Antidiarrheal and antioxidant activities of chamomile (Matricaria recutita L.) decoction extract in rats

Ethnopharmacological relevance

Matricaria recutita L. (Chamomile) has been widely used in the Tunisian traditional medicine for the treatment of digestive system disorders. The present work aims to investigate the protective effects of chamomile decoction extract (CDE) against castor oil-induced diarrhea and oxidative stress in rats.

Methods

The antidiarrheal activity was evaluated using castor oil-induced diarrhea method. In this respect, rats were divided into six groups: Control, Castor oil, Castor oil+Loperamide (LOP) and Castor oil+various doses of CDE. Animals were per orally (p.o.) pre-treated with CDE during 1 h and intoxicated for 2 or 4 h by acute oral administration of castor oil.

Results

Our results showed that CDE produced a significant dose-dependent protection against castor oil-induced diarrhea and intestinal fluid accumulation. On the other hand, we showed that diarrhea was accompagned by an oxidative stress status assessed by an increase of malondialdehyde (MDA) level and depletion of antioxidant enzyme activities as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx). Castor oil also increased gastric and intestinal mucosa hydrogen peroxide (H₂O₂) and free iron levels. Importantly, we showed that chamomile pre-treatment abrogated all these biochemical alterations.

Conclusion

These findings suggested that chamomile extract had a potent antidiarrheal and antioxidant properties in rats confirming their use in traditional medicine.     

Cytotoxicity and inhibition of P-glycoprotein by selected medicinal plants from Thailand

Ethnopharmacological relevance

Thai medicine has a long tradition of tonifying medicinal plants. In the present investigation, we studied the flower extracts of Jasminum sambac, Mammea siamensis, Mesua ferrea, Michelia alba, Mimusops elengi, and Nelumbo nucifera and speculated that these plants might influence metabolism and substance flow in the body.

Materials and methods

Isolation of porcine brain capillary endothelial cells (PBCECs) as well as multidrug-resistance CEM/ADR5000 leukemia cells, MDA-M;B-231 breast cancer, U-251 brain tumor, and HCT-116 colon cancer cells were used. The calcein-acetoxymethylester (AM) assay was used to measure inhibition of P-glycoprotein transport. XTT and resazurin assays served for measuring cytotoxicity.

Results

The extracts revealed cytotoxicity towards CCRF-CEM leukemia cells to a different extent. The strongest growth inhibition was found for the n-hexane extracts of Mammea siamensis and Mesua ferrea, and the dichloromethane extracts of Mesua ferrea and Michelia alba. The flower extracts also inhibited P-glycoprotein function in porcine brain capillary endothelial cells and CEM/ADR5000 leukemia cells, indicating modulation of the blood–brain barrier and multidrug resistance of tumors. Bioactivity-guided isolation of coumarins from Mammea siamensis flowers revealed considerable cytotoxicity of mammea A/AA, deacetylmammea E/BA and deacetylmammea E/BB towards human MDA-MB-231 breast cancer, U-251 brain tumor, HCT-116 colon cancer, and CCRF-CEM leukemia cells.

Conclusion

The plants analyzed may be valuable in developing novel treatment strategies to overcome the blood–brain barrier and multidrug-resistance in tumor cells mediated by P-glycoprotein.     

The anti-inflammatory activities of an extract and compounds isolated from Platycladus orientalis (Linnaeus) Franco in vitro and ex vivo

Ethnopharmacological relevance

As a Chinese traditional herbal medicine, leaves of Platycladus orientalis (Linnaeus) Franco (LPO) are used to treat coughs, excessive mucus secretion, chronic bronchitis, bronchiectasis, and asthma, etc. The experiments were carried out to investigate their anti-inflammatory properties and mechanisms, which could support the Chinese traditional uses of treating inflammatory airway diseases.

Materials and methods

The anti-inflammatory activities of the chloroform fraction (CHL) and pure compounds of LPO were evaluated for their abilities to inhibit pro-inflammatory enzymes in vitro, and production of tumor necrosis factor-α (TNF-α) and nitric oxide in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Furthermore, the arachidonic acid metabolites, stimulated by calcium ionophore A23187, were also determined by HPLC.

Results

For the first time, the assays of eicosanoids in intact cells showed that the CHL, hinokiol, and acacetin had significant inhibitory effects on 5-hydroxy-eicosa-tetra-enoic acid (5-HETE) and leukotriene B₄ (LTB4) formations. And cell-free enzyme assays (5-lipoxygenase, leukotriene A₄-hydrolase, cyclooxgenase-2) demonstrated the potent inhibitory effects of the CHL, hinokiol and acacetin on 5-lipoxygenase (5-LOX). Then, the inhibitions of the CHL, hinokiol on NO biosynthesis and the inhibitions of the CHL, 8(14),15-pimaradien-3β,18-diol, and hinokiol on TNF-α release were also confirmed in the RAW264.7 murine macrophages.

Conclusion

The data indicate that the inhibitory effects of the CHL and its components (hinokiol and acacetin) on 5-LOX contribute to the anti-inflammatory activity of LPO. Moreover, the CHL and its components also show beneficial effects on NO and TNF-α production. Consequently, these results provide a rationale for LPO's traditional applications in the treatment of inflammatory airway diseases.     

Chemopreventive action of Lygodium flexuosum extract in human hepatoma PLC/PRF/5 and Hep 3B cells

Ethnopharmacological relevance

Lygodium flexuosum (Lygodiaceae), a medicinal fern used in Indian traditional medicine against liver disorders.

Aim of the study

The rationale of the study was to examine whether the n-hexane extract from plant Lygodium flexuosum affects apoptosis on human hepatoma PLC/PRF/5 and Hep 3B cells.

Materials and methods

Chemopreventive activity of the Lygodium flexuosum extract was determined by MTT assay, annexin-V FITC binding to phosphatidyl serine and cleavage of PARP. Subdiploid condition of cells treated with Lygodium flexuosum was analyzed by flow cytometry. Further, used transiently transfected NF-κB reporter in PLC/PRF/5 cells to evaluate the inhibitive effect of Lygodium flexuosum extract.

Results

Lygodium flexuosum extract inhibited the cell viability and induced apoptosis in hepatoma cells in a concentration dependent manner as evidenced by apoptotic changes such as flipping of phosphatidyl serine, cleavage of PARP. Cell cycle analysis showed the subG1 apoptotic population in cells treated with higher concentrations of the extract. When activated with exogenous TNF-α in transfected hepatoma cells it was observed that NF-κB dependent gene expression was inhibited by treatment with Lygodium flexuosum extract in PLC/PRF/5 cells dose-dependently.

Conclusions

This investigation suggests that the Lygodium flexuosum extract has antiproliferative and apoptotic activity in both cancer cells and has inhibitive role in TNF-α induced NF-κB activation in PLC/PRF/5 cells confirms the potential of the extract as a chemopreventive agent.     

Aegiceras corniculatum extract suppresses initial and late phases of inflammation in rat paw and attenuates the production of eicosanoids in rat neutrophils and human platelets

Aim of the study

The present study is designed to explore the anti-inflammatory potential of Aegiceras corniculatum Linn. Blanco stems extracts and their mechanism of action against various pro-inflammatory mediators and to validate its traditional use against inflammatory diseases.

Materials and methods

Rat paw edema and peritonitis models were employed for in vivo studies. For in vitro studies human platelets and rat neutrophils were stimulated with Ca²⁺-ionophore A23187 leading to the production of various pro-inflammatory metabolites, i.e., 12-HTT, 12-HETE and LTB₄ and 5-HETE which were quantified by HPLC.

Results

The highly polar methanol extract (100 mg/kg) caused ∼90% reduction in the carrageenan- and prostaglandin E2-induced paw edema in rats. It also caused the inhibition of cycloxygenase-1 metabolite, 12-HHT (IC₅₀ 41.1 ± 1.5 μg/ml) with a concomitant rise in 12-lipoxygenase metabolite, 12-HETE in A23187 stimulated human platelets. Conversely, the non-polar hexane extract attenuated (IC₅₀ 0.36 ± 0.12 μg/ml) 12-HETE formation with a parallel rise in 12-HHT, thereby displaying a selectivity towards 12-lipoxygenase. Non-polar hexane extract also antagonized the production of 5-lipoxygenase metabolites, i.e., leukotriene B₄ and 5-HETE in the rat neutrophils. Furthermore, ethyl acetate extract inhibited both COX and 5-LOX with a marked decline in the production of 12-HHT (IC₅₀ 0.08 ± 0.002 μg/ml) and LTB₄ (IC₅₀ 0.86 ± 0.03 μg/ml), respectively. The anti-inflammatory effect of hexane and ethyl acetate extracts was also reflected by the diminution of carrageenan-induced cell infiltration in rat peritoneum. Additionally, plant extracts caused ∼60% suppression in dextran-induced paw edema implying that they also ameliorate histamine and serotonin release.

Conclusion

Hexane, ethyl acetate and methanol extracts derived from Aegiceras corniculatum possess significant anti-inflammatory activity via multiple mechanisms and validate their traditional use against inflammation-related diseases.     

Cordyceps militaris extract stimulates Cl(-) secretion across human bronchial epithelia by both Ca(2+)(-) and cAMP-dependent pathways

Ethnopharmacological relevance

The caterpillar fungus Cordyceps militaris (CM; Clavicipitaceae) is a well-known traditional Chinese medicine that can be artificially cultivated on a large scale. We have previously demonstrated that its stimulatory action on ion transport in human airway epithelia is similar to Cordyceps sinensis (Clavicipitaceae), which has been traditionally used to treat respiratory diseases.

Aim of the study

To investigate the signal transduction mechanism(s) underlying CM-induced ion transport activity in cultured human bronchial epithelia.

Materials and methods

16HBE14o-, a human bronchial epithelial cell line, was used to study the regulation of ion transport by the water extract of CM. CM extract was added to the apical or basolateral aspect of the epithelia. In subsequent experiments, different Cl⁻ channel and K⁺ channel blockers, adenylate cyclase and protein kinase A (PKA) inhibitors, and an intracellular Ca²⁺ chelator were used to examine the involvement of apical Cl⁻ and basolateral K⁺ channels in mediating CM-induced Cl⁻ secretion and the underlying signal transduction mechanism(s). PKA activity was also measured in 16HBE14o- cells.

Results

CM stimulated Cl⁻ secretion across 16HBE14o- monolayers in a dose-dependent manner. Cl⁻ secretion could be inhibited by apical application of the cystic fibrosis transmembrane conductance regulator (CFTR) Cl⁻channel blocker and the calcium-activated Cl⁻ channel (CaCC) blocker. Cl⁻ secretion was sensitive to basolateral application of different K⁺ channel blockers. Similar inhibitory patterns were obtained in nystatin-permeabilized epithelia. The CM-induced Cl⁻ secretion could be inhibited by adenylate cyclase and PKA inhibitors as well as an intracellular Ca²⁺ chelator. Data from the PKA assay suggested that CM extract caused a significant increase in PKA activity compared with untreated control epithelia.

Conclusions

These results suggest that CM extract stimulated Cl⁻ secretion across human bronchial epithelia, possibly via apical CFTR and CaCC, and the basolateral K⁺ channels are involved in driving apical Cl⁻ exit. The underlying signal transduction mechanisms involve both cAMP- and Ca²⁺-dependent pathways.     

A fraction of stem bark extract of Entada africana suppresses lipopolysaccharide-induced inflammation in RAW 264.7 cells

Ethnopharmacological relevance

Entada africana is a plant used in African traditional medicine for the treatment of stomachache, fever, liver related diseases, wound healing, cataract and dysentery.

Aims of the study

This study aimed at evaluating the anti-inflammatory activity of fractions of the stem bark extract of the plant using lipopolysaccharide (LPS)-induced inflammation in RAW 264.7 macrophages model.

Materials and methods

The crude extract was prepared using the mixture CH₂Cl₂/MeOH (1:1, v/v) and fractionated by flash chromatography using solvents of increasing polarity to obtain five different fractions. The effects of the fractions on the cells viability were studied by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and their inhibitory activity against LPS-induced nitric oxide (NO) production screened by Griess test. The most active fraction was further investigated for its effects on reactive oxygen species (ROS) production using flux cytometry, the expression of inducible nitric oxide synthase (iNOS), pro-and anti-inflammatory cytokines (IL1β, TNFα, IL6, IL10 and IL13) by RT-PCR, and the activity of the enzyme p38 MAPK kinase by enzyme-linked immunosorbent assay (ELISA).

Results

The fractions presented no significant effect on the viability of macrophages at 100 μg/ml after 24 h incubation. The CH₂Cl₂/MeOH 5% (Ea5) fraction was found to be the most potent in inhibiting NO production with a half inhibition concentration (IC₅₀)=18.36 μg/ml, and showed the highest inhibition percentage (89.068%) in comparison with Baicalin (63.34%), an external standard at 50 μg/ml. Ea5, as well as Baicalin significantly (P<0.05) inhibited the expression of TNFα, IL6 and IL1β mRNA, attenuated mRNA expression of inducible NO synthase in a concentration-dependent manner, stimulated the expression of anti-inflammatory cytokines (IL10 and IL13), and showed a 30% inhibition of the activity of p38 MAPK kinase.

Conclusion

The results of the present study indicate that the fraction Ea5 of Entada africana possesses most potent in vitro anti-inflammatory activity and may contain compounds useful as a therapeutic agent in the treatment of inflammatory related diseases cause by over-activation of macrophages.     

Dragon's Blood extract has antithrombotic properties, affecting platelet aggregation functions and anticoagulation activities

Ethnopharmacological relevance

Dragon's Blood from Dracaena cochinchinensis (Lour.) S.C. Chen (Yunnan, China), as a traditional Chinese medicinal herb, was shown to have certain antithrombotic effects. A new preparation process was used to extract effective components from Dragon's Blood. A 95% ethanol extract A (EA) and a precipitate B (PB) fraction were obtained and compared. Reliability of the preparation process was validated by pharmacodynamic experiments.

Materials and methods

A rat/mouse thrombosis and blood stasis model was developed for this study, and EA and PB effects on thrombosis, platelet functions and blood coagulation activities were analyzed.

Results

It was observed that the EA fraction had significantly better inhibitory effects than the PB fraction on thrombosis (p < 0.05), platelet aggregation function (p < 0.01) and anticoagulation activity (p < 0.05-0.01).

Conclusions

The results obtained here showed that EA fraction from Dragon's Blood contained pharmacologically effective compounds with antithrombotic effects, partially improving platelet function and anticoagulation activity.     

Traditionally used Thai medicinal plants: In vitro anti-inflammatory,anticancer and antioxidant activities

Aims of the study

In order to assess traditional Thai claims about the therapeutic potential of medicinal plants and to select plants for future phytochemical research, nine plant species with anti-inflammatory uses were selected from Thai textbooks and assessed for their in vitro anti-inflammatory, antiproliferative and antioxidant activities.

Methods

Nuclear factor-kappaB (NF-κB) inhibitory effects in stably transfected HeLa cells were determined by luciferase assay, and effects on LPS-induced pro-inflammatory mediators prostaglandin E2 (PGE2), interleukin (IL)-6, IL-1β, and tumour necrosis factor (TNF)α in primary monocytes were assessed by ELISA. Cytotoxic activities were examined against HeLa cells, human leukaemia CCRF-CEM cells and the multidrug-resistant CEM/ADR5000 subline using the MTT and XTT tests. However, a redox status has been linked with both inflammation and cancer, antioxidant effects were also assessed using the DPPH, lipid-peroxidation, and Folin-Ciocalteau methods.

Results

Among all the nine species, Gynura pseudochina var. hispida and Oroxylum indicum showed the most promising NF-κB inhibitory effects with the lowest IC₅₀ values (41.96 and 47.45 μg/ml, respectively). Muehlenbeckia platyclada did not inhibit the NF-κB activation but effectively inhibited the release of IL-6, IL-1β and TNF-α with IC₅₀ values ranging between 0.28 and 8.67 μg/ml. Pouzolzia indica was the most cytotoxic against CCRF-CEM cells and the multidrug-resistant CEM/ADR5000 cells (9.75% and 10.48% viability, at 10 μg/ml, respectively). Rhinacanthus nasutus was the most potent cytotoxicity against HeLa cells (IC₅₀ 3.63 μg/ml) and showed specific cytotoxicity against the multidrug-resistant CEM/ADR5000 cells (18.72% viability at 10 μg/ml, p < 0.0001 when compared to its cytotoxicity against CCRF-CEM cells). Moreover, Oroxylum indicum showed a high level of antioxidant activity by inhibiting lipid-peroxidation (IC₅₀ 0.08 μg/ml).

Conclusions

This study provides in vitro evidence for the use of the Thai plants, most importantly Gynura pseudochina var. hispida, Oroxylum indicum and Muehlenbeckia platyclada as Thai anti-inflammatory remedies and these plants are now a priority for further phytochemical research.     

Antibacterial, antioxidant and fibroblast growth stimulation activity of crude extracts of Bridelia ferruginea leaf, a wound-healing plant of Nigeria

Aim of the study

Determination of pharmacological activity relevant to wound healing of Bridelia ferruginea leaf, a traditional medicine used to treat wounds in rural Nigeria.

Materials and methods

Aqueous and ethanolic leaf extracts were tested against bacterial species of relevance to wound infections: Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The ethanolic extracts were assessed for their ability to stimulate the growth of human dermal fibroblasts (FS5) and protect against damage induced by hydrogen peroxide. Antioxidant activity was also assessed using the DPPH assay.

Results

Both aqueous and ethanolic extracts had weak antibacterial activity (MIC > 470 μg/ml). A significant effect (p < 0.001) on the growth of FS5 fibroblasts was observed only at a concentration of 5 μg/ml (28% increase), above which the extracts appeared toxic to the cells. The ethanolic extract offered the highest protection against H₂O₂ damage to FS5 cells, comparable with catalase (82% at 250 μg/ml). The DPPH assay revealed antioxidant activity of the ethanolic leaf extract with IC₅₀ 12.5 ± 0.3 μg/ml comparable to l-ascorbic acid (7.3 ± 0.1 μg/ml).

Conclusion

The antibacterial, modest fibroblast stimulation activity and relatively strong antioxidant activity lend some support to the topical use of Bridelia ferruginea leaf for wound-healing in the traditional medicine of South-western Nigeria.     

Comparative antioxidant and anti-inflammatory effects of [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol

Ethnopharmacological relevance

Zingiber officinale Rosc. (Zingiberaceae) has been traditionally used in Ayurvedic, Chinese and Tibb-Unani herbal medicines for the treatment of various illnesses that involve inflammation and which are caused by oxidative stress. Although gingerols and shogaols are the major bioactive compounds present in Zingiber officinale, their molecular mechanisms of actions and the relationship between their structural features and the activity have not been well studied.

Aim of the study

The aim of the present study was to examine and compare the antioxidant and anti-inflammatory activities of gingerols and their natural analogues to determine their structure–activity relationship and molecular mechanisms.

Materials and methods

The in vitro activities of the compounds [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol were evaluated for scavenging of 1,1-diphenyl-2-picyrlhydrazyl (DPPH), superoxide and hydroxyl radicals, inhibition of N-formyl-methionyl-leucyl-phenylalanine (f-MLP) induced reactive oxygen species (ROS) production in human polymorphonuclear neutrophils (PMN), inhibition of lipopolysaccharide induced nitrite and prostaglandin E₂ production in RAW 264.7 cells.

Results

In the antioxidant activity assay, [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol exhibited substantial scavenging activities with IC₅₀ values of 26.3, 19.47, 10.47 and 8.05 μM against DPPH radical, IC₅₀ values of 4.05, 2.5, 1.68 and 0.85 μM against superoxide radical and IC₅₀ values of 4.62, 1.97, 1.35 and 0.72 μM against hydroxyl radical, respectively. The free radical scavenging activity of these compounds also enhanced with increasing concentration (P < 0.05). On the other hand, all the compounds at a concentration of 6 μM have significantly inhibited (P < 0.05) f-MLP-stimulated oxidative burst in PMN. In addition, production of inflammatory mediators (NO and PGE₂) has been inhibited significantly (P < 0.05) and dose-dependently.

Conclusions

6-Shogaol has exhibited the most potent antioxidant and anti-inflammatory properties which can be attributed to the presence of α,β-unsaturated ketone moiety. The carbon chain length has also played a significant role in making 10-gingerol as the most potent among all the gingerols. This study justifies the use of dry ginger in traditional systems of medicine.     

Antinociceptive action of ethanolic extract obtained from roots of Humirianthera ampla Miers

Humirianthera ampla Miers is a member of the Icacinaceae family and presents great amounts of di and triterpenoids. These chemical constituents in roots of Humirianthera ampla sustain not only the ethnopharmacological use against snake venom, but also some anti-inflammatory and analgesic properties of the plant. In this study we investigated the antinociceptive action of the ethanolic extract (EE) from roots of the Humirianthera ampla in chemical and thermal models of pain in mice. The oral treatment with ethanolic extract dose-dependently inhibited glutamate-, capsaicin- and formalin-induced licking. However, it did not prevent the nociception caused by radiant heat on the tail-flick test. The ethanolic extract (30 mg/kg) caused marked inhibition of the nociceptive biting response induced by glutamate, (+/-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid (trans-ACPD), N-methyl-d-aspartate (NMDA) and substance P. The antinociception caused by ethanolic extract was significantly attenuated by naloxone, l-arginine, WAY100635, ondansetron or ketanserin, but not by caffeine or naloxone methiodide. In conclusion, the ethanolic extract from roots of Humirianthera ampla produces antinociception against neurogenic and inflammatory models of nociception. The mechanisms of antinociception involve nitric oxide, opioid, serotonin and glutamate pathways. Therefore, our results support the ethnopharmacological use of the Humirianthera ampla against inflammatory and painful process caused by snake venom.     

Antibacterial, antioxidant and fibroblast growth stimulation of aqueous extracts of Ficus asperifolia Miq. and Gossypium arboreum L., wound-healing plants of Ghana

AIM OF THE STUDY: Use of in vitro tests to search for relevant activities in bark of Ficus asperifolia Miq. and leaves of Gossypium arboreum L., used in Ghana for wound healing. MATERIALS AND METHODS: Aqueous extracts of the relevant parts of the two species were tested for antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Micrococcus flavus, Escherichia coli, Pseudomonas aeruginosa and resistant strains of Staphylococcus aureus SA1199B, RN4220 and XU212. The effects of the plants on fibroblast growth stimulation as well as antioxidant protective effect against hydrogen peroxide induced damage in the same cell line were also studied. RESULTS: The extracts of Gossypium arboreum and Ficus asperifolia had weak antibacterial action against all bacteria tested. The extracts of the two plants had significant (p<0.001) effects on the growth of human dermal fibroblast at 50mug/ml and lower. They also significantly protected fibroblast cells against oxidative damage at doses up to 50mug/ml. Gossypium arboreum leaf extract displayed the higher activity. CONCLUSION: The stimulatory effect on fibroblast growth and protection against peroxide-induced oxidative damage give some support to the traditional use of these two plants as wound-healing agents.     

Ethnopharmacological studies on antispasmodic and antiplatelet activities of Ficus carica

ETHNOPHARMACOLOGICAL RELEVANCE: The ripe dried fruit of Ficus carica Linn. (Moraceae) commonly known as "Fig" has medicinal value in traditional system of medicine for its use in gastrointestinal and inflammatory disorders. AIM OF THE STUDY: To rationalize the medicinal use of Fig (Ficus carica) in gastrointestinal and inflammatory disorders. MATERIALS AND METHODS: The aqueous-ethanolic extract of Ficus carica (Fc.Cr) was studied for antispasmodic effect on the isolated rabbit jejunum preparations and for antiplatelet effect using ex vivo model of human platelets. RESULTS: Fc.Cr tested positive for alkaloids, flavonoids, coumarins, saponins, sterols and terpenes. When tested in isolated rabbit jejunum, Fc.Cr (0.1-3.0mg/mL) produced relaxation of spontaneous and low K(+) (25mM)-induced contractions with negligible effect on high K(+) (80mM) similar to that caused by cromakalim. Pretreatment of the tissue with glibenclamide caused rightward shift in the curves of low K(+)-induced contractions. Similarly, cromakalim inhibited the contractions induced by low K(+), but not of high K(+), while verapamil equally inhibited the contractions of K(+) at both concentrations. Fc.Cr (0.6 and 0.12mg/mL) inhibited the adenosine 5'-diphosphate and adrenaline-induced human platelet aggregation. CONCLUSION: This study showed the presence of spasmolytic activity in the ripe dried fruit of Ficus carica possibly mediated through the activation of K(+)(ATP) channels along with antiplatelet activity which provides sound pharmacological basis for its medicinal use in the gut motility and inflammatory disorders.     

Anti-inflammatory and antioxidant activities of Costus afer Ker Gawl. hexane leaf fraction in arthritic rat models

Ethnopharmacological relevance

Costus afer Ker Gawl is an indigenous tropical African medicinal plant used as therapy in the treatment of inflammatory ailments such as rheumatoid arthritis. This study was designed to evaluate the anti-inflammatory and antioxidant activities of the hexane fraction of C. afer leaves (CAHLF).

Materials and methods

The anti-inflammatory effect of varying doses of CAHLF on carrageenan, arachidonic acid, and formaldehyde induced arthritis in male albino rats? models were investigated in order to study the acute inflammatory phase. Complete Freund?s Adjuvant (CFA)-induced arthritis model was used to study the chronic inflammatory phase. Two known anti-inflammatory drugs, Diclofenac sodium (non-steroidal anti-inflammatory drug [NSAID]) and prednisolone (glucocorticoid [steroidal drug]) were used as standards for comparison. Various biochemical indices viz. superoxide dismutase (SOD), catalase (CAT), glutathione S-transferase (GST), reduced glutathione (GSH) and malondialdehyde (MDA), aspartate amino transferase (AST), alanine amino transferase (ALT), alkaline phosphatase (ALP), total bilirubin (TB), total protein (TP), globulin and albumin levels were assayed using spectrophotometric methods.

Results

Control animals in which arthritis have been induced using carrageenan, arachidonic acid, formaldehyde or CFA showed significant increases (P<0.05) in paw edema when compared with normal animals. Treatment of the arthritis induced rats with CAHLF significantly (P<0.05) suppressed the edema. in vivo antioxidant study showed that CAHLF treated animals had a significantly (P<0.05) elevated GSH level, SOD, CAT and GST activities while MDA levels were significantly (P<0.05) reduced in the plasma, liver, kidney and brain. CAHLF treated rats had a significantly (P<0.05) reduced plasma AST, ALT and ALP. Plasma TP, globulin, TB levels were reduced while albumin levels were elevated in CAHLF treated animals.

Conclusions

CAHLF possesses substantial anti-inflammatory and antioxidant activities against inflammatory diseases especially arthritis. It could be considered as a choice candidate in pharmaceutical anti-inflammatory drug development.     

Pharmacological and phytochemical study on a Sisymbrium officinale Scop. extract

Ethnopharmacological relevance

The aerial parts of Sisymbrium officinale Scop. are commonly used to treat airway ailments, moreover in antiquity the herbal drug was reputed to possess anticancer properties. The results obtained in present work support the traditional use and the properties ascribed to Sisymbrium officinale.

Aim of the study

In order to give a scientific basis to the traditional uses of Sisymbrium officinale, this study was aimed to evaluate in vitro the myorelaxant activity, the antimicrobial properties and the antimutagenic effect of an aqueous dry extract of the aerial parts of the plant. A phytochemical characterization of the extract was also performed.

Materials and methods

The myorelaxant activity was studied against the contractions induced by carbachol, histamine and leukotriene C₄, in isolated guinea-pig trachea. The antimicrobial activity was tested against six bacteria and one yeast. The Ames test, performed by the preincubation method, was used to study the antimutagenic activity of the extract by its capability to inhibit the mutagenic effect of 2-nitrofluorene, sodium azide, methyl methanesulfonate and 2-aminoanthracene, in Salmonella typhimurium TA98, Salmonella typhimurium TA100 and Escherichia coli WP2uvrA strains. The chemical composition of the extract was analyzed by TLC and HPLC.

Results

Sisymbrium officinale showed to reduce the chemically-induced contractions of isolated guinea-pig trachea with major potency against leukotriene C₄ and histamine. The extract did not show any antibacterial activity. The Ames test showed a strong antimutagenic activity against 2-aminoanthracene, in Escherichia coli WP2uvrA and in Salmonella typhimurium TA98 strains. The phytochemical study highlighted the presence of putranjivine, the glucosinolate marker of Sisymbrium officinale, and of proline.

Conclusions

The myorelaxant activity of Sisymbrium officinale offers a scientific basis to its use in traditional medicine. The strong antimutagenic effect suggests further studies to evaluate its possible chemopreventive activity.     

Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis

Aim of the study

Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were isolated. Anti-HIV-1 activities and possible action mechanisms of these compounds were investigated.

Methods

The syncytial formation induced by HIV-1 was determined under the inverted microscope, cellular toxicity and protection assay were assessed by MTT method, reduction of p24 antigen expression level and RT activity were measured by ELISA, and inhibition of recombinant HIV-1 PR was monitored by the fluorescent signal.

Results

The compounds 1 and 13 inhibited HIV-1-induced syncytium formation potently with TI value of 42.31 and 19.07, respectively. Compounds 4, 5, 6, 9 and 10 were less potent with TI value of 8.94, 8.22, 4.14, 5.11 and 5.34, respectively. Compound 1, a benzofuranone-type compound, previously reported as a novel anti-HIV-1 agent, might target late-steps of HIV-1 life cycle. Compound 13 inhibited HIV-1 replication with EC₅₀ of 7.16 μg/ml and might target at/before integration step.

Conclusion

These compounds might contribute to anti-HIV-1 activities extracts of the medicinal plant Rhus chinensis.