase
... Previous studies have demonstrated that a number of Asteraceae families displayed important antileishmanial activity [42]. In fact, the dichloromethane fraction from aerial parts of Acanthospermum hispidum used in traditional medicine in Benin as antiparasitic agents showed the best activity against L. Mexicana promastigote (IC50 = 11.1 g/mL) [43]. The same study has reported that dichloromethane and ethyl acetate fractions of Maytenus senegalensis exhibited the highest antileishmanial activity at 5 mg/mL. ...
In the present study the phytochemical composition and biological activities of the aerial part extracts of Asteriscus graveolens against pathogenic bacteria and leishmania parasite were evaluated. Phytochemical analysis revealed the presence of polyphenols, flavonoids and tannins. The ethyl acetate fraction exhibited high antioxidant potential of 359.72 ± 32.03 μg and 326.76 ± 15.86 μg of ascorbic acid equivalents and 13.32 ± 0.19 μg/mL by PM, FRAP and DPPH assays respectively. This fraction also displayed a moderate antibacterial activity against Listeria monocytogenes ATCC 19115 (MIC = 0.312 mg/mL) and strong antileishmanial activity against both promastigote and amastigote forms with IC50 ranging from 22.93 ± 0.39 μg/mL to 35.23 ± 0.62 μg/mL. Furthermore the ethyl acetate fraction exhibited low cytotoxicity and good selectivity index towards the macrophage cell line Raw 264.7. HPLC analysis of the active fraction revealed the presence of hydroxycinnamic acid as major compound (30.56%). Asteriscus graveolens is a promising source of bioactive compounds that could be potentially used in cosmetic and pharmaceutical industry.
Background: Medicinal herbs are used to cure parasitic protozoan diseases. Protozoan parasites continue difficult
to treat, but diverse extracts from both terrestrial and aquatic plants have been shown to provide a variety of
medical benefits for people’s personal health. One of the main issues in the management of health and disease is
the absence of treatment resistance in parasites. It affects millions of people’s health globally, poses a threat to
get worse, and threatens to cause financial losses. Drug resistance in parasites is progressively complex and
challenging the treatment of parasitic disorders, which is disappointing because it does not receive serious
consideration from every part of society.
Methods: In this regard, our focus has been on examining the antiparasitic plants of the Asteraceae family and
their potential use in the management of protozoan parasites.
Results: This review is divided into a i) analysis of traditional parasite treatments using Asteraceae plants (ii) an
overview of the major chemical classes found in Asteraceae and their effects on parasites; (iii) with special focus
on flavonoids, terpenoids, and alkaloids, antiparasitic properties. In-depth information on isolated bioactive
compounds that can inhibit protozoan parasites such Plasmodium, Leishmania, Trypanosoma, Entamoeba, and
Toxoplasma is provided in this study. It also includes information on Asteraceae plant extracts that have been
reported around the globe.
Conclusion: These medicinal plants can be further studied to determine whether they have the potential to be
turned into novel pharmaceuticals or utilised as a medicinal plant to treat a variety of protozoan diseases.
Neglected tropical diseases (NTDs) such as leishmaniasis, filariasis, trypanosomiasis, and schistosomiasis have claimed the lives of over one billion people, mainly affecting the less privileged in Africa and Asia. In the face of the fact that obtainable actions for these ailments are of limited effectiveness and often highly toxic, there has been scarce attention in developing improved therapeutics as there would be little commercial value in the treatment of these poor patient populations. This chapter explores new, inexpensive, and efficient therapeutics from medicinal plants and phytochemicals for these diseases. The probable druggable targets were also discussed.
Introduction: The present study was carried out to identify the phytochrmicals and antidiabetic activity of Sansevieria liberica leaves
Introduction: The present study was carried out to identify the phytochrmicals and antidiabetic activity of Sansevieria liberica leaves
The recent massive reduction in the numbers of fresh Human African Trypanosomiasis (HAT) infection has presented an opportunity for the global elimination of this disease. To prevent a possible resurgence, as was the case after the reduced transmission of the 1960s, surveillance needs to be sustained and the necessary tools for detection and treatment of cases need to be made available at
the points of care. In this review, we examine the available resources and make recommendations for improvement to ensure the sustenance of the already achieved gains to keep the trend moving
towards elimination.
Leishmaniasis is one ignored ailment in the area of new drug and drug delivery research that is caused by different intercellular protozoan species of the genus Leishmania. Pentavalent antimonials are currently the drugs of choice against leishmaniasis in the endemic regions, but due to the emerging incidence of pentavalent antimonial drug resistance in endemic and nonendemic regions, their use has been hindered. Therefore treatment of leishmaniasis remains a major public health issue. Presently, combined therapies have been used to reduce the duration of therapy and cost of treatment. Recently, researchers have focused on the potential of phytoconstituents having antileishmanial activity. The chapter emphasizes on the current status of leishmaniasis, therapeutic options presently available, prophylactic vaccines, and various approaches for drug targeting that are being developed for the effective and safe …
New anti-infective agents are urgently needed to fight microbial resistance. Methicillin-resistant Staphylococcus aureus (MRSA) strains are particularly responsible for complicated pathologies that are difficult to treat due to their virulence and the formation of persistent biofilms forming a complex protecting shell. Parasitic infections caused by Trypanosoma brucei and Leishmania mexicana are also of global concern, because of the mortality due to the low number of safe and effective treatments. Female inflorescences of hop produce specialized metabolites known for their antimicrobial effects but underexploited to fight against drug-resistant microorganisms. In this study, we assessed the antimicrobial potential of phenolic compounds against MRSA clinical isolates, T. brucei and L. mexicana. By fractionation process, we purified the major prenylated chalcones and acylphloroglucinols, which were quantified by UHPLC-UV in different plant parts, showing their higher content in the active flowers extract. Their potent antibacterial action (MIC < 1 µg/mL for the most active compound) was demonstrated against MRSA strains, through kill curves, post-antibiotic effects, anti-biofilm assays and synergy studies with antibiotics. An antiparasitic activity was also shown for some purified compounds, particularly on T. brucei (IC50 < 1 to 11 µg/mL). Their cytotoxic activity was assessed both on cancer and non-cancer human cell lines.
The purpose of this review is to survey the antiparasitic plants of the Asteraceae family and their applicability in the treatment of parasites. This review is divided into three major parts: (a) literature on traditional uses of Asteraceae plants for the treatment of parasites; (b) description of the major classes of chemical compounds from Asteraceae and their antiparasitic effects; and (c) antiparasitic activity with special reference to flavonoids and terpenoids. This review provides detailed information on the reported Asteraceae plant extracts found throughout the world and on isolated secondary metabolites that can inhibit protozoan parasites such as Plasmodium, Trypanosoma, Leishmania, and intestinal worms. Additionally, special attention is given to the Asteraceae plants of Odisha, used by the tribes of the area as antiparasitics. These plants are compared to the same plants used traditionally in other regions. Finally, we provide information on which plants identified in Odisha, India and related compounds show promise for the development of new drugs against parasitic diseases. For most of the plants discussed in this review, the active compounds still need to be isolated and tested further.
Sudan folklore medicine is characterized by a unique combination of Islamic, Arabic, and African cultures. In poor communities, traditional medicine has remained as the most reasonable source of treatment of several diseases and microbial infections. Although the traditional medicine is accepted in Sudan, to date there is no updated review available, which focuses on most effective and frequently used Sudanese medicinal plants. Thus, this review aims to summarize the published information on the ethnobotanical uses of medicinal plants from Sudan, preparation methods, phytochemistry, and ethnopharmacology. The collected data demonstrate that Sudanese medicinal plants have been reported to possess a wide range of traditional medicinal uses including different microbial infections, gastrointestinal disorders, malaria, diabetes, rheumatic pain, respiratory system disorders, jaundice, urinary system inflammations, wounds, cancer, and different microbial infections. In most cases, the pharmacological studies were in agreement with traditional uses. Moreover, several bioactive compounds such as flavonoids, saponins, alkaloids, steroids, terpenes, tannins, fatty acids, and essential oils have been identified as active constituents. Although this review demonstrates the importance of ethnomedicine medicines in the treatment of several diseases in Sudan, further researches to validate the therapeutic uses and safety of these plants through phytochemical screening, different biological activity assays, and toxicological studies are still needed. © 2017 Pharmacognosy Reviews | Published by Wolters Kluwer - Medknow.
In order to establish the possible relationship between their chemical structures and pharmacological properties, the oral and topical anti-inflammatory activities of ten triterpenoids belonging to the lupane, oleanane, and ursane series, were evaluated. All triterpenoids were remarkably active against the edema produced by TPA. While the basic carbon skeleton has no influence on the activity, the presence of a C-28 or C-30 carboxylic group and an alcoholic group at C-28 increases the activity in carrageenan- and EPP-induced edemas, respectively.
Cassytha filiformis (Lauraceae), a widely distributed parasitic plant, contains several aporphine alkaloids and is often used in African folk medicine to treat cancer, African trypanosomiasis and other diseases. In a previous investigation, we showed that the alkaloid plant extract and the isolated aporphines possessed in vitro cytotoxic properties. In this paper, we evaluated the in vitro activity of the alkaloid extract (IC50 = 2.2 microg/mL) and its three major aporphine alkaloids (actinodaphnine, cassythine, and dicentrine) on Trypanosoma brucei brucei as well as four related commercially available aporphines (bulbocapnine, glaucine, isocorydine, boldine). Only the three alkaloids from Cassytha filiformis were active on the trypanosomes in vitro (IC50 = 3-15 microM). Additionally, we compared the cytotoxicity of these seven compounds on HeLa cells. Glaucine was the most cytotoxic compound on HeLa cells (IC50 = 8.2 microM) in the series. In order to elucidate their mechanism of action, the binding mode of these molecules to DNA was studied by UV absorption, circular and linear dichroism spectroscopy. The results of the optical measurements indicated that all seven aporphines effectively bind to DNA and behave as typical intercalating agents. Biochemical experiments showed that actinodaphnine, cassythine and dicentrine also interfere with the catalytic activity of topoisomerases in contrast to the four other aporphines. These interactions with DNA may explain, at least in part, the effects observed on cancer cells and on trypanosomes.
Bioassay-guided fractionation of a Satureja parvifolia MeOH extract led to the isolation of eriodictyol, luteolin and ursolic and oleanolic acids as its active components against Plasmodium falciparum K1. This is the first time these compounds are reported as constituents of S. parvifolia. Ursolic acid showed an IC
Besides, the four compounds showed activity against P. falciparum 3D7 strain and Trypanosoma brucei rhodesiense. Eriodictyol showed moderate activity on all the parasites but was the most selective compound as a result of its rather low cytotoxicity (IC
Fractionation of an antitrypanosomal lipophilic leaf extract from Strychnos spinosa led to the isolation of eight triterpenoids and sterols in this plant part for the first time. Two of these were found to possess in vitro antitrypanosomal activity, namely, saringosterol (14) and 24-hydroperoxy-24-vinylcholesterol (15), with IC(50) values of 7.8 +/- 1.2 and 3.2 +/- 1.2 microM, respectively. The latter compound was isolated from a plant source for the first time. A comparative study on the antitrypanosomal activity of the isolated triterpenoids and sterols and some related compounds has indicated that the presence of an oxygenated function at C-28 or an oxygenated side chain at C-17 seems to be important for the antitrypanosomal activity of triterpenoids and sterols, respectively.
Purpose: Terminalia arjuna Roxb (Combretaceae) is commonly known as Arjjhan and Arjun in Bengal, India. The anti-leishmanial and anticancer activities of a pentacyclic triterpenoid isolated from its leaves were evaluated. Methods: Dried and crushed leaves of Terminalia arjuna were de-fatted with petroleum ether (40 -60°C) and extracted with methanol. The extract was subjected to column chromatography and column fractions were monitored on TLC plates developed in a suitable solvent system. Structures of the isolated pure compounds were elucidated by infra-red spectroscopy, mass spectrometry and nuclear magnetic resonance spectroscopy. One of the compounds was screened for anti-leishmanial activity against promastigotes of Leishmania donovani, and anti-cancer activity on K562 leukaemic cell line. Results: A pentacyclic triterpenoid, characterized as 3β-hydroxyurs-12-en-28-oic acid (together with ß-D-glucoside) and designated ursolic acid, was successfully isolated. The structure was determined on the basis of spectroscopic analyses. In vitro anti-leishmanial activity against promastigotes of Leishmania donovani (strain AG 83) and anti-cancer activity on K562 leukaemic cell line were shown by the isolated ursolic acid. Conclusion: The methanol extract of the leaves of Terminalia arjuna led to the isolation of a pentacyclic triterpenoid, ursolic acid. This compound demonstrated in vitro anti-leishmanial and anti-cancer activities.
In order to establish the possible relationship between their chemical structures and pharmacological properties, the oral and topical anti-inflammatory activities of ten triterpenoids belonging to the lupane, oleanane, and ursane series, were evaluated. All triterpenoids were remarkably active against the edema produced by TPA. While the basic carbon skeleton has no influence on the activity, the presence of a C-28 or C-30 carboxylic group and an alcoholic group at C-28 increases the activity in carrageenan- and EPP-induced edemas, respectively.
Purpose: Terminalia arjuna Roxb (Combretaceae) is commonly known as Arjjhan and Arjun in Bengal, India. The anti-leishmanial and anticancer activities of a pentacyclic triterpenoid isolated from its leaves were evaluated.Methods: Dried and crushed leaves of Terminalia arjuna were de-fatted with petroleum ether (40-60°C) and extracted with methanol. The extract was subjected to column chromatography and column fractions were monitored on TLC plates developed in a suitable solvent system. Structures of the isolated pure compounds were elucidated by infra-red spectroscopy, mass spectrometry and nuclear magnetic resonance spectroscopy. One of the compounds was screened for anti-leishmanial activity against promastigotes of Leishmania donovani, and anti-cancer activity on K562 leukaemic cell line.Results: A pentacyclic triterpenoid, characterized as 3ß-hydroxyurs-12-en-28-oic acid (together with ß- D-glucoside) and designated ursolic acid, was successfully isolated. The structure was determined on the basis of spectroscopic analyses. In vitro anti-leishmanial activity against promastigotes of Leishmania donovani (strain AG 83) and anti-cancer activity on K562 leukaemic cell line were shown by the isolated ursolic acid.Conclusion: The methanol extract of the leaves of Terminalia arjuna led to the isolation of a pentacyclic triterpenoid, ursolic acid. This compound demonstrated in vitro anti-leishmanial and anti-cancer activities
The EtOH, CH2Cl2, and petroleum ether extracts from Morinda lucida. Benth. leaves have been shown to exhibit an in vitro. antiplasmodial activity against a chloroquine-sensitive Plasmodium falciparum. strain with IC50 values 5.7 ± 1.3, 5.2 ± 0.8, and 3.9 ± 0.3 µg/mL, respectively. In vivo., at a daily oral dose of 200 mg/kg body weight, they produced at least 62.5%, 67.5%, and 72.2% reduction of parasitemia in mice infected with Plasmodium berghei berghei., respectively. A bioassay-guided fraction of the most active petroleum ether extract resulted in the isolation of two known triterpenic acids as ursolic acid 1 and oleanolic acid 2. In vitro., 1 and 2 exhibited an antiplasmodial activity with IC50 values of 3.1 ± 1.3 and 15.2 ± 3.4 µg/mL, respectively. In vivo., at a daily dose of 200 mg/kg body weight, they produced 97.7% and 37.4% chemosuppression, respectively. However, all tested samples were inactive in vitro. against chloroquine-resistant Plasmodium falciparum. (K1) at the highest tested concentration of 25 µg/mL.
The present study evaluates the in vitro and in vivo trypanocidal activity of ursolic acid and oleanolic acid against the Bolivia strain of Trypanosoma cruzi. Their acute toxicity is also assessed on the basis of median lethal dose (DL50) determination and quantification of biochemical parameters. Ursolic acid is the most active compound in vitro, furnishing IC50 of 25.5 microM and displaying 77% of trypomastigote lysis at a concentration of 128 microM. In agreement with in vitro assays, the results obtained for the in vivo assay reveals that ursolic acid (at a dose of 20 mg/Kg/day) provides the most significant reduction in the number of parasites at the parasitemic peak. Results concerning the LD50 assay and the biochemical parameters evaluated in the present study demonstrate that these substances can be safely used on an experimental basis.
The aim of the study was to evaluate the in vitro antiplasmodial activity of crude extracts of 12 plant species traditionally used in Benin for the treatment of malaria in order to validate their use.
For each species, dichloromethane, methanol and total aqueous extracts were tested. The antiplasmodial activity of extracts was evaluated using the measurement of the plasmodial lactate dehydrogenase activity on chloroquine-sensitive (3D7) and resistant (W2) strains of Plasmodium falciparum. The selectivity of the different extracts was evaluated using the MTT test on J774 macrophage-like murine cells and WI38 human normal fibroblasts.
The best growth inhibition of both strains of Plasmodium falciparum was observed with the dichloromethane extracts of Acanthospermum hispidum DC. (Asteraceae) (IC(50)=7.5 microg/ml on 3D7 and 4.8 microg/ml on W2), Keetia leucantha (K. Krause) Bridson (syn. Plectronia leucantha Krause) (Rubiaceae) leaves and twigs (IC(50)=13.8 and 11.3 microg/ml on 3D7 and IC(50)=26.5 and 15.8 microg/ml on W2, respectively), Carpolobia lutea G.Don. (Polygalaceae) (IC(50)=19.4 microg/ml on 3D7 and 8.1 microg/ml on W2) and Strychnos spinosa Lam. (Loganiaceae) leaves (IC(50)=15.6 microg/ml on 3D7 and 8.9 microg/ml on W2). All these extracts had a low cytotoxicity.
Our study gives some justifications for the traditional uses of some investigated plants.
The drug sensitivities of eleven Trypanosoma evansi isolates from China were examined using two different in vitro assays, a 3H-hypoxanthine incorporation assay and a long incubation low inoculation test (LILIT). Better discrimination of the drug susceptibility of the strains was observed with the LILIT. The drug responses of all the isolates to the arsenical melarsoprol were very similar. In contrast, for suramin, minimal inhibitory concentrations (MIC) varied within a 27-fold range and for diminazene within a 55-fold range. Comparison of MIC values with expected drug levels in the host as well as in vivo experiments with selected isolates and drugs indicated that all the isolates examined would be sensitive to melarsoprol, diminazene and suramin under in vivo conditions. For isometamidium, the difference in MIC values between the most and the least sensitive isolate was 724-fold. Neither of two isolates tested in mice--the most resistant and the second most sensitive--was cured with the highest acceptable dose of 10 mg kg-1 isometamidium chloride. Comparison of our results with blood levels of drug to be expected in cattle support the assumption that the Chinese T. evansi isolates have more or less innate resistance to isometamidium under in vivo conditions. One Trypanosoma equiperdum isolate was tested in the 3H-hypoxanthine incorporation assay. The results indicated that this isolate was highly sensitive to melarsoprol, isometamidium and suramin; with regard to diminazene, T. equiperdum was not as sensitive as the most sensitive T. evansi strains.
The MeOH extract of the leaves of rosemary (Rosmarinus officinalis L.) completely inhibited the motility of cultured epimastigotes of Trypanosoma cruzi at the concentration of 2 mg/ml after 2 h of incubation. Activity-guided fractionation of the MeOH extract has resulted in the isolation of three triterpene acids, betulinic, oleanolic and ursolic acids. Ursolic acid stopped the movement of all T. cruzi epimastigotes at the minimum concentration (MC(100)) of 40 micro g/ml (88 micro M) after 48 h of incubation. Oleanolic acid was less active (MC(100): 250 micro g/ml, 550 micro M) and betulinic acid was practically inactive.
The bioassay-guided fractionation of methylene chloride extracts of Miconia fallax DC. and Miconia stenostachya DC. led to the isolation of five triterpene acids. The triterpenes ursolic acid, oleanolic acid and gypsogenic acid were active against blood trypomastigote forms of Trypanosoma cruzi. In contrast, the acetyl and methyl ester derivatives were not found to potentiate the trypanocidal activity. These results suggest the importance of the polar groups for activity.
The inhibiting activity of triterpenoids isolated from the methanolic extract of Pourouma guianensis (Moraceae) leaves is described for promastigotes and intracellular amastigotes of Leishmania amazonensis. Whereas the fractions containing apigenin, friedelin, epi-friedelinol, arjunolic acid, hyptatic acid B, stigmasterol and sitosterol were of no or relatively low inhibitory activity, fractions containing tormentic acid, 2alpha,3beta-dihydroxyursan-12-en-28-oic acid, 2alpha,3beta-dihydroxyolean-12-en-28-oic acid, oleanolic acid and ursolic acid were very potent in inhibiting promastigote growth at 100 microg/ml. Of the eleven isolated compounds, however, only ursolic acid and oleanolic acid showed high activity against intracellular amastigotes (IC50 value = 27 microg/ml and 11 microg/ml, respectively), which was superior to the control drug Glucantime (IC50 value = 83 microg/ml). The antileishmanial activity of oleanolic acid was directed against the parasite and not due to activation of nitric oxide intermediates by macrophages, but this triterpenoid also significantly inhibited the phagocytic capacity of those cells at concentrations above 40 microg/ml, indicating a cytotoxic effect. These results indicate that Pourouma guianensis contains many triterpenoids and some, such as ursolic and oleanolic acids, may serve as lead compounds for new antileishmanial drugs, but chemical modifications may be necessary to avoid unselective cytotoxicity.
In this article, Hiroyuki Hirumi and Kazuko Hirumi review recent technical developments of in vitro systems that support the growth of bloodstream forms of African trypanosomes in the absence of mammalian feeder layer cells, which were required in earlier methods.
From the leaves of Ilex affinis and Ilex buxifolia, two adulterant species of "erva mate" (Ilex paraguariensis), three new triterpenoid glycosides were isolated. Affinoside 1 (3beta-O-[beta-D-glucopyranosyl-(1-->3)-[2-O-acetyl-(1-->2]]-alpha-L-arabinopyranosyl pomolic acid 28-O-beta-D-glucopyranosyl ester, 1) was isolated from I. affinis, while buxifolioside I (28-O-beta-D-glucopyranosyl ester of (20S)-3alpha,19alpha-dihydroxyurs-12-ene-23,28-dioic acid, 7) and buxifolioside II (28-O-beta-D-glucopyranosyl ester of (20S)-3beta,19alpha-dihydroxyurs-12-en-24,28-dioic acid, 8) were isolated from I. buxifolia. Along with these new compounds, ilexoside II (2), ursolic acid (3), 28-nor-ursolic acid (4), 3beta-O-acetylursolic acid (5), and uvaol (6) were also isolated. The observed results confirm the structural specificity of the I. paraguariensis triterpenoids and reinforce a previous proposal to detect mate adulteration by triterpenoid analysis. In addition, the in vitro antitrypanosomal activity of some Ilex triterpenoids is also reported.
Triterpene acids, including ursolic acid (1), urjinolic acid (4) and oleanoic acid (5) along with a mixture of 2alpha-hydroxyursolic acid (2) and maslic acid (3) were isolated from methylene chloride extracts of the Miconia sellowiana and M. ligustroides species and their activities against the trypomastigote blood forms of Trypanosoma cruzi were evaluated. The potassium salt derivative of ursolic acid (1a) was also tested. The in vitro assays showed that compounds 1, 5 and 1a were the most active (IC(50) 17.1 microm, 12.8 microm and 8.9 microm, respectively). In contrast, a mixture of 2 plus 3, that exhibit a hydroxyl at C-2 and C-3, is much less potent than a mixture of 1 and 5 (IC(50) 48.5 microm and 11.8 microm, respectively). In the same manner, compound 4, that differs from 5 by two additional hydroxyl groups (at C-2 and C-23) displayed weak trypanocidal activity (IC(50) 76.3 microm) when compared with the other triterpenes. These results suggest that the free hydroxyl at C-3 and the polarity of C-28 are the most influential structural features for determining the in vitro trypanocidal activity of triterpenes. In vivo assays were also undertaken for the most active compounds 1, 1a and the mixture of 1 plus 5. The most significant reduction in parasite number in the parasitemic peak were obtained for compound 1 and its salt derivative 1a (75.7% and 70.4%, respectively). Moreover, the survival time was increased for all the treated animals.
A series of new ursolic and oleanolic acids derivatives was synthesized via ursolic or oleanolic acids, previously extracted from South American Ilex species. These new compounds were tested for in vitro antiparasitic activity on Leishmania amazonensis and Leishmania infantum strains. Some of these compounds showed activity against the promastigote forms of L. amazonensis or L. infantum, with IC(50) ranging from 5 to 12 microM. As expected, most of the compounds showed a significant level of cytotoxicity against monocytes (IC(50) = 2-50 microM). From a structure-activity relationships point of view, these pharmacological results enlightened mainly the importance of an acetylation at position 3 of the oleanolic acid skeleton in the activity against the L. amazonensis strain, and of a bis-(3-aminopropyl)piperazine moiety on the carboxylic function of ursolic acid against the L. infantum strain.
- W R Cunha
- C Martins
- D D Ferreira
- A F M Crotti
- N P Lopes
- S Albuquerque
Cunha, W.R., Martins, C., Ferreira, D.D., Crotti, A.F.M., Lopes, N.P., Albuquerque, S.,
2003. In vitro trypanocidal activity of Triterpenes from Miconia species. Planta
Medica 69, 470–472.
The WHO programme to eliminate sleeping sickness
World Health Organisation (WHO), 2002. The WHO programme to eliminate sleeping sickness. WHO/CDS/CSR/EPH/2002.13.
- R K Cimanga
- G L Tona
- G K Mesia
- O K Kambu
- D P Bakana
- P D T Kalenda
- A O Penge
- J J T Muyembe
- J Totte
- L Pieters
- A J Vlietinck
Cimanga, R.K., Tona, G.L., Mesia, G.K., Kambu, O.K., Bakana, D.P., Kalenda, P.D.T.,
Penge, A.O., Muyembe, J.J.T., Totte, J., Pieters, L., Vlietinck, A.J., 2006. Bioassayguided isolation of antimalarial triterpenoid acids from the leaves of Morinda
lucida. Pharmaceutical Biology 44, 677–681.