Holarrhena Floribunda Research Articles

Ethnobotanical Survey and Biological Activities of Two Lactogenic Plants in the Cascades Region of Burkina Faso

An ethnobotanical survey for a better knowledge of lactogenic plants has been conducted in Cascades region of Burkina Faso. Biological activities of the two most used plants were evaluated. The survey concerned 25 species classified into 22 genera and 19 families. The most represented families were Moraceae, Apocynaceae, Fabaceae-Caesalpinioideae and Malvaceae. The most used species were Euphorbia hirta, Calotropis procera and Ficus sycomorus with respectively 16.98%, 13.21% and 13.21% followed by Ficus platyphylla (9.43%) and Carica papaya, Holarrhena floribunda, Scoparia dulcis, Sorghum bicolor, each with 3.77% of frequency use. Plants organs mostly used for medicinal preparation were leaves, whole plant for herbaceous species, fruits and seeds. The main mode of medicinal preparation was decoction with 60.42% of frequency use. The most route of administration was oral (68.75%). Biological activities evaluation concerned Euphorbia hirta and Calotropis procera which were the most used plants. The acute toxicity of aqueous extracts of Calotropis procera (AECP) and Euphorbia hirta (AEEH) showed a LD50 of 2063 and 603 mg/kg body weight (b.w), respectively. These LD50 values permitted to classify these plants as slightly toxic herbal drugs. The uterotrophic test showed that the AECP and AEEH exhibited estrogenic activity. In conclusion, important medicinal plants in the Cascades region of Burkina Faso were used to stimulate or ameliorate lactation. However further studies must be conducted to confirm the traditional use of these plants.

Hepatic tolerance of an ethyl acetate extract of Holarrhena floribunda (G. Don) Durand and Schinz leaves in Wistar Rats

Purpose: This study aims to evaluate the hepatic biochemical effects associated with the use of ethyl acetate extract of Holarrhena floribunda leaves as a traditional medicine. Methods: The rats were randomly divided into four groups of 10 (male control, female control, male test and female test) and combined with four groups of 5 (male control satellite, female control satellite, male test satellite and female test satellite) were force-fed for 90 days. The control and control satellite control rats received distilled water at a rate of 2 mL / 100g PC, and treated and treated satellite treated rats received the 1000 mg / kg PC dose of the acetate extract of ethyl leaves of Holarrhena floribunda. The blood collected each week during the first month, then at the end of each month as of the 2nd month allowed to assay liver serum markers such as ALT, ASAT, PAL, LDH, total bilirubin, direct bilirubin, albumin, glucose, HDL-cholesterol, LDL-cholesterol, total cholesterol and triglycerides. Results: The animals were well supported gavage of the extract since no sign of pathological manifestation was observed on them. The biochemical analysis indicated on the one hand a significant decrease in the level of total cholesterol, glucose (in both sexes), LDL cholesterol (in the female rats), and on the other hand an increase in the HDL cholesterol level (in both sexes), the rate of ASAT activities (in female rats) and PAL (in rats). On the other hand serum levels of total bilirubin, direct bilirubin, albumin, triglycerides, activities of ALT and LDH did not significantly vary. Microscopic observations of the liver tissue sections of the rats in the test lot did not show any lesions. Conclusion: Administration of the ethyl acetate extract of Holarrhena floribunda leaves to the rats for 90 days did not interfere with liver function or cause liver tissue damage.

Steroid Alkaloids from Holarrhena africana with Strong Activity against Trypanosoma brucei rhodesiense.

In our continued search for natural compounds with activity against Trypanosoma brucei, causative agent of human African trypanosomiasis (HAT, “sleeping sickness”), we have investigated extracts from the leaves and bark of the West African Holarrhena africana (syn. Holarrhena floribunda; Apocynaceae). The extracts and their alkaloid-enriched fractions displayed promising in vitro activity against bloodstream forms of T. brucei rhodesiense (Tbr; East African HAT). Bioactivity-guided chromatographic fractionation of the alkaloid-rich fractions resulted in the isolation of 17 steroid alkaloids, one nitrogen-free steroid and one alkaloid-like non-steroid. Impressive activities (IC50 in µM) against Tbr were recorded for 3β-holaphyllamine (0.40 ± 0.28), 3α-holaphyllamine (0.37 ± 0.16), 3β-dihydroholaphyllamine (0.67 ± 0.03), N-methylholaphyllamine (0.08 ± 0.01), conessimine (0.17 ± 0.08), conessine (0.42 ± 0.09), isoconessimine (0.17 ± 0.11) and holarrhesine (0.12 ± 0.08) with selectivity indices ranging from 13 to 302. Based on comparison of the structures of this congeneric series of steroid alkaloids and their activities, structure-activity relationships (SARs) could be established. It was found that a basic amino group at position C-3 of the pregnane or pregn-5-ene steroid nucleus is required for a significant anti-trypanosomal activity. The mono-methylated amino group at C-3 represents an optimum for activity. ∆5,6 unsaturation slightly increased the activity while hydrolysis of C-12β ester derivatives led to a loss of activity. An additional amino group at C-20 engaged in a pyrrolidine ring closed towards C-18 significantly increased the selectivity index of the compounds. Our findings provide useful empirical data for further development of steroid alkaloids as a novel class of anti-trypanosomal compounds which represent a promising starting point towards new drugs to combat human African trypanosomiasis.

THERAPEUTIC POTENTIALS OF ETHANOLIC EXTRACT OF LEAVES OF HOLARRHENA FLORIBUNDA (G. DON) DUR. AND SCHINZ (APOCYNACEAE).

Background:Holarrhena floribunda is a plant of wide usage in the Togolese folk medicine. A previous ethnobotanical survey on the latex plants of the Maritime region of the country revealed that this plant was included in several recipes curing malaria and microbial infections. Therefore, this study aimed to seek for the effectiveness of the ethanolic extract of the plant in the treatment of these diseases.Methods:The antimicrobial test was performed using the agar well-diffusion and the NCCLS broth microdilution methods, while the in vivo antimalarial activity was evaluated following the four-day suppressive test of Peters. The acute toxic effects of the extract were monitored after a single oral dose (5,000 mg/kg body weight) administration in NMRI mice.Results:The results indicated that the ethanolic extract of leaves of H. floribunda was active on Staphylococcus aureus ATCC 29213 and clinical strains of Staphylococcus aureus, Salmonella typhi and Klebsiella pneumoniae with MICs ranging from 0.62 to 1.25 mg/mL. The extract also showed significant parasitaemia suppression in a dose-dependent manner. In the acute toxicity assay, the oral administration of the extract to the mice did not affect the relative weight of vital organs, and there were no signs of toxicity or death during the study period. The LD50 of the tested extract was found to be greater than 5,000 mg/kg, indicating its safety.Conclusion:This study demonstrates the antibacterial and antimalarial activities of leaves of H. floribunda and then, supports its medicinal use in the treatment of microbial infections.

Alpha-amylase Inhibition and Brine Shrimp Lethality Activities of Nine Medicinal Plant Extracts from South-West Nigerian Ethnomedicine

ABSTRACTAcanthospermum hispidum, Alchornea laxiflora, Calyptrochilum christyanum, Heliotropicum indicum, Holarrhena floribunda, Ipomoea asarifolia, Nauclea diderrichii, Piper guineense, and Tetracera scandens were extracted into methanol and screened for the availability of alpha-amylase inhibitors. Plant extracts’ toxicity was determined by brine shrimp lethality assay (BSLA). The most active plant, Nauclea diderichii, was fractionated into four solvent systems (n-hexane fractions, ethyl acetate, dichloromethane, and n-butanol) and tested. All the extracts showed varying degrees of alpha-amylase inhibitory activity. N. diderrichii with IC50 = 248.30 ± 0.27 µg.mL–1 had the highest inhibitory activity, while its butanol fraction with IC50 = 137.8 µg.mL–1 had activity comparable to the standard α-amylase inhibitor acarbose (IC50 = 177.50 ± 0.42 µg.mL–1). LC50 values for BSLA ranged from 11.35 to 1,127.50 µg.mL–1, with T. scandens being the most toxic with 11.35 µg.mL–1 and N. diderrichii the least toxic with 1,127.50 µg.mL–1.

Conessine Interferes with Oxidative Stress-Induced C2C12 Myoblast Cell Death through Inhibition of Autophagic Flux.

Conessine, a steroidal alkaloid isolated from Holarrhena floribunda, has anti-malarial activity and interacts with the histamine H3 receptor. However, the cellular effects of conessine are poorly understood. Accordingly, we evaluated the involvement of conessine in the regulation of autophagy. We searched natural compounds that modulate autophagy, and conessine was identified as an inhibitor of autophagic flux. Conessine treatment induced the formation of autophagosomes, and p62, an autophagic adapter, accumulated in the autophagosomes. Reactive oxygen species such as hydrogen peroxide (H2O2) result in muscle cell death by inducing excessive autophagic flux. Treatment with conessine inhibited H2O2-induced autophagic flux in C2C12 myoblast cells and also interfered with cell death. Our results indicate that conessine has the potential effect to inhibit muscle cell death by interfering with autophagic flux.

Isolation and antioxidant activity of flavonoids from Holarrhena floribunda (G.don) leaves.

Bioactive polyphenolics are ubiquitously present in plants and may play an important role in the prevention and management of certain human diseases. Three known flavonoids viz Kaemperol-3-O-rutinoside (1), quercetin-3-O-glucoside (2) and kaemperol-3-O-glucoside (3) and inseparable mixture (1:1) of quercetin-3-O-glucose/galactose (4) were isolated, and identified for the first time from Holarrhena floribunda. The antioxidant capacity using the ORAC, FRAP and TEAC assays and inhibition of lipid peroxidation were measured for isolated flavonoids. The result showed that compounds 2 and 4 showed significantly increased ORAC, TEAC, and FRAP activities with low pro-oxidant potential as well as improved lipid peroxidation inhibition levels when compared to compounds 1 and 3. The most active compounds were found to be flavonoids with a quercetin basic structure. These results imply that the isolated flavonoid glycosides are responsible for the antioxidant activity of the plant leaves and it forms the scientific basis for its traditional usage.

Alternative to Conventional Diabetic Management: The Antihyperglycaemic potential of an Ethyl Acetate Fraction Extract of Holarrhena floribunda

Alternative to Conventional Diabetic Management: The Antihyperglycaemic potential of an Ethyl Acetate Fraction Extract of Holarrhena floribunda

Beninese Medicinal Plants as a Source of Antimycobacterial Agents: Bioguided Fractionation and In Vitro Activity of Alkaloids Isolated from Holarrhena floribunda Used in Traditional Treatment of Buruli Ulcer.

Buruli ulcer (BU) imposes a serious economic burden on affected households and on health systems that are involved in diagnosing the disease and treating patients. Research is needed to find cost-effective therapies for this costly disease. Plants have always been an important source of new pharmacologically active molecules. Consequently we decided to undertake the study of plants used in traditional treatment of BU in Benin and investigate their antimycobacterial activity as well as their chemical composition. Extracts from forty-four (44) plant species were selected on account of reported traditional uses for the treatment of BU in Benin and were assayed for antimycobacterial activities. Crude hydroethanolic extract from aerial parts of Holarrhena floribunda (G. Don) T. Durand and Schinz was found to have significant antimycobacterial activity against M. ulcerans (MIC = 125 µg/mL). We describe here the identification of four steroidal alkaloids from Mycobacterium ulcerans growth-inhibiting fractions of the alkaloidal extract of the aerial parts of Holarrhena floribunda. Holadysamine was purified in sufficient amount to allow the determination of its MCI (=50 µg/mL). These results give some support to the use of this plant in traditional medicine.

In vitro antitrypanosomal activity, antioxidant property and phytochemical constituents of aqueous extracts of nine Nigerian medicinal plants

ObjectiveTo study the in vitro antitrypanosomal activity, antioxidant property and phytochemical constituents of aqueous extracts of nine Nigerian medicinal plants. MethodsIn vitro antitrypanosomal activity test was carried out on aqueous extracts of dried leaves of Acacia albida (A. albida), Artemisia absinthium, Bryophyllum pinnatum, Gongronema latifolium, Holarrhena floribunda, Leptadenia hastata, Pericopsis laxiflora (P. laxiflora) and dried stem barks of A. albida and P. laxiflora. The phytochemical constituents and composition of the extracts and the in vitro antioxidant activity of the extracts were subsequently measured using the α,α-diphenyl-β-picryl-hydrazyl (DPPH) radical scavenging assay, Ferric reducing antioxidant power (FRAP) assay, thiobarbituric acid (TBA) activity assay and H2O2 radical scavenging activity assay. ResultsFrom the study, it was discovered that the stem bark extracts of A. albida and P. laxiflora were most active against both Trypanosoma evansi and Trypanosoma congolense. There was complete cessation of motility in both trypanosomes within 5 min at 40 mg/mL of the stem bark extract of A. albida and complete cessation of motility within 25 min and 40 min at 40 mg/mL with P. laxiflora stem bark extract for Trypanosoma congolense and Trypanosoma evansi, respectively. Quantitative analysis of the phytochemical constituents of the aqueous extracts of the plant parts such as alkaloids, saponins, flavonoids and phenols revealed that the stem barks of A. albida, P. laxiflora and leaves of Leptadenia hastata contained relatively high amount of all the phytochemicals quantified. The stem bark extracts of A. albida, P. laxiflora and leaves of Gongronema latifolium possess more scavenging capacity when compared to other extracts in relation to vitamin C, the reference antioxidant. ConclusionsThis study provides scientific evidence for the use of A. albida, and P. laxiflora for the treatment of trypanosomosis and diseases associated with oxidative stress.

English

This work reports the activity (at various conditions) of conessine isolated from methanolic extract of Holarrhena floribunda, on the inhibition of the germination of two Bacillus spores species. This activity was studied by treating spores of Bacillus cereus T and Bacillus stearothermophilus CNCH 5781 with effective concentrations of conessine at various temperature, pH and treatment times. The inhibition of germination was evaluated by the culture of treated spores on agar medium and the number of colony obtained was compared with that of control culture (not treated with conessine). We found that conessine used at 50 and 100 µg/ml for 20 min each decreased considerably the germination of spore of B. cereus T and B. stearothermophilus CNCH 5781. The maximum temperature of conessine activity for B. cereus T was at 30 and 60°C for B. stearothermophilus CNCH 5781 spores. Furthermore, the activity of conessine was sensitive to pH change and was more effective at pH 6 on both bacterial spore strains. The treatment of spores with conessine at various lengths of time demonstrated that, the activity of the compound on both bacterial spores was strongly related to the bacterial species. This study suggested that the activity of conessine on the inhibition of germination of Bacillus spore depends on physico-chemical factors and the bacterial species.

Evaluation of antioxidant, antimutagenic, and lipid peroxidation inhibitory activities of selected fractions of Holarrhena floribunda (G. Don) leaves.

Exposure to environmental pollutants often leads to an upsurge in the production of reactive oxygen species (ROS). ROS oxidize cellular fatty acids to produce lipid peroxyl radicals, subsequently transformed into lipid peroxides, which decrease membrane fluidity and increase the activity of various enzymes implicated in degenerative diseases and cancer formation. Edible plants that contain exogenous compounds like curcumeroid, β-carotene, turmeric, and so on, protect the aerobic cells from oxidation of free radicals. This study thus evaluates antioxidant and antimutagenic activities of ethyl acetate, aqueous and methanolic fractions of Holarrhena floribunda leaves. Inhibitory activities of the ethyl acetate fraction on Fe(2+)-induced lipid peroxidation in hen egg yolk; rat liver and brain tissues were also evaluated. The Allium cepa root assay was used to evaluate antimutagenic activity. Results showed that the ethyl acetate scavenged DPPH, OH•, and •O2(-) much stronger than other fractions, as evidenced by its lowest respective IC50 values. All the fractions displayed antimutagenic activities against cyclophosphamide-induced chromosomal aberrations. Likewise, all the fractions induced a reduction in mitotic index, a hallmark of cytotoxicity in the root meristem of Allium cepa. The decrease in mitotic index was most profound for the ethyl acetate fraction, which also demonstrated a significant lipid peroxidation inhibitory activity in the liver and brain homogenates, but not in egg yolk, compared with the ascorbic acid standard. In general, the results suggest that the ethyl acetate fraction might contain beneficial phytochemicals that should be explored as novel candidates for preclinical drug development.

Studies of analgesic activity of the different fractions of Holarrhena floribunda stem bark in mice

The antinociceptive effect of crude extract of Holarrhena floribunda T.Durand & Schinz together with its fractions prepared with hexane, chloroform, ethylacetate, butanol and aqueous were investigated using hot plate, tail immersion and acetic acid-induced abdominal constriction tests in mice. Acute toxicity studies were carried out on the crude extract and fractions by oral and intraperitoneal administration using Lorkes (1983) method. The crude extract was prepared by soaking the stem bark in 70% ethanol for 72 hours. It was filtered and evaporated using rota vapour. The dry crude extract was dissolved in distilled water followed by butanol, ethylacetate, hexane and chloroform in a separating funnel to obtained the fractions. The result shows that the crude extract and the fractions were not toxic with the exception of butanol fraction. The crude extract and the fractions shows dose independent significant increase in latency period in the hot plate and tail immersion tests. They also reduced the abdominal constriction induced by acetic acid in mice. The analgesic effect of the extract and fractions were reversed by naloxone an opioid receptor antagonist in the hot plate and tail immersion test; while naloxone did not reverse the inhibitory effect of the extract and fractions on the acetic acid-induced abdominal constriction test. The results show that the central analgesic effect of the crude extract and fraction is mediated through opioid receptor in the brain. The peripheral analgesic effect of the extract and fractions is not mediated through opioid receptors.

Trypanocidal activity of the aqueous leave extract of <i>Holarrhena Africana (Apocynaceae)</i>

This study evaluated the trypanocidal activity of aqueous extracts of leaves of young Holarrhena africana. The trypanocidal activity was evaluated by treatment of mice infected with Trypanosoma brucei brucei at the peak of infection. The aqueous extract was administered intraperitoneally for 5 consecutive days with varied doses (100, 200,400 mg/kg weight). Treatment with the extract led to significant reduction in the level of parasitaemia in infected mice though relapse of parasitaemia occurred later. Parasite clearance by the extract was observed to be dose-dependent, the maximal effects being attained at the dose of 400 mg/kg body weight. There were also significant improvements in the packed cell volume and reduction in the severity of clinical sign / symptom of trypanosomiasis in the treated groups during and after administration ofextracts. A determination of the LD50 in acute toxicity studies showed that the extract was relatively safe at very high doses.

Phytochemical and microbial screening of herbal remedies in Akwa Ibom State, South Southern Nigeria

Ethanolic extracts of six commonly used medicinal plants (by traditional medicine practitioners in Uyo and Ikot-Ekpene), Vernonia amygdalina del. (“Etidod”), Ocimum gratissimum L. (“Nton”), Smilax anceps wild. (“Odufad”),Holarrhena floribunda (“Idid ikot”), Parkia biglobosa (“Epo igba”), and Khaya senegalensis (“Ogawo”), were analysed phytochemically and evaluated for their significant antimicrobial activity (P < 0.05) against different multiple drug resistant, MDR (pathogenic) organisms: Neisseria gonorrhea, Shigella flexineri, Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. Mean inhibitory zones were calculated for each of the extracts. Five of the plant extracts contain spanning and tannins only; two contain salkowski, and keller-kilini only, while three extracts contain just one of alkaloids, plobatannins, liberman. The results revealed that each of the six plants extracts, at different concentrations of 80 and 40 mg/ml, exhibited various degrees of inhibition and activity index on the test organisms. The extract of the O. graissimum (“Nton”), had the highest mean inhibitory zone of 23 mm against S. flexineri. This was followed by H. floribunda (“Idid ikot”) with a mean inhibitory zone of 22 mm against N. gonorrhoea, V. amygdalina(“Etidod”) with a mean inhibitory zone of 19 mm against S. aureus and S.anceps wild (“Odufad”) had a mean inhibitory zone of 17 mm against both N.gonorrhoea and S. aureus. The MIC results of S. flexineri in 26.24 mg/ml ofO. gratissimum excite us to analyse for its MBC which was 47.24 mg/ml. These results provide a rationalization for the traditional use of these plants for the treatment of infectious diseases. Key words: Ethanolic extract, phytochemical, pathogenic organisms, Smilax anceps, activity index.

Antibacterial activities of the extracts and conessine from Holarrhena floribunda G. Don. (Apocynaceae).

The methanolic extract and conessine isolated from the stem bark of Holarrhena floribunda (Hf) were tested for their antibacterial activities on Bacillus: Bacillus cereus, Bacillus subtilis, Bacillus megaterium and Bacillus stearothermophilus using the disc diffusion method. Phytochemical analysis of the crude extract and fractions was also conducted. The inhibition parameters of the crude methanol extract and the total alkaloid fraction were determined using the macrodilution method. The results showed that the crude extract, the total alkaloid fraction and conessine exhibited a significant antibacterial effect against all the strains studied. The antibacterial effect of conessine is almost similar to that of chloramphenicol used as reference. The ratio of the minimal bactericidal concentration (MBC) over the minimal inhibitive concentration (MIC) indicates the bactericidal effect of the plant. These results support common use of stem bark of Hf and conessine isolated from Hf in the treatment of some infectious diseases.

Identification and chemical study of plants used in the traditional treatment of Buruli Ulcer in Benin

Buruli ulcer (BU) is a skin disease caused by infection with Mycobacterium ulcerans. Currently, surgery associated or not with specific antibiotic therapy is the only proven effective treatment. However, it is presently only being carried out in a few medical centers with proper and adequate equipment for the management of BU [1]. Due to cultural and economic reasons in Benin, traditional treatment remains the first option for patients with generally low income resources [2]. In Benin, plants make up the main component of traditional treatment for BU. We recently carried out an ethnobotanical survey involving 17 traditional practitioners within the Ouinhi community in Zou department. We noted that 49 different plants are being used for the traditional treatment of BU and different parts of these plants are employed in various pharmaceutical forms for internal or external uses. The chemical study of these plants revealed the presence of alkaloids, tannins, flavonoids, saponins, quinone derivatives, essential oils, steroids and terpenoids. Many compounds of these characterized groups of chemicals known for their antibacterial properties. Extracts of 20 plants taken from the 49 identified were screened against Mycobacterium ulcerans using Resazurin Microtiter Assay (REMA) [3]. Holarrhena floribunda (G. Don) T. Durand and Schinz and Jatropha curcas Linn inhibited in vitro the growth of Mycobacterium ulcerans at concentrations of 125µg/ml and 250µg/ml respectively.

Conessine isolated from Holarrhena floribunda

The title compound, C24H40N2, has been isolated from Holarrhena floribunda G. Don. (Apocynaceae). The compound has a pentacyclic steroidal nucleus; the ring junctions share the same stereochemistry reported for this class of compounds. Of the three six-membered rings, rings A and C adopt a chair-like and ring B forms a half-chair-like conformation. The cyclopentane ring D shows a half-chair conformation and the methylpyrrolidine ring E adopts an envelope conformation. The dimethylamino substituent in ring A is equatorially oriented.

In vitro and in vivo evaluation of the antitrypanosomal activity of fractions of Holarrhena africana

The aqueous extract of young leaves of Holarrhena africana, a plant used in the Nigerian traditional medicine, exhibited good activity against Trypanosoma brucei spp. The extract was fractionated and eight fractions were obtained. One fraction designated as HaF 5 showed in vitro activity against Trypanosoma brucei rhodesiense with an IC 50 value of 0.785 μg/mg and no overt cytotoxicity against L-6 cells. Fraction HaF 5 was tested in vivo at two doses and found to exhibit in vivo efficacy in Trypanosoma brucei brucei infected mice leading to a complete disappearance of parasitaemia followed by a relapse.

Meliola simillima . [Descriptions of Fungi and Bacteria

Abstract A description is provided for Meliola simillima . Information is included on the disease caused by the organism that can cause reduced photosynthetic capability in severe infections. Some information is given on its transmission, geographical distribution (Africa (Ghana, Guinea, Sierra Leone, Togo), Asia (Bangladesh, China (Hainan), India (Uttar Pradesh), Indonesia, Myanmar, Philippines, Sri Lanka) and Caribbean (Bahamas, Dominican Republic, Jamaica)) and hosts ( Echites brownei, Echites sp., Hemidesmus indicus, Holarrhena africana [ Holarrhena floribunda ], Holarrhena antidysenterica [ Holarrhena pubescens ], Holarrhena wulfsbergii, Holarrhena sp., Rauwolfia [ Rauvolfia ] nitida, R. vomitoria, Wrightia javanica [ W. pubescens ], W. lanitii [ W. pubescens ], W. pubescens and W. tomentosa [ W. arborea ]).