Antinociceptive, anti-inflammatory and wound healing features in animal models treated with a semisolid herbal medicine based on Aleurites moluccana L. Willd. Euforbiaceae standardized leaf extract: Semisolid Herbal

Ethnopharmacological relevance

Aleurites moluccana L. (Willd) Euforbiaceae is a native tree of Indonesia and India that has become acclimatized and well-adapted to the South and Southwest of Brazil. It is commonly used in traditional medicine to treat pain, fever, inflammation, asthma, hepatitis, headache, gastric ulcer, cuts, skin sores and other ailments. The oral antinociceptive effects of standardized 70:30 (v/v) ethanol:water spray dried extract of A. moluccana leaf, as well as its flavonoids 2?-O-rhamnosylswertisin (I) and swertisin (II), have previously been reported.

Aim

The aim of this study was to develop a stable and effective semisolid herbal medicine for topical use in the treatment of pain, inflammation and wound healing, containing 0.5 and 1.0% of standardized dried extract of A. moluccana.

Materials and methods

The chemical markers I and II were assayed by HPLC-UV analysis after extraction by matrix solid dispersion phase (MSDP) followed analytical validation as ICH Guidelines. The semisolid preparations of Hostacerin CG^® vehicle containing 0.5 and 1.0% of dried extract of A. moluccana were submitted to stability studies (180 day of accelerated and long-term studies). The phytomedicine semisolid was analysed in croton oil-induced ear oedema model in mice, in the healing process, using the excisional wound model in rats, and to prevent mechanical sensitization following plantar incision in rats in the postoperative model of pain.

Results

The MSDP method showed average recovery of 101.6 and 105.7% for I and II, respectively, with good precision (RSD<2.0%) and selectivity, without interference of the excipients. The formulations were approved in the stability studies, maintaining conformity after 180 day of accelerated and long-term studies, with variation<10% in the analytical parameters. The phytomedicine reduced the ear oedema in 37.6±5.7% and 64.8±6.2%, for 0.5 and 1.0% of dried extract, respectively. The formulation also accelerated the healing process by up to 50.8±4.1% and 46.0±4.0% at 0.5 and 1.0% of extract, respectively, and both amounts were capable of preventing the development of mechanical sensitization following plantar incision in rats.

Conclusions

The MSDP followed by HPLC-UV analytical method was appropriate for the quality control of the topical phytomedicine based on A. moluccana. The formulation developed at 0.5 and 1.0% of A. moluccana dried extract proved to be effective as an analgesic, anti-inflammatory and wound healing in the pre-clinical studies, which is in agreement with the ethnopharmacological data.     

千年桐对鹌鹑实验性动脉粥样硬化影响

目的：研究千年桐对鹌鹑实验性动脉粥样硬化（ＡＳ）的影响。方法：采用食饵性ＡＳ模型,测血脂,显微镜下观察主动脉病变。结果：千年桐能升高血浆ＨＬＤ－Ｃ,减少主动脉病变。结论：千年桐有调血脂和抗动脉粥样硬化作用。     

千年桐抗心肌缺血的药理

实验结果表明，千年桐叶水提醇沉液能降低小鼠机体耗氧量，延长夹闭气管小鼠心电消失时间，对抗垂体后叶素致家兔心电图改变和结扎冠脉致大鼠心电图Ｓ－Ｔ段抬高。促癌试验表明千年桐无促癌作用。急性毒性试验表明千年桐叶毒性很小。     

Hypolipidaemic activity of seaweed from Karachi coast

During the present study, ethanol extracts of five seaweed species Solieria robusta, Iyengaria stellata, Colpomenia sinuosa, Spatoglossum asperum and Caulerpa racemosa at 10 mg/ 200 g body weight were tested for their hypolipidaemic activity. All the species significantly decreased the serum total cholesterol, triglyceride and low density lipoprotein cholesterol levels in normal, triton-induced and diet-induced hyperlipidaemic rats. Solieria robusta was found to be the most effective in reducing the lipid profile, particularly in diet-induced hyperlipidaemic rats. A beneficial effect of the ethanol extract of S. asperum was also found on cardiac and liver enzymes in diet-induced hyperlipidaemic rats.     

Hypolipidaemic activity of aqueous Ocimum basilicum extract in acute hyperlipidaemia induced by triton WR-1339 in rats and its antioxidant property

Hyperlipidaemia, atherosclerosis and related diseases are becoming a major health problem in developing countries. Ocimum basilicum is one of the medicinal plants widely used in Morocco to reduce plasma cholesterol and to reduce the risk of atherosclerosis-related diseases. However, mechanisms underlying the reported hypolipidaemic effect of this plant have not been investigated. This study evaluates the lipid lowering effect of aqueous Ocimum basilicum extract in Triton WR-1339-induced hyperlipidaemic rats. Hyperlipidaemia was developed in animals by intraperitoneal injection of Triton (200 mg/kg). After injection of Triton the animals were divided into three treatment groups: hyperlipidaemic, hyperlipidaemic plus herb extract and hyperlipidaemic plus fenofibrate treated rats. At 7 h after the Triton injection, levels of plasma cholesterol, triglycerides and LDL-cholesterol in rats treated also with the Ocimum basilicum extract (0.5 g/100 g body weight) were, respectively, 50%, 83% and 79% lower than Triton-treated rats and HDL-cholesterol was 129% higher than in rats given Triton alone. At 24 h following Ocimum basilicum administration, total cholesterol, triglycerides and LDL-cholesterol levels decreased by 56%, 63% and 68%, respectively, in comparison with the Triton treated group and HDL-cholesterol was not increased significantly. The hypolipidaemic effect exerted by Ocimum basilicum extract was markedly stronger than the effect induced by fenofibrate treatments. Further it was demonstrated that Ocimum basilicum aqueous extract displayed a very high antioxidant power. These results indicate that Ocimum basilicum extract may contain hypolipidaemic and antioxidant substances and its use as a therapeutic tool in hyperlipidaemic subjects may be of benefit and encourage further investigation in this field.     

Antinociceptive activity of methanol extract of flowers of Impatiens balsamina

Ethnopharmacological relevance

Impatiens balsamina Linn. (Balsaminaceae), an annual herb locally called “Dopati”, is cultivated as an ornamental garden plant in Bangladesh. Flowers of the plant are used in folk medicine to treat lumbago, neuralgia, burns and scalds.

Aim of the study

This study evaluated the antinociceptive effect of the methanol extract of I. balsamina flowers (MIB).

Materials and methods

The extract was evaluated for antinociceptive activity using chemical- and heat-induced pain models such as acetic acid-induced writhing, hot plate, tail immersion and formalin test. To verify the possible involvement of opioid receptor in the central antinociceptive effect of MIB, naloxone was used to antagonize the effect. The effect of MIB on central nervous system (CNS) was also studied using hole cross and open field tests.

Results

MIB demonstrated strong and dose-dependent antinociceptive activity in all the chemical- and heat-induced mice models (p<0.05). These findings imply the involvement of both peripheral and central antinociceptive mechanisms. The use of naloxone confirmed the association of opioid receptors in the central antinociceptive effect. MIB also showed significant central nervous system depressant effect (p<0.05).

Conclusion

This study reported the peripheral and central antinociceptive activity of the flowers of I. balsamina and rationalized the traditional use of the flower in the treatment of different painful conditions.     

Hypolipidaemic effect of fenugreek seeds. A clinical study

The hypolipidaemic effect of fenugreek seeds (Trigonella foenum graecum L.) was evaluated in ten hyperlipidaemic subjects. Isocaloric diets with and without fenugreek were each given for 20 days. Ingestion of experimental diets, containing 100 g of debitterized fenugreek powder, resulted in a significant reduction in the serum total cholesterol, LDL and VLDL cholesterol and triglyceride levels. HDL cholesterol levels were not altered but the ratio with total cholesterol and LDL and VLDL cholesterol were significantly increased. These results indicate the beneficial effect of fenugreek seeds in hyperlipidaemic patients.     

Antidiarrhoeal activity of the aqueous extract of Terminalia avicennoides roots

The antidiarrhoeal effects of the aqueous root extract of Terminalia avicennoides were evaluated in rodents. Studies were carried out on the isolated rabbit jejunum, gastrointestinal motility in vivo and on castor oil-induced diarrhoea in mice. The results revealed that the extract exhibited a concentration-dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum and attenuated acetylcholine induced contractions. The extract (100, 200 and 400 mg/kg) also caused a dose-dependent decrease of gastrointestinal transit and markedly protected mice against castor oil-induced diarrhoea. The intraperitoneal LD(50) of the extract was found to be 871.4-917.4 mg/kg in mice (95% confidence). A preliminary phytochemical screening of the aqueous extract of T. avicennoides roots revealed the presence of tannins, saponins and flavonoids. The results obtained showed that the water extract of T. avicennoides roots may contain some biologically active principles that may be active against diarrhoea and this may be the basis for its use traditionally for gastrointestinal disorders.     

复方桐叶烧伤油对细胞性皮肤溃疡模型大鼠的影响

目的:研究复方桐叶烧伤油对皮肤溃疡的作用.方法:切割大鼠背部皮肤造成缺损皮肤伤口,再涂粪水细菌感染3天形成皮肤溃疡模型.然后经复方桐叶烧伤油治疗14天,测定大鼠创面面积,溃疡皮肤组织病理及TGF-α、TNF-β含量.结果:经复方桐叶烧伤油治疗14天后创面明显缩小,溃疡皮肤组织中的TGF-α含量升高,TNF-β含量降低;溃疡皮肤组织中肉芽组织厚度明显降低,炎症细胞数明显减少.结论:复方桐叶烧伤油对慢性皮肤溃疡有较好的治疗作用.     

Antiasthmatic activity of the methanol extract of leaves of Passiflora incarnata

The methanol extract of the leaves of P. incarnata was evaluated for its antiasthmatic effects against acetylcholine chloride (Ach)-induced-bronchospasm in guinea-pigs at doses of 50, 100 and 200 mg/kg. Using a 7-day treatment regimen, significant prevention of dyspnoea-related-convulsions was noted in the animals treated with a 100 mg/kg dose of this extract. No preventive effect was exhibited by the 50 mg/kg dose and at a higher dose, i.e. 200 mg/kg, the preventive effects against Ach-chloride-induced-dyspnoea were also reduced. This may be due to defective alpha-adrenoceptor function reported after excessive or continuous administration of an alpha-receptor agonist.     

Three‐arm,placebo‐controlled,randomized clinical trial evaluating the metabolic effect of a combined nutraceutical containing a bergamot standardized flavonoid extract in dyslipidemic overweight subjects

Our double‐blind, placebo‐controlled, parallel‐group, dose‐escalation, clinical trial aimed to test the effect of a combined nutraceutical containing bergamot extract (120‐mg flavonoids), phytosterols, vitamin C, and chlorogenic acid from dry artichoke extract on 90 overweight dyslipidemic subjects. Participants were randomly allocated to treatment with two pills of either active treatment or placebo, or a combination of both (a pill per treatment). After 8 weeks, all active‐treated groups experienced a significant improvement in triglycerides (TG) versus placebo and in low‐density lipoprotein cholesterol (LDL‐C) versus baseline and placebo treatments. In the high‐dose‐treated group, also total cholesterol (TC), nonhigh‐density lipoprotein cholesterol (non‐HDL‐C), γ‐glutamil transpeptidasi, high‐sensitivity C‐reactive protein (hs‐CRP), and tumor necrosis factor‐α (TNF‐α) significantly decreased. At 24‐week follow‐up, TG levels maintained lower than baseline in all groups. All patients allocated to either low‐dose or high‐dose active treatment experienced a significant decrease in TG, LDL‐C, and homeostatin model assessment of insulin resistance. In subjects taking high‐dose active treatment, adiponectin significantly increased, whereas TC, non‐HDL‐C, insulin (fasting plasma insulin), leptin, leptin/adiponectin ratio, hs‐CRP, and TNF‐α were significantly reduced. The tested nutraceutical showed to improve lipid and glucose metabolism, adipokines pattern, and systemic inflammation in dyslipidemic overweight subjects.     

Antioxidant activity of the methanol fraction of Pluchea indica root extract

Studies were carried out to evaluate the influence of the methanol fraction of Pluchea indica Less root extract (PIRE), the dual inhibitors (BW 755C and phenidone) and vitamin on both in vivo and in vitro free radical-scavenging activities, CCl(4)-induced lipid peroxidation and the metabolism of arachidonic acid by lipoxygenase. PIRE produced significant antiinflammatory activity against glucose oxidase-induced paw oedema (in vivo), inhibited hydroxyl radical and superoxide generation, lysis of erythrocytes induced by hydrogen peroxide, CCl(4)-induced lipid peroxidation and also dioxygenase activity of lipoxygenase (both in the presence and absence of hydrogen peroxide). Significantly higher free radical-scavenging activity was observed with BW 755C and phenidone compared with PIRE. However, both BW 755C and phenidone stimulated hydroxyl radical generation compared with the observed inhibitory effects of PIRE and vitamin E.     

Hypolipidemic activity of aqueous extract of Withania coagulans Dunal in albino rats

Administration of an aqueous extract of fruits of Withania coagulans (1 g/kg; p.o.) to high fat diet induced hyperlipidemic rats for 7 weeks, significantly reduced elevated serum cholesterol, triglycerides and lipoprotein levels. This drug also showed hypolipidemic activity in triton induced hypercholesterolemia. The histopathological examination of liver tissues of treated hyperlipidemic rats showed comparatively lesser degenerative changes compared with hyperlipidemic controls. The hypolipidemic effect of W. coagulans fruits was found to be comparable to that of an Ayurvedic product containing Commiphora mukkul.     

Evaluation of hypoglycemic and hypolipidemic activity of methanol extract of Brassica oleracea

AIM： The hypoglycemic and hypolipidemic effects of the methanol extract of Brassica oleracea var. capitata（MEB） was evaluated in alloxan-induced diabetic rabbits. METHOD： The study was conducted on twenty-eight healthy white rabbits of either sex. All animals were equally divided into four groups. After confirmation of hyperglycemia, the animals of the treated and standard groups were administered MEB（500 mg·kg-1） and glibenclamide（10 mg·kg-1）, respectively for 15 and 30 days. The animals of the normal and diabetic controls received normal saline 1 mL/day equivalent to the volume of doses given to the test and standard animals. Biochemical tests were performed at the end of dosing, i.e. the 16 th and 31 st days. RESULTS： The MEB revealed a decrease of 106.6 mg·dL-1 in fasting blood glucose as compared to diabetic control, which was almost comparable to glibenclamide; both of these changes were highly significant. The decrease in total cholesterol and low density lipoprotein was 94.3 and 96.5 mg·dL-1, respectively, whereas the high-density lipoprotein was increased by 26.7 mg·dL-1, as compared to diabetic control. All of the changes in lipid profile were statistically significant. CONCLUSION： These results suggest the potential of MEB as a hypoglycemic and hypolipidemic agent.     

Antiinflammatory activity of methanol extract isolated from stem bark of Magnolia kobus

The present study reports the antiinflammatory activity of a methanol extract isolated from the stem bark of Magnolia kobus (MK). MK potently inhibited lipopolysaccharide (LPS)-induced production of nitric oxide and interleukin-1beta (IL-1beta) in RAW 264.7 cells, a murine macrophage-like cell line. The secretion of tumor necrosis factor-alpha (TNF-alpha) was also suppressed in LPS-stimulated RAW 264.7 cells although the magnitude of inhibition was weaker than that of nitric oxide and IL-1beta. The mRNA expressions of inducible nitric oxide synthase (iNOS), IL-1beta and TNF-alpha were also suppressed by MK in LPS-stimulated RAW 264.7 cells. Further study demonstrated that LPS-induced DNA binding of AP-1 and phosphorylation of c-jun N-terminal kinase (JNK) were inhibited by MK treatment in RAW 264.7 cells, whereas phosphorylation of p38 mitogen-activated protein kinase was unaffected. Moreover, topical application of MK suppressed ear swelling in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin inflammation model. Collectively, these results suggest that MK exerts antiinflammatory effects in vitro and in vivo and this might be mediated, at least in part, by blocking AP-1 and JNK activation.     

Anti-inflammatory activity of methanol extract of Kalopanax pictus bark and its fractions

Dried pulverized bark of Terminalia arjuna Linn (TA) was administered orally to Wistar albino rats (120-150 g) in two doses [500 and 750 mg/kg in 2% carboxy methyl cellulose (CMC)], 6 days per week for 12 weeks. Thereafter, rats were sacrificed either for determination of baseline changes in cardiac endogenous antioxidant compounds [superoxide dismutase (SOD), reduced glutathione (GSH) and catalase (CAT)] or the hearts were subjected to oxidative stress associated with in vitro ischemic-reperfusion injury (IRI). There was significant increase in the baseline contents of thiobarbituric acid reactive substance (TBARS) (a measure of lipid peroxidation) with both doses of TA. However, only in the 500 mg/kg treated group, this was accompanied by a simultaneous increase in SOD, GSH and CAT levels, but not in the 750 mg/kg treated group, where only CAT was raised. Significant rise in myocardial TBARS and loss of SOD, CAT and GSH (suggestive of increased oxidative stress) occurred in the vehicle-treated hearts subjected to in vitro IRI. Only hearts, harvested from the 500 mg/kg rats treated rats, were significantly protected from oxidative stress, when subjected to in vitro IRI. The results suggest that crude bark of TA augments endogenous antioxidant compounds of rat heart and also prevents oxidative stress associated with IRI of the heart.     

Aphrodisiac activity of methanol extract of leaves of Passiflora incarnata Linn in mice

The aphrodisiac properties of the methanol extract of leaves of Passiflora incarnata Linn. have been evaluated in mice by observing the mounting behaviour. The methanol extract of P. incarnata exhibited significant aphrodisiac behaviour in male mice at all doses, i.e. 75, 100 and 150 mg/kg. Amongst these, the highest activity was observed with the 100 mg/kg dose when the mountings were calculated about 95 min after the administration of the test extracts.     

Anti-angiogenic activity of methanol extract of Phellinus linteus and its fractions

Aim of the study

The aim of the present study was to investigate the effects of MeOH extract of PL (PLME) and its fractions on angiogenesis.

Materials and methods

PLME and its subsequent fractions (methylene chloride, ethyl acetate, n-butanol and aqueous fractions) were evaluated in vitro. Specifically, the anti-angiogenic activities of PLME and its fractions were investigated by measuring their effects on the proliferation, migration, tube formation and phosphorylation of vascular endothelial growth factor receptor (VEGFR)-2 in human umbilical vein endothelial cells (HUVECs). In addition, the in vivo Matrigel plug model was applied to evaluate new vessel formation.

Results

The results revealed that PLME and its subsequent fractions, except for the aqueous fraction, led to significant inhibition of the proliferation, migration, tube formation and VEGFR-2 phosphorylation of HUVECs as well as in vivo angiogenesis.

Conclusions

These findings indicate the potential for the use of PLME in pathological situations involving stimulated angiogenesis, such as inflammation and tumor development.     

Central nervous system activity of the methanol extract of Ficus platyphylla stem bark

The central nervous system (CNS) activity of the methanolic extract of Ficus platyphylla stem bark was studied on locomotor activity, pentobarbital sleeping time, exploratory behaviour, amphetamine-induced hyperactivity, apomorphine-induced stereotypy, active-avoidance and performance on tread mills (rota-rod), using mice and rats. The results revealed that the extract significantly reduced the locomotor and exploratory activities in mice, prolonged pentobarbital sleeping time in rats, attenuated amphetamine-induced hyperactivity and apomorphine-induced stereotypy in mice, dose-dependently. The extract significantly suppressed the active-avoidance response in rats, with no significant effect on motor co-ordination as determined by the performance on rota-rod. The results suggest that the extract may possess sedative principles with potential neuroleptic properties.