Evaluation of the use of Cocos nucifera as antimalarial remedy in Malaysian folk medicine

Ethnopharmacological relevance

White flesh extract of Cocos nucifera (coconut) was studied to ascertain the ethnopharmacological standing of its antimalarial usage in Malaysian folk medicine.

Materials and methods

The crude methanol extract was investigated for phytochemical constituents and acute oral toxicity. Antimalarial activity of different extract doses of 50, 100, 200 and 400 mg/kg were investigated in vivo against Plasmodium berghei (NK65) infections in mice during early, established and residual infections. Chloroquine (20 mg/kg) and pyrimethamine (1.2 mg/kg) were used as reference drugs.

Results

The results revealed that the extract contained some phytochemical constituents and is toxicologically safe by oral administration. The extract significantly reduced the parasitaemia by the 200 and 400 mg/kg doses in the all three in vivo assessment assays. However, the extract did not significantly increase the survival time of the infected mice.

Conclusions

The observed pharmacological activities suggest that the Malaysian folkloric medicinal application of Cocos nucifera has a pharmacological basis.     

In vivo anti-tussive activity and structural features of a polysaccharide fraction from water extracted Withania somnifera

Aim of the study

Anti-tussive drugs are amongst the most widely used medications worldwide; however no new class of drugs has been introduced into the market for many years. The present study aims at evaluating the structural features and in vivo anti-tussive activity of a polysaccharide fraction from water extracted Withania somnifera.

Materials and methods

Herein, we have analyzed water extracted material of Withania somnifera using chemical, chromatographic, spectroscopic and biological methods.

Results

A polysaccharide fraction (F3) containing arabinosyl, galactosyl and galacturonosyl residues were obtained by anion exchange chromatography of the water extracted material. This polymer is branched and contained (1,5)-/(1,3,5)-linked arabinofuranosyl, (1,3)-/(1,6)-/(1,3,6)-linked galactopyranosyl residues together with small amount of terminal rhamnopyranosyl and terminal arabinofuranosyl residues. Peroral administration of this pectic arabinogalactan in a dose of 50 mg kg⁻¹ body weight (b.w.) decreased the number of cough efforts induced by citric acid in guinea pigs like that of codeine.

Conclusions

This study provides a scientific basis for the past and present ethnomedical uses of this plant.     

Anti-diabetic activity of Chiliadenus iphionoides

Ethnopharmacological relevance

Chiliadenus iphionoides (Boiss. & Blanche) Brullo (Asteraceae), a small aromatic shrub found throughout Israel, is used traditionally in the treatment of diabetes mellitus. In this study, Chiliadenus iphionoides anti-diabetic activity was characterized using cellular and animal models.

Materials and methods

Pancreatic β cells, adipocytes, and skeletal myotubes were treated with an ethanolic extract of Chiliadenus iphionoides to study the extract's effects on insulin secretion and glucose uptake. The sand rat (Psammomys obesus) was used to study Chiliadenus iphionoides acute and long term effects in vivo. An oral starch tolerance test was performed as well as a 30 day feeding study.

Results

Chiliadenus iphionoides extract increased insulin secretion in β cells as well as glucose uptake in adipocytes and skeletal myotubes. The extract also displayed hypoglycemic activity in the diabetic sand rat.

Conclusions

Chiliadenus iphionoides exhibits considerable anti-diabetic activity, although the mechanism of action remains to be determined.     

Wound repair and anti-inflammatory potential of essential oils from cones of Pinaceae: preclinical experimental research in animal models

Ethnopharmacological relevance

Ethnobotanical surveys revealed that Abies bornmulleriana, Abies cilicica, Abies nordmanniana and Cedrus libani have been used to promote wound healing in Turkish folk medicine. Four different fir species (Abies cilicica subsp. cilicica, Abies nordmanniana subsp. bornmulleriana, Abies nordmanniana subsp. equi-trojani, and Abies nordmanniana subsp. nordmanniana), Cedrus libani and Picea orientalis were assessed for their in vivo wound healing and anti-inflammatory activities.

Materials and methods

The essential oils from six different coniferous cones were used. In vivo wound healing activity of the plants was evaluated by linear incision and circular excision experimental wound models subsequently histopathological analysis. The healing potential was comparatively assessed with a reference ointment Madecassol^®, which contains 1% extract of Centella asiatica. Additionally acetic acid-induced capillary permeability test was used for the oils’ anti-inflammatory activity.

Results

The essential oils from Cedrus libani and Abies cilicica subsp. cilicica demonstrated the highest activities on the both wound models. Moreover, the oil from Abies nordmanniana subsp. bornmulleriana was found generally highly effective. On the other hand, the rest of the species did not show any remarkable wound healing effect. Results of the present study support the continued and expanded utilization of these plant species employed in Turkish folk medicine.

Conclusion

The experimental study revealed that Cedrus libani and Abies cilicica subsp. cilicica display remarkable wound healing and anti-inflammatory activities.     

Analgesic, anti-inflammatory and antipyretic activities of the petroleum ether fraction from the ethanol extract of Desmodium podocarpum

Ethnopharmacological relevance

Desmodium podocarpum is a plant that has been used in the folk medicine to treat febrile diseases, cough and bleeding wounds. However, there is no scientific basis or reports in the modern literature regarding its effectiveness as an analgesic, anti-inflammatory and antipyretic agent.

Aims of the study

The objective of this study is to evaluate the analgesic, anti-inflammatory and antipyretic activities of the petroleum ether fraction (PEF) from the ethanol extract of Desmodium podocarpum.

Materials and methods

PEF (50, 100, 200 mg/kg) was estimated for its pharmacological properties by using the acetic acid-induced writhing test, the hot plate test, the Carrageenan-induced rat paw edema model, the dimethylbenzene-induced mouse inflammation model, and the lipopolysaccharide (LPS)-induced rat fever model. In addition, the acute toxicity of PEF was also studied.

Results

PEF significantly and dose-dependently inhibited the writhing responses in mice, increased reaction time of mice in the hot plate test, reduced carrageenan-induced paw edema in rats and the dimethylbenzene-induced ear edema in mice, and attenuated LPS-induced fever in rats. No death of mice was observed when orally administered PEF up to 4.2 g/kg.

Conclusions

These findings suggest that PEF possesses evident analgesic, anti-inflammatory and antipyretic activities, and has a favorable safety, which supports the use of Desmodium podocarpum as an analgesic, anti-inflammatory and antipyretic drug in the folk medicine.     

Analgesic effects and anti-inflammatory properties of the crude methanolic extract of Schwenckia americana Linn (Solanaceae)

Aim of the study

To evaluate analgesic effect and anti-inflammatory properties of Schwenckia americana (Solanaceae), a medicinal plant used for treating rheumatic pains and swelling in North-western Nigeria.

Materials and methods

Three doses (25 mg/kg, 50 mg/kg and 100 mg/kg) of the crude methanolic extract of Schwenkia americana were evaluated for analgesic and anti-inflammatory activities using acetic acid induced writhing test, formalin induced nociception, and formalin induced hind paw oedema in rats.

Results

All doses (25, 50, 100 mg/kg) of the extract tested were effective. The extract at the tested doses produced a percentage inhibition of the acetic acid induced abdominal constriction of (53.3, 58.0 and 86.7%), respectively. A percentage inhibition of the formalin induced nociception of 44.00, 56.04, and 56.04% (early phase) and 33.00, 36.63 and 59.71% (late phase) was also produced. The inhibition of oedema formation increased with increasing dosage from 25 to 100 mg/kg. The crude extract produced a statistically significant analgesic and anti-inflammatory activity comparable to the effect of standard drug (10 mg/kg Piroxicam).

Conclusion

This study demonstrated the potential analgesic and anti-inflammatory properties of crude methanolic extract of Schwenkia americana thus justifying its traditional usage.     

Evaluation of an ethnopharmacologically selected Bhutanese medicinal plants for their major classes of phytochemicals and biological activities

Ethnopharmacological relevance

As many as 229 medicinal plants have been currently used in the Bhutanese Traditional Medicine (BTM) as a chief ingredient of polyherbal formulations and these plants have been individually indicated for treating various types of infections including malaria, tumor, and microbial. We have focused our study only on seven species of these plants.

Aim of the study

We aim to evaluate the antiplasmodial, antimicrobial, anti-Trypanosoma brucei rhodesiense and cytotoxicity activities of the seven medicinal plants of Bhutan selected using an ethno-directed bio-rational approach. This study creates a scientific basis for their use in the BTM and gives foundation for further phytochemical and biological evaluations which can result in the discovery of new drug lead compounds.

Materials and methods

A three stage process was conducted which consisted of: (1) an assessment of a pharmacopoeia and a formulary book of the BTM for their mode of plant uses; (2) selecting 25 anti-infective medicinal plants based on the five established criteria, collecting them, and screening for their major classes of phytochemicals using appropriate test protocols; and (3) finally analyzing the crude extracts of the seven medicinal plants, using the standard test protocols, for their antiplasmodial, antimicrobial, anti-Trypanosoma brucei rhodesiense and cytotoxicity activities as directed by the ethnopharmacological uses of each plant.

Results

Out of 25 medicinal plants screened for their major classes of phytochemicals, the majority contained tannins, alkaloids and flavonoids. Out of the seven plant species investigated for their biological activities, all seven of them exhibited mild antimicrobial properties, five plants gave significant in vitro antiplasmodial activities, two plants gave moderate anti-Trypanosoma brucei rhodesiense activity, and one plant showed mild cytotoxicity. Meconopsis simplicifolia showed the highest antiplasmodial activity with IC₅₀ values of 0.40 μg/ml against TM4/8.2 strain (a wild type chloroquine and antifolate sensitive strain) and 6.39 μg/ml against K1CB1 (multidrug resistant strain) strain. Significantly the extracts from this plant did not show any cytotoxicity.

Conclusions

These findings provide the scientific basis for the use of seven medicinal plants in the BTM for the treatment of malaria, microbial infections, infectious fevers, and the Trypanosoma brucei rhodesiense infection. The results also form a good preliminary basis for the prioritization of candidate plant species for further in-depth phytochemical and pharmacological investigations toward our quest to unearth lead antiparasitic, anticancer and antimicrobial compounds.     

An ethnomedicinal, phytochemical and pharmacological profile of Desmodium gangeticum (L.) DC. and Desmodium adscendens (Sw.) DC

Ethnopharmacological relevance

Desmodium gangeticum (L.) DC. and Desmodium adscendens (Sw.) DC. are two important and well explored species of genus Desmodium (Fabaceae (alt. Leguminosae) subfamily: Faboideae). Desmodium gangeticum is used as a tonic, febrifuge, digestive, anticatarrhal, antiemitic, in inflammatory conditions of chest and in various other inflammatory conditions in the Ayurvedic System of Medicine while Desmodium adscendens is widely used for the treatment of asthma in Ghana, Africa.

Aim of the review

The aim of this review is to provide comprehensive information on the botany, traditional uses, phytochemistry, pharmacological research and toxicology of Desmodium gangeticum and Desmodium adscendens to explore their therapeutic potential and future research opportunities.

Materials and methods

All the available information on Desmodium gangeticum and Desmodium adscendens was collected via electronic search (using Pubmed, SciFinder, Scirus, Google Scholar, JCCC@INSTIRC and Web of Science) and a library search for articles published in peer-reviewed journals.

Results

About 25 different species of Desmodium including Desmodium gangeticum and Desmodium adscendens are used ethnomedicinally all over the world. Phytochemical research on Desmodium gangeticum and Desmodium adscendens has led to the isolation of alkaloids, pterocarpans, phospholipids, sterols, flavones and flavonoid glycosides from Desmodium gangeticum and triterpenoid saponins, phenylethylamines and indole-3-alkyl amines from Desmodium adscendens. Crude extracts, fractions and isolated components of Desmodium gangeticum and Desmodium adscendens showed a wide spectrum of in vitro and in vivo pharmacological activities like antileishmanial, immunomodulatory, antiasthmatic, smooth muscle relaxant, anti-inflammatory, anti-ulcer, cardio-protective, antidiabetic, antiamnesic, antiviral, antioxidant and hepatoprotective activities.

Conclusions

Desmodium gangeticum and Desmodium adscendens have emerged as a good source of traditional medicine. Desmodium gangeticum possesses the ability to scavenge the free radicals generated during ischaemia and ischaemia reperfusion thereby preserving the mitochondrial respiratory enzymes that eventually lead to cardio-protection and has potential prophylactic and therapeutic efficacy against Leishmania infection. Desmodium adscendens is useful against chronic bronchitis and asthma. However, there is a need to search for individual secondary metabolites responsible for these actions and study their mode of actions, bioavailability, pharmacokinetics and physiological pathways in sufficient detail. The promising results should be further substantiated by clinical trials.     

Procyanidin-rich fractions from Parkia biglobosa (Mimosaceae) leaves cause redox-sensitive endothelium-dependent relaxation involving NO and EDHF in porcine coronary artery

Aim of the study

Parkia biglobosa leaves are traditionally used as an antihypertensive agent in Benin. The present study assessed the vasorelaxant activity of different Parkia biglobosa leaf extracts using isolated porcine coronary artery rings.

Materials and methods

A hydroalcoholic leaf extract was submitted to a multi-step liquid-liquid fractionation with solvents of increasing polarity and the polyphenolic content of the different fractions was analyzed. Vascular reactivity of the different extracts was assessed using porcine coronary artery rings, in the presence or absence of specific pharmacological inhibitors.

Results

The hydroalcoholic, ethyl acetate and butanolic extracts contained mainly procyanidins and monomeric flavonoids. Parkia biglobosa leaf crude extract induced a redox-sensitive endothelium-dependent relaxation mediated by both nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF). The fractionation of the butanolic extract generated 6 fractions, two of which induced stronger vasorelaxation than the original extract and they had a higher phenolic content.

Conclusions

Parkia biglobosa leaf extract is able to induce endothelium-dependent NO- and EDHF-mediated relaxation in porcine coronary artery rings. The vasorelaxant activity is dependent on their phenolic content and appears to involve mainly procyanidins.     

In vitro and in vivo antioxidant effects of the ethanolic extract of Swertia chirayita

Ethnopharmacological relevance

Swertia chirayita, a medicinal herb endemic to the Tibetan region, is used as a special remedy for liver disorders. The hepatoprotective activity of its plant extracts has been associated with its antioxidant activity. This paper aims to investigate the in vitro and in vivo antioxidant effects of Swertia chirayita extracts (SCE).

Materials and methods

Antioxidant ability of Swertia chirayita was investigated by employing several established in vitro methods. In vivo antioxidant activity was tested against CCl₄-induced toxicity in mice. The levels and activities of malondialdehyde (MDA) and antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH), were then assayed using standard procedures.

Results

SCE exhibited strong antioxidant ability in vitro. The liver and kidney of CCl₄-intoxicated animals exhibited a significant (p < 0.001) decrease in SOD, CAT, and GSH levels. Additionally, these organs exhibited a significant (p < 0.001) increase in MDA level. CCl₄ did not exhibit toxicity on mice treated with SCE and Vitamin E. The effects of Swertia chirayita (three dosages) were comparable to those of Vitamin E, except in MDA level in the liver and GSH level in the kidney (p < 0.05).

Conclusion

This study suggests that the ethanolic extract of Swertia chirayita possesses in vitro and in vivo antioxidant effects. This supports the traditional use of Swertia chirayita in Tibetan medicine to cure liver diseases.     

Gastric antisecretory and antiulcer activities of Cedrus deodara (Roxb.) Loud. in Wistar rats

Ethnopharmacological relevance: Cedrus deodara (Roxb.) Loud. is used in Ayurvedic medicine to treat peptic ulcer.

Aim of the study

To evaluate the gastric antisecretory and antiulcer activity of Cedrus deodara.

Materials and methods

The volatile oil extracted by steam distillation of Cedrus deodara wood was examined for its gastric antisecretory and antiulcer effect in the pylorus-ligated rat model and ethanol induced gastric lesions in rats.

Results

The volatile oil showed significant antisecretory activity as evidenced by decreased gastric fluid volume, total acidity, free acidity and increase in the pH of the gastric fluid in pylorus-ligated rats. Our studies also revealed that pretreatment with Cedrus deodara significantly reduced the number of ulcer, ulcer score and ulcer index in pylorus-ligated and ethanol treated rats. The antiulcer activity of Cedrus deodara is further supported by histopathological study which showed protection of mucosal layer from ulceration and inflammation.

Conclusion

The present findings conclude that volatile oil of Cedrus deodara wood has potent antisecretory and antiulcer effects and justify the traditional usage of this herb to treat peptic ulcers.     

Saponin rich fractions from Polygonatum odoratum (Mill.) Druce with more potential hypoglycemic effects

Ethnopharmacological relevance

Peppers from Capsicum species (Solanaceae) are native to Central and South America, and are commonly used as food and also for a broad variety of medicinal applications.

Aim of the study

The red pepper Capsicum baccatum var. pendulum is widely consumed in Brazil, but there are few reports in the literature of studies on its chemical composition and biological properties. In this study the antioxidant and anti-inflammatory activities of Capsicum baccatum were evaluated and the total phenolic compounds and flavonoid contents were determined.

Materials and methods

The antioxidant property was assayed by scavenging abilities using DPPH and the anti-inflammatory activity was tested through the carrageenan-induced pleurisy model in mice. The total phenolic compounds and flavonoid contents were determined spectrophotometrically.

Results

The ethanolic and butanol extracts (200 mg/kg, p.o.) presented a significant anti-inflammatory activity toward carrageenan-induced pleurisy model in mice in comparison to dexamethasone (0.5 mg/kg, s.c.). Among the parameters evaluated, the treatment with these samples inhibited leukocyte migration and reduced the formation of exudate. The contents of flavonoids and total phenolic compounds could be correlated with the antioxidant and anti-inflammatory activities observed for Capsicum baccatum.

Conclusions

Our findings suggest that Capsicum baccatum contains potential antioxidant and anti-inflammatory compounds which could be tested as drug candidates against oxidative and inflammation-related pathological processes in medicinal chemistry studies.     

Antihypertensive and neuroprotective activities of rhynchophylline: The role of rhynchophylline in neurotransmission and ion channel activity

Ethnopharmacological relevance

Uncaria species (Gouteng in Chinese) have been used as ethnopharmacological medicines to treat ailments of the cardiovascular and central nervous systems. As the main alkaloid constituent of Uncaria species, rhynchophylline has drawn extensive attention in recent years for its antihypertensive and neuroprotective activities, and its pharmacological effects are related to ethnopharmacological medicine properties of Uncaria species.

Aim of the review

This review examined the pharmacological studies and mechanisms of rhynchophylline, with an emphasis on cardiovascular and central nervous system diseases linked to the ethnopharmacological uses of Uncaria species.

Methods

We conducted both an electronic search and a library search of in vivo and in vitro studies. The terms and keywords for the search included rhynchophylline, Uncaria species, Gouteng, pharmacological effects, and mechanism. We focused on the papers, including ours, with studies on all related pharmacological effects and mechanisms of rhynchophylline.

Results

Rhynchophylline was the main constituent of several components identified from Uncaria species. Rhynchophylline mainly acts on cardiovascular and central nervous system diseases, including hypertension, bradycardia, arrhythmia, sedation, vascular dementia, epileptic seizures, drug addiction, and cerebral ischemia. Rhynchophylline also has effects on anticoagulation, inhibits vascular smooth muscle cell proliferation, and has been shown to be anti-endotoxemic. The active mechanisms are related to modulation of calcium and potassium ion channels, protection of neural and neuroglial cells, and regulation of central neurotransmitter transport and metabolism. More studies are necessary to verify the pharmacological activities and determine the exact mechanisms of rhynchophylline activity.

Conclusions

Rhynchophylline treatment of cardiovascular and central nervous system diseases has a strong linkage with traditional concepts and uses of Uncaria species in ethnopharmacological medicine, such as treatment for lightheadedness, convulsions, numbness, and hypertension. As a candidate drug for several cardiovascular and central nervous system diseases, rhynchophylline will attract scientists to pursue the potential pharmacological effects and mechanisms with new technologies. Relatively few clinically relevant studies of rhynchophylline have been conducted. Thus, more in vivo validations and investigations of antihypertensive and neuroprotective mechanisms of rhynchophylline are necessary.     

Genotoxicity of polar and apolar extracts obtained from Qualea multiflora and Qualea grandiflora

Ethnopharmacological relevance

The species Qualea grandiflora and Qualea multiflora, which belong to the Vochysiaceae family, are common in the Brazilian savannah (Cerrado biome), and the local inhabitants use these species to treat external ulcers and gastric diseases and as an anti-inflammatory agent. Studies have demonstrated that these plants contain compounds that exhibit pharmacological activities; however, the risks associated with their consumption are not known.

Material and methods

In the present study, the mutagenicity of polar and apolar extracts from Qualea grandiflora and Qualea multiflora were assessed by employing the Ames assay with and without metabolic activation. Additionally, phytochemical analyses (HPLC-ESI-IT-MS, HPLC-UV-PDA and GC-IT-MS) were performed to identify the chemical constituents present in these species, including the evaluation of physico-chemical properties, such as polarity or apolarity of the organic compounds, which are related to each fraction obtained. These studies provide important information regarding the biochemical behaviour of these compounds.

Results

All extracts exhibited mutagenicity, inducing frameshift mutations and base substitutions in DNA. Phytochemical analysis identified terpenes, ellagic acid derivatives and phytosteroids.

Conclusions

The mutagenicity observed might be due to the presence of pentacyclic triterpenes and polyphenols, which are able to generate reactive oxygen species (ROS) and result in the potential to cause DNA damage. The genetic risk identified in this present work shows that special attention should be considered for the use of compounds obtained from these plant species in medicinal treatments. Further studies must be conducted to identify safe therapeutic doses.     

Chemical composition, antinociceptive and anti-inflammatory effects in rodents of the essential oil of Peperomia serpens (Sw.) Loud

Ethnopharmacological relevance

Peperomia serpens (Piperaceae), popularly known as “carrapatinho”, is an epiphyte herbaceous liana grown wild on different host trees in the Amazon rainforest. Its leaves are largely used in Brazilian folk medicine to treat inflammation, pain and asthma.

Aim of the study

This study investigated the effects of essential oil of Peperomia serpens (EOPs) in standard rodent models of pain and inflammation.

Materials and methods

The antinociceptive activity was evaluated using chemical (acetic acid and formalin) and thermal (hot plate) models of nociception in mice whereas the anti-inflammatory activity was evaluated by carrageenan- and dextran-induced paw edema tests in rats croton oil-induced ear edema, as well as cell migration, rolling and adhesion induced by carrageenan in mice. Additionally, phytochemical analysis of the EOPs has been also performed.

Results

Chemical composition of the EOPs was analyzed by gas chromatography and mass spectrometry (GC/MS). Twenty-four compounds, representing 89.6% of total oil, were identified. (E)-Nerolidol (38.0%), ledol (27.1%), α-humulene (11.5%), (E)-caryophyllene (4.0%) and α-eudesmol (2.7%) were found to be the major constituents of the oil. Oral pretreatment with EOPs (62.5-500 mg/kg) significantly reduced the writhing number evoked by acetic acid injection, with an ED₅₀ value of 188.8 mg/kg that was used thereafter in all tests. EOPs had no significant effect on hot plate test but reduced the licking time in both phases of the formalin test, an effect that was not significantly altered by naloxone (0.4 mg/kg, s.c.). EOPs inhibited the edema formation induced by carrageenan and dextran in rats. In mice, EOPs inhibited the edema formation by croton oil as well as the leukocyte and neutrophil migration, the rolling and the adhesion of leukocytes.

Conclusions

These data show for the first time that EOPs has a significant and peripheral antinociceptive effect that seems unrelated to interaction with the opioid system. EOPs also displays a significant anti-inflammatory effect in acute inflammation models. This effect seems to be related to components which inhibit the production of several inflammatory mediators. These results support the widespread use of Peperomia serpens in popular medicine to treat inflammation and pain.     

In vitro modulatory effects of Andrographis paniculata, Centella asiatica and Orthosiphon stamineus on cytochrome P450 2C19 (CYP2C19)

Ethno pharmacological relevance

Andrographis paniculata (AP), Centella asiatica (CA) and Orthosiphon stamineus (OS) are three popular herbs traditionally used worldwide. AP is known for the treatment of infections and diabetes and CA is good for wound healing and healthy skin while OS is usually consumed as tea to treat kidney and urinary disorders. Interaction of these herbs with human cytochrome P450 2C19 (CYP2C19), a major hepatic CYP isoform involved in metabolism of many clinical drugs has not been investigated to date.

Aim of the study

In this study, the modulatory effects of various extracts and major active constituents of AP, CA and OS on CYP2C19 activities were evaluated.

Materials and methods

S-Mephenytoin, the CYP2C19 substrate probe, was incubated in the presence or absence of AP, CA and OS components. The changes in the rate of metabolite (hydroxymephenytoin) formation were subsequently determined by a high-performance liquid chromatography (HPLC)-based enzyme assay to characterize the modulatory effects.

Results

Among the herbal extracts studied, AP ethanol extract and CA dichloromethane extract exhibited mixed type inhibition towards CYP2C19 with K_i values of 67.1 and 16.4 μg/ml respectively; CA ethanol extract and OS petroleum ether extract competitively inhibited CYP2C19 activity (K_i = 39.6 and 41.5 μg/ml respectively). Eupatorin (a major active constituent of OS) was found to significantly inhibit CYP2C19 by mixed type inhibition (K_i = 7.1 μg/ml or 20.6 μM).

Conclusions

It was observed that AP, CA and OS inhibited CYP2C19 activity with varying potency. While weak inhibitory effect was observed with AP, moderate to strong inhibition was observed with CA dichloromethane extract and eupatorin, the major OS constituent. Therefore care should be taken when these CA and OS components are co-administered with CYP2C19 substrates (such as omeprazole, proguanil, barbiturates, citalopram, and diazepam).     

Antiplasmodial and cytotoxic activities of medicinal plants traditionally used in the village of Kiohima, Uganda

Aim of the study

In Uganda, malaria is the most common disease and Ugandan people largely rely on traditional medicine. In this context, we carried out an ethnobotanical study on the Kiohima village, located close to the Kibale National Park in South-Western Uganda and investigated in vitro the antiplasmodial and cytotoxic activities of selected medicinal plants.

Materials and methods

Seventy-five plants-using adults (men and women) were interviewed to find out their plant use. From these information, 48 plants used in traditional medicine were identified and according to their reported uses and to bibliographic data, several parts of 28 plants (leaves, barks, roots), were selected and collected for biological evaluations. These samples were dried, extracted with ethyl acetate and the crude extracts were assayed for in vitro antiplasmodial and cytotoxic activities at 10 μg/mL.

Results

One third of the screened plants showed a significant antiplasmodial activity with inhibition greater than 50% at 10 μg/mL.

Conclusion

These results may indicate a possible explanation of the use of some medicinal plant against malaria in the village of Kiohima and have also allowed to highlight a plant with potent antimalarial activity: Citropsis articulata root barks.     

Antihypertensive effect of total flavone extracts from Puerariae Radix

Aim of the study

To evaluate the antihypertensive effect of total flavone extracts from Puerariae Radix (FEPR). To explore the hemodynamic profiles and pertinent mechanism of the extracts.

Materials and methods

Acute and chronic antihypertensive effects of FEPR were examined in spontaneous hypertensive rats (SHRs) and reno-hypertensive rats (two kidneys one clip model, 2K1C). Anesthetized dogs were used to evaluate the hemodynamic effects of FEPR. The determination of angiotensin converting enzyme (ACE) activity in vitro and plasma renin activity (PRA) and endothelin (ET) in vivo were used to study the pilot mechanism of FEPR. Moreover, the toxicity study of FEPR was evaluated.

Results

FEPR (100, 200 and 400 mg/kg, i.v.) notably reduced the blood pressure of SHRs in a short time period. A two-week administration of FEPR (45, 90 and 180 mg/kg, p.o.) decreased the blood pressure of both 2K1C rats and SHRs. The results of hemodynamic study in anesthetized dogs showed that, left ventricular end systolic pressure and left ventricular dP/dt_max had shown no significant difference between FEPR-treated dogs and those from the control group, while the cerebral blood flow increased significantly in FEPR-treated groups. FEPR significantly inhibited the ACE activities in vitro dose dependently, and inhibited the PRA in vivo, while the content of ET showed no difference in the FEPR treated group comparing with the control group.

Conclusions

FEPR shows significantly blood pressure lowering and cerebral vascular resistance (CVR) decreasing effect, which can partly be explained by the involvement of the Renin-Angiotensin-System (RAS).     

Anti-inflammatory and antinociceptive effects of the stem bark of Byrsonima intermedia A. Juss

Ethnopharmacological relevance

Byrsonima intermedia A. Juss. is popularly known as “murici pequeno” and is native to the Brazilian Cerrado. This species has been used as an antimicrobial, anti-hemorrhagic, anti-diarrheal and anti-inflammatory. Nevertheless, scientific information regarding Byrsonima intermedia is limited; there are no reports related to its possible anti inflammatory and antinociceptive effects. This study employed in vivo inflammatory and nociceptive models to evaluate the scientific basis for the traditional use of Byrsonima intermedia.

Materials and methods

Carrageenan-induced paw edema, peritonitis and fibrovascular tissue growth induced by s.c. cotton pellet implantation tests were used to investigate the anti-inflammatory activity of Byrsonima intermedia aqueous extract (BiAE) in rats. Mechanical nociceptive paw, formalin and hot plate tests were used to evaluate the antinociceptive activity in mice. High-performance liquid chromatography (HPLC), phytochemistry screening and determination of total phenolics and flavonoids were used to determine the chemical profile of the BiAE.

Results

BiAE at test doses of 30-300 mg/kg p.o. clearly demonstrated anti-inflammatory effects by reduced carrageenan-induced paw edema, by inhibited leukocyte recruitment into the peritoneal cavity and, in the model of chronic inflammation, by using the cotton pellet-induced fibrovascular tissue growth in rats. The extracts at test doses of 30-300 mg/kg p.o. clearly demonstrated antinociceptive activity in all tests. Administration of the opioid receptor antagonist naloxone completely inhibited the antinociceptive effect induced by BiAE (100 mg/kg).

Conclusion

BiAE markedly exhibits anti-inflammatory action in rats and antinociceptive activity in mice. Thus, it may be useful in the treatment of inflammatory hyperalgesic disorders, which supports previous claims of its traditional use.     

The in vivo expectorant and antitussive activity of extract and fractions from Reineckia carnea

Aim of study

To evaluate the potential expectorant and antitussive activity of a traditional Chinese medicine.

Materials and methods

The water extract and four fractions of the aerial part of Reineckia carnea were orally administrated to coughing mice induced by ammonium hydroxide and mice injected with phenol red, respectively, to investigate their medification effect on coughing and mucus scretion.

Results and discussion

90% Ethanol fraction significantly lengthened the latent period of cough and decreased cough frequency caused by ammonium hydroxide at the dose of 0.372 g/kg (p < 0.05). Sixty percent ethanol fraction reduced the cough frequency as well as the mucus secretion from mouse tracheas obviously at the dose of 0.570 g/kg (p < 0.05) by measuring the tracheal output of phenol red in mice. The medication effects in multiple doses of the active fractions were then performed and it has been proved that the 60% ethanol and 90% ethanol fraction were curatively effective on expectoration and coughing, respectively both at the high and middle dose, which supplied proofs for the further research on chemical constituents in both of two effective fractions.