The genus Desmodium (Fabaceae)-traditional uses in Chinese medicine, phytochemistry and pharmacology

Ethnopharmacological relevance

Plants of the genus Desmodium (Fabaceae), such as Desmodium styracifolium (Osbeck) Merr. and Desmodium gyrans (L. f.) DC., have a long history of medical use in Traditional Chinese Medicine to treat various ailments including rheumatism, pyrexia, dysentery, wounds, cough, malaria, hepatitis, hemoptysis, etc. In the theory of Traditional Chinese Medicine, most species have the effect of relieving internal heat or fever, neutralizing toxins, inhibiting pain, invigorating blood circulation, suppressing cough and alleviating dyspnea.

Materials and methods

A bibliographic investigation was accomplished by analyzing secondary sources including Chinese Herbal Classics, and worldwide accepted scientific databases (Pubmed, Scopus and Web of Science, SciFinder) were scrutinized for the available information on the ethnopharmacological uses in Chinese medicine, phytochemistry, pharmacology and toxicology of Desmodium species.

Results

The genus Desmodium is a large member of the Papilionaceae (Fabaceae) family. It contains about 350 plant species used for both feeding stuffs and herbal medicines, of which only about 30 species have been phytochemically or pharmacologically investigated. Desmodium plant extracts, as well as the active principles, have been experimentally studied for their anti-inflammatory, cytotoxic, antidiabetic, antinephrolithic, antibacterial, and nootropic activities in vitro or in vivo. And so far, a total of 212 compounds have been isolated from 15 Desmodium species and characterized mainly as flavonoids and alkaloids, followed by terpenoids, steroids, phenols, phenylpropanoids, glycosides and a number of volatile oils. The remaining unrevealed species are recorded chiefly in Asia and Africa being used in empirical treatment for various diseases.

Conclusions

Desmodium species have long been used in TCM to treat various ailments. Available scientific references revealed that the traditional medical uses of some important Desmodium species in TCM have been evaluated by modern pharmacological studies. As literature demonstrated, flavonoids and alkaloids are perhaps responsible for most of the activities shown by the plants of this genus. Further studies are still required to reveal the structure-activity relationship of these active constituents.     

Medicinal and therapeutic potential of Sea buckthorn (Hippophae rhamnoides L.)

Ethnopharmacological context

This review explores the medicinal and therapeutic applications of Sea buckthorn (Hippophae rhamnoides L.) in curtailing different types of acute as well as chronic maladies. The plant is being used in different parts of the world for its nutritional and medicinal properties.

Materials and methods

Sea buckthorn based preparations have been extensively exploited in folklore treatment of slow digestion, stomach malfunctioning, cardiovascular problems, liver injury, tendon and ligament injuries, skin diseases and ulcers. In the recent years, medicinal and pharmacological activities of Sea buckthorn have been well investigated using various in vitro and in vivo models as well as limited clinical trials.

Results

Sea buckthorn has been scientifically analyzed and many of its traditional uses have been established using several biochemical and pharmacological studies. Various pharmacological activities such as cytoprotective, anti-stress, immunomodulatory, hepatoprotective, radioprotective, anti-atherogenic, anti-tumor, anti-microbial and tissue regeneration have been reported.

Conclusion

It is clear that Sea buckthorn is an important plant because of its immense medicinal and therapeutic potential. However, several knowledge gaps identified in this paper would give impetus to new academic and R&;D activities especially for the development of Sea buckthorn based herbal medicine and nutraceuticals.     

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.     

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.     

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.     

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).     

The synergistic anti-inflammatory effect of the combination of sodium ferulate and oxymatrine and its modulation on inflammation-associated mediators in RAW 264.7 cells

Ethnopharmacological relevance

The combination of Radix Angelicae sinensis (Oliv.) Diels and Radix Sophora flavescens Ait. was extensively used in traditional Chinese medicine to treat inflammatory diseases, such as acne, heart disease, and hepatitis. Sodium ferulate (SF) and oxymatrine (OMT) were effective component of Radix Angelicae sinensis (Oliv.) Diels and Radix Sophora flavescens Ait., respectively.

Aim of the study

In this study, we investigated the synergistic anti-inflammatory effect of the combination of SF and OMT, and its modulation on inflammation-associated mediators in RAW 264.7 cells.

Materials and methods

In vivo, the anti-inflammatory effects of the combination of SF and OMT were evaluated with the xylene-induced mouse ear edema model and the carrageenan-induced rat paw edema model. In vitro, chemokines and cytokines mRNA expressions in lipopolysaccharide (LPS)-activated RAW 264.7 cells were determined by real-time PCR (RT-PCR) microarray analysis. The levels of interleukin-11 (IL-11), C-reactive protein (CRP) and interferon-γ (INF-γ) in the supernatant of LPS-stimulated RAW 264.7 cells were measured by enzyme-linked immune-sorbent assay (ELISA).

Results

The combination of SF and OMT could significantly inhibit the edema in the xylene-induced mouse ear edema and carrageenan-induced rat paw edema, but no effect was found when each drug was used alone according to above doses. The combination exhibited a better effect in down-regulating mRNA expressions of inflammation-associated mediators in LPS-stimulated RAW 264.7 cells than SF or OMT alone. The ELISA results showed that the combination synergistically inhibited LPS-induced IL-11, CRP and INF-γ production in a dose-dependent manner.

Conclusion

The combination of SF and OMT showed synergistic anti-inflammatory effect, and the activity was probably related to its modulation on inflammation-associated mediators, especially IL-11, CRP and INF-γ.     

Antisecretory actions of Baccharis trimera (Less.) DC aqueous extract and isolated compounds: analysis of underlying mechanisms

Ethnopharmacological relevance

Baccharis trimera (Less.) DC. (Asteraceae) is a species native to South America used in Brazilian folk medicine to treat gastrointestinal and liver diseases, kidney disorders and diabetes. Previous studies from this laboratory confirmed the antacid and antiulcer activities of the plant aqueous extract (AE) in rat and mouse models.

Aim of the study

To investigate the mechanisms involved in the antacid action of AE and isolated compounds from Baccharis trimera.

Materials and methods

AE was assayed in vivo in cold-restraint stress gastric ulcers and in pylorus-ligated mice. Nine fractions (F2-F10) previously isolated from AE were assayed in vitro on acid secretion measured as [¹⁴C]-aminopyrine ([¹⁴C]-AP) accumulation in rabbit gastric glands, and on gastric microsomal H⁺, K⁺-ATPase preparations. Chlorogenic acids (F2, F3, F6, F7), flavonoids (F9), an ent-clerodane diterpene (F8) and a dilactonic neo-clerodane diterpene (F10) have been identified in these fractions.

Results

Intraduodenal injection of AE (1.0 and 2.0 g/kg) in 4 h pylorus-ligated mice decreased the volume (20 and 50%) and total acidity (34 and 50%) of acid secretion compared to control values. Administered orally at the same doses AE protected against gastric mucosal lesions induced in mice by restraint at 4 °C. Exposure of isolated rabbit gastric glands to fractions F8 (10-100 μM) and F9 (10-300 μg/ml) decreased the basal [¹⁴C]-AP uptake by 50 and 60% of control (Ratio = 6.2 ± 1.1), whereas the remaining fractions were inactive. In the presence of the secretagogues F2 and F4 (30-300 μg/ml) decreased the [¹⁴C]-AP uptake induced by histamine (His) with a 100-fold lower potency than that of ranitidine. F5 and F6 reduced the [¹⁴C]-AP uptake stimulated by carbachol (CCh), but they were 10 to 20-fold less potent than atropine. F8 (diterpene 2) and F9 (flavonoids) decreased both the His- and CCh-induced [¹⁴C]-AP uptake, whereas F10 (diterpene 1) was inactive against the [¹⁴C]-AP uptake stimulated by secretagogues. Diterpene 2 was the most active of all tested compounds being 7-fold less potent than ranitidine and equipotent to atropine in reducing acid secretion in vitro. This compound also reduced the gastric H⁺, K⁺-ATPase activity by 20% of control, while the remaining fractions were inactive on the proton pump in vitro.

Conclusions

The results indicate that Baccharis trimera presents constituents that inhibit gastric acid secretion by acting mainly on the cholinergic regulatory pathway. The plant extract also contains compounds that exert moderate inhibition of the histaminergic regulatory pathway of acid secretion and the gastric proton pump. Altogether these active constituents appear to provide effective inhibition of acid secretion in vivo, which may explain the reputed antiulcer activity of the plant extract.     

The absorption characterization effects and mechanism of Radix Angelicae dahuricae extracts on baicalin in Radix Scutellariae using in vivo and in vitro absorption models

Ethnopharmacological relevance

Angelicae Dahurica(Hoffm.)Benth.&Hook.f.ex Franch.&Sav combined with Scutellaria baicalensis Georgi. has been widely used as herb-pairs in traditional Chinese medicine (TCM) to treat migraine headache and cataract, but the underlying compatibility mechanism of the two herbs remains unknown.

Aim of study

In the present work, we investigated the additive or synergistic effects of absorption behavior of Radix Angelicae dahuricae extracts on baicalin, and the absorption-enhancing mechanism of Radix Angelicae dahuricae extracts on baicalin.

Materials and methods

Total coumarins (Cou) and volatile oil (VO), as the two main components of Radix Angelicae dahuricae, were extracted by supercritical fluid extraction (SFE) further treated with liquid-liquid separation method. The absorption behavior was investigated by applying the everted gut sac technique and in situ single-pass intestinal perfusion method.

Results and conclusions

The results showed that both the Cou and the VO could improve the intestinal absorption of baicalin in vivo, and had synergistic action the enhanced absorption of baicalin. Since verapamil did not affect the P_app and K_a of baicalin significantly, we concluded that the absorption of Baicalin could not be an active transportation in dependent of P-glycoprotein-Mediated efflux systems. Based on intestinal absorption of drug studying was one of the efficacious methods to clarify the compatibility of principles of herb-pairs. The everted gut sac technique and in situ single-pass intestinal perfusion technique model were the effective methods to study the absorption of drug, the application of the animal model to investigating the absorption of herb-drug interactions or other relevant research purposes is envisioned.     

Standardized extract of Dicksonia sellowiana Presl. Hook (Dicksoniaceae) decreases oxidative damage in cultured endothelial cells and in rats

Aims

Aging and a variety of pathologies, including cancer, diabetes, cardiovascular and inflammatory diseases have been associated with reactive oxygen species (ROS), such as superoxide anion (O₂⁻), hydroxyl radical (OH) and hydrogen peroxide (H₂O₂) generation. Plant polyphenols bear radical scavenging/antioxidant activity. A phytomedicinal preparation obtained from aerial parts of Dicksonia sellowiana (Dicksoniaceae), a native plant from Central and South America, has been widely used in Brazil against asthma and presents beneficial effects in several other diseases, including cardiovascular disturbance. In this work, we investigated whether Dicksonia sellowiana, which is also known to contain high levels of polyphenols, presents antioxidant activity.

Methods

The antioxidant activity of the hydroalcoholic extract obtained from Dicksonia sellowiana leaves (HEDS) was investigated by in vitro and in vivo tests.

Results

HEDS (0.1-100 μg/mL) exhibited a strong scavenging activity against all reactive species tested (DPPH, O₂⁻,OH and H₂O₂; IC₅₀ = 6.83 ± 2.05, 11.6 ± 5.4, 2.03 ± 0.4, and 4.8 ± 0.4 μg/mL, respectively). HEDS strongly protected endothelial cells against H₂O₂-induced oxidative stress by mechanisms other than increasing catalase activity. In addition, HEDS protected cell membrane from oxidative damage. HEDS, (20 and 40 mg/kg) inhibited lipid peroxidation in vivo (29.8% and 24.5%, respectively).

Conclusions

According to our results, we can speculate that the traditional uses of Dicksonia sellowiana for cardiovascular diseases, asthma and skin diseases could be, at least in part, related to the potent antioxidant and endothelial protective activities of the plant.     

Wound healing and anti-inflammatory activities of the Michauxia L'Hérit (Campanulaceae) species native to Turkey

Ethnopharmacological relevance

The leaves of Michauxia species are used for the treatment of wounds in Turkish traditional medicine. In the present study, wound healing, anti-inflammatory and antioxidant activities of the extracts obtained from the root and herb of 5 species of Michauxia collected in different parts of Turkey were evaluated.

Material and methods

In vivo incision and excision wound models were used in order to assess the wound healing effects of the methanolic extracts of the plants. Skin samples were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. TBA (thiobarbituric acid) test, qualitative and quantitative DPPH (2,2-diphenyl-1-picrylhydrazyl) tests were used to evaluate the antioxidant activity.

Results

Noteworthy wound healing activity was observed for the ointment formulation prepared with 1% Michauxia nuda (root) and Michauxia tchihatchewii (herb) extracts. The results of histopathological evaluation supported the outcome of incision and excision wound models. Moreover, the Michauxia nuda (root) exerted remarkable anti-inflammatory effect. The highest antioxidant activity was observed with the ethyl acetate extract of Michauxia tchihatchewii herb.

Conclusion

The experimental study revealed that Michauxia displays remarkable wound healing and anti-inflammatory and antioxidant activities.     

The inhibitory activities of the components of Huang-Lian-Jie-Du-Tang (HLJDT) on eicosanoid generation via lipoxygenase pathway

Aim of the study

Huang-Lian-Jie-Du-Tang (HLJDT) is a traditional Chinese medicine with anti-inflammatory use. In the present study, the effects of its component herbs and pure components were observed on eicosanoid generation to find out the contributory components and their precise targets on arachidonic acid (AA) cascade.

Materials and methods

By monitoring leukotriene B₄ (LTB₄), 5-hydroxyeicosatetraenoic acid (5-HETE), and 12-hydroxy-5,8,10-heptadecatrienoic acid (12-HHT), we compared the effects of HLJDT, HLJDT free of one or two component herbs, and water extract of four single component herbs of HLJDT (Rhizoma coptidis, Radix scutellariae, Cortex phellodendri and Fructus gardeniae) on eicosanoid generation in rat elicited peritoneal macrophages. In addition, thirteen pure compounds from HLJDT (baicalin, baicalein, wogonoside, wogonin, berberine, magnoflorine, phellodendrine, coptisine, palmatine, jateorrhizine, crocin, chlorogenic acid, and geniposide) were tested in the macrophages. Furthermore, the efficacies of these thirteen compounds were evaluated on cell-free purified enzymes: leukotriene A₄ hydrolase (LTA₄H), 5-, 15-lipoxygenase (5-, 15-LO), and cyclo-oxygenase-1/2 (COX-1/2). Moreover, the possible synergetic effect on LO pathway derived LTB₄ generation between the active components was also tested in rat peritoneal macrophages.

Results

Our experiments showed that Rhizoma coptidis and Radix scutellariae were responsible for the suppressive effect of HLJDT on eicosanoid generation. Some of the pure components including baicalein, baicalin, wogonoside, wogonin, coptisine, and magnoflorine inhibited eicosanoid generation in rat macrophages via LO pathway of AA cascade. Further experiments on cell-free purified enzymes confirmed that Radix scutellariae derived baicalein and baicalin showed significant inhibition on 5-LO and 15-LO, while Rhizoma coptidis derived coptisine showed medium inhibition on LTA₄H. On the other hand, no significant inhibition of thirteen components on COX-1/2 was observed. Moreover, the slight synergetic inhibition on LTB₄ between baicalein and coptisine was proved in the rat peritoneal macrophages.

Conclusions

Baicalein and coptisine, the active components of HLJDT, for the first time are found to interfere with arachidonic acid cascade via inhibition on different points of LO pathway. This finding makes the mechanism of HLJDT clearer and achieves its safer therapeutic application.     

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.     

The effects of hydroxysafflor yellow A on blood pressure and cardiac function

Aim of the study

This work aims to investigate the effects of HSYA on cardiac function and blood pressure.

Materials and methods

To evaluate changes in mean arterial pressure (MAP) and heart rate (HR), different groups of pentobarbitone-anesthetized normotensive and spontaneously hypertensive rats (SHR) were treated with intravenous HSYA (0.1-3 mg/kg). Isolated WKY rat hearts in Langendorff system were employed for examining the effect of HSYA on hemodynamic. After 30 min equilibration time the isolated hearts were perfused with HSYA (30 μmol/L) in a stepwise fashion. Potassium channel inhibitors were used to determine the role of potassium channel activation in HSYA effect.

Results

Intravenous injection of the HSYA significantly reduced MAP and HR in both normotensive rats and SHR in a dose-dependent manner. HSYA reduced left ventricular systolic pressure (LVSP), left ventricular end-diastolic pressure (LVEDP), the maximum rate of increase of left ventricular pressure (+dp/dt_max) and heart rate (HR) in a dose-dependent manner. HSYA had no remarkable effect on the maximum rate of decrease of left ventricular pressure (−dp/dt_max); BK_Ca and K_ATP blocker can weakened the inhibitory effect of HSYA on heart function and HR, but K_V and K_ACh blocker did not significantly weaken the HSYA effects.

Conclusion

Our results show that HSYA could significantly reduce blood pressure and heart rate, which may be related to activation of BK_Ca and K_ATP channels.     

Phaleria macrocarpa (Scheff.) Boerl fruit aqueous extract enhances LDL receptor and PCSK9 expression in vivo and in vitro

Ethnopharmacological relevance

Phaleria macrocarpa (Scheff.) Boerl (Pm) has been shown to reduce cholesterol level in vitro and in vivo experiment.

Aim of the study

This study investigated the effects of Pm fruit on weight control and mechanistic basis of its anti-hypercholesterolemic effect in both in vivo and in vitro.

Materials and method

In the in vivo study, thirty six male Sprague Dawley were randomized to six groups. Five groups were induced into hypercholesterolemia by giving 3% cholesterol enriched-diet for 52 days while one group acted as control. The rats were then treated with Pm extract (0, 20, 30 and 40 mg/ml) or simvastatin for 84 days. The following parameters were determined: (1) body weight, (2) blood lipid profile (total cholesterol, triglyceride, HDL and LDL) and (3) hepatic LDL receptor (160 kDa and 120 kDa) and PCSK9 proteins. In the in vitro study, HepG2 cells were cultured in serum-free RPMI supplemented with 0.2% BSA with or without LDL and in the presence of Pm extract (0, 0.1, 2, 40 and 1000 μg/ml) or simvastatin (4.60 μg/ml) for 24 h. The abundance of both LDL receptor and PCSK9 proteins and mRNA were investigated.

Results

Pm extract significantly (P < 0.05) reduced body weight gain, total cholesterol, triglycerides, HDL LDL levels and upregulated hepatic LDL receptor as well as PCSK9 proteins of hypercholesterolemic rats. These results were supported by studies in HepG2 cells whereby Pm extract also significantly upregulated both LDL receptor and PCSK9 at protein and mRNA levels.

Conclusion

This study enhances the potential usage of Pm fruit for controlling the body weight of obese people and for treating hypercholesterolemia.     

Hypoglycemic activity of Thai medicinal plants selected from the Thai/Lanna Medicinal Recipe Database MANOSROI II

Ethnopharmacological relevance

Five medicinal plants including Anogeissus acuminata (Roxb. ex DC.) Gills. & Perr. (Combretaceae), Catunaregam tormentosa (Bl. ex DC.) Tirveng (Rubiaceae), Dioecrescis erythroclada (Kurz) Tirveng. (Rubiaceae), Mimosa pudica Linn. var. hispida Bren. (Fabaceae), and Rauwolfia serpentina (L). Benth. ex Kurz. (Apocyanaceae), which have been traditionally used for the treatment of diabetes mellitus and other diseases for several generations by the Thai-Lanna people in the Northern part of Thailand were investigated for their hypoglycemic activity in normoglycemic and alloxan, induced diabetic mice.

Materials and methods

The aqueous extracts of the selected five medicinal plants were tested for their phytochemicals, free radical scavenging activity and hypoglycemic activity on 18 h fasted normoglycemic and alloxan induced diabetic mice over a period of 4 h comparing with the standard anti-diabetic drugs (insulin and glibenclamide) using two way analysis of variance (ANOVA) as analytical tool. Phytochemical analysis was performed using the standard methods while 2,2-diphenyl-1-picrylhydrazine (DPPH) was used to test for free radical scavenging activities of the medicinal plant extracts.

Results

Phytochemicals detected in the extracts were glycosides, xanthones, tannins, alkaloids and saponins. Anogeissus acuminata showed the highest free radical scavenging activity with the IC₅₀ value of 11.00 μg/mL which was 4 folds of the standard ascorbic acid. Significant reduction in fasting blood glucose (FBG) levels of the normoglycemic mice was observed at 4 and 3 h with the extracts of Mimosa pudica (200 mg/kg bw) and Rauwolfia serpentina (100 mg/kg bw), and percentage decreases of 46.15 and 27.94% which were 0.76 and 1.47; 0.53 and 0.91 folds of insulin and glibenclamide, respectively. In alloxan induced diabetic mice, all extracts showed significant (p < 0.05) hypoglycemic activity, with the maximum FBG reduction of 78.96 at 100 mg/kg bw shown by Anogeissus acuminata at the 4 h. The hypoglycemic activity of Anogeissus acuminata was comparable to insulin (1.1 fold), but more potent than glibenclamide (1.76 folds).

Conclusions

Medicinal plants selected from the Thai/Lanna Medicinal Plant Recipe Database MANOSROI II showed hypoglycemic activity in normoglycemic and alloxan induced diabetic mice. This study confirmed the traditional use of these medicinal plants for the treatment of diabetes mellitus and the thiazolidiendiones mimic hypoglycemic effects of the medicinal plants was suggested.     

Anti-inflammatory and antinociceptive effects of Arrabidaea brachypoda (DC.) Bureau roots

Aim of the study

Arrabidaea brachypoda (DC.) Bureau has been used to relieve general pain, painful joints and kidney stones in Brazilian folk medicine. Nevertheless, scientific information regarding this species is scarce; there are no reports related to its possible analgesic and anti-inflammatory effects. This study was aimed at evaluating the traditional use of Arrabidaea brachypoda root using in vivo inflammatory and nociceptive models.

Materials and methods

Carrageenan-induced paw edema, peritonitis and fibrovascular tissue growth induced by s.c. cotton pellet implantation were used to investigate the anti-inflammatory activity of Arrabidaea brachypoda roots ethanolic extract (AbEE) in rats. Formalin and acetic acid-induced writhing tests were used to investigate the antinociceptive activity in mice. High-performance liquid chromatography (HPLC) was used to determine the fingerprint chromatogram of AbEE.

Results

The AbEE at test doses of 30-300 mg/kg p.o. demonstrated anti-inflammatory effects. AbEE reduced paw edema induced by carrageenan, inhibited leukocyte recruitment into the peritoneal cavity and, in the model of chronic inflammation using the cotton pellet-induced fibrovascular tissue growth in rats, significantly inhibited the formation of granulomatous tissue. The extracts at test doses of 30-300 mg/kg p.o. clearly demonstrated antinociceptive activity, except during the first phase of the formalin test. The presence of quercetin and phenolic compounds in the extract Arrabidaea brachypoda was confirmed using HPLC.

Conclusion

Arrabidaea brachypoda ethanol extract markedly demonstrated anti-inflammatory action in rats and antinociceptive activity in mice, which supports the previous claims of traditional use.     

Isolation of narciprimine from Cyrtanthus contractus (Amaryllidaceae) and evaluation of its acetylcholinesterase inhibitory activity

Ethnopharmacological relevance

Plants of the family Amaryllidaceae are used widely in traditional medicine in South Africa. Several of these, including representatives of the genus Cyrtanthus find use in the treatment of mental illness and age-related dementia.

Aim of the study

Based on the distribution of central nervous system-activating alkaloidal constituents within the genus Cyrtanthus, Cyrtanthus contractus was here explored for such compounds which could interact with acetylcholinesterase (AChE), of significance in the progression of neurodegeneration associated with Alzheimer's disease.

Materials and methods

The known phenanthridone alkaloid narciprimine was isolated via column chromatography of the ethanolic extract of bulbs of Cyrtanthus contractus. The structure of the compound was determined by high field 2D NMR and mass spectroscopic techniques. The classical method of Ellman et al. was used in the determination of AChE inhibitory activity.

Results

The isolation of narciprimine from Cyrtanthus contractus is a landmark find since it has previously only been identified in Zephyranthes, Narcissus and Lycoris, genera endemic to the Americas, Europe and Asia, respectively. Narciprimine exhibited micromolar inhibitory activity (IC₅₀ 78.9) against the enzyme acetylcholinesterase.

Conclusion

This work represents the first isolation of narciprimine from an African Amaryllidaceae species, which may be of chemotaxonomic significance. The AChE inhibitory activity of narciprimine, taken together with activities of other structurally similar inhibitors within the series affords further insight to the structural details of the lycorine alkaloid acetylcholinesterase inhibitory pharmacophore.     

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.