Structures of steroidal alkaloid oligoglycosides, robeneosides A and B, and antidiabetogenic constituents from the Brazilian medicinal plant Solanum lycocarpum

In the course of our studies on antidiabetogenic compounds from natural medicines and medicinal foodstuffs, a methanolic extract of the fruits of Solanum lycocarpum showed an inhibitory effect on the increase of serum glucose levels in oral sucrose-loaded rats. Through bioassay-guided separation, three known steroidal alkaloid oligoglycosides, solamargine (1), solasonine (3), and 12-hydroxysolasonine (5), were isolated from the active fraction together with two new steroidal alkaloid oligoglycosides, robeneosides A (2) and B (4). The major constituents, solamargine (1) and solasonine (3), exhibited an inhibitory effect on the increase of serum glucose levels in oral sucrose-loaded rats. In addition, these compounds suppressed gastric emptying in mice. However, this methanolic extract from S. lycocarpum fruits did not have any effect on intestinal alpha-glucosidase (sucrase and maltase) in vitro. It was concluded that these steroidal alkaloid oligoglycosides, 1 and 3, inhibited the increase of rat serum glucose levels by suppressing the transfer of sucrose from the stomach to the small intestine.     

Analgesic and antiinflammatory properties of Sideritis lotsyi var. Mascaensis

The antiinflammatory, analgesic and antimicrobial activities of crude ethanol extracts of Sideritis lotsyi var. mascaensis (Lamiaceae), and chloroform and aqueous fractions were evaluated in mice using paw and ear oedema induced by carrageenan and 12-o-tetradecanoyl-phorbol-acetate (TPA), respectively, as inflammation models, the writhing test induced by acetic acid for evaluating analgesic activity and the disk-diffusion method for testing antimicrobial actions. The results obtained demonstrated significant topical antiinflammatory and analgesic activities for the ethanol extract and chloroform fraction, but no relevant antimicrobial activity against the microorganisms tested.     

Antipyretic and analgesic studies of the ethanalic extract of Teclea nobilis delile

The crude ethanol extract of the leaves of an African medicinal plant Teclea nobilis has been studied for its antipyretic, analgesic and anti-inflammatory activities. The extract exhibited marked antipyretic and analgesic activities while it was found to be weakly active against carrageenin oedema.     

Anti-inflammatory effect of crude extract and isolated compounds from Baccharis illinita DC in acute skin inflammation

Ethnopharmacologycal relevance

The tea from the leaves of Baccharis illinita DC (Asteraceae family) is commonly used by the population as anti-inflammatory (including topically), protective gastric and anti-infectious. However, no studies have been done with this species to confirm its topical anti-inflammatory action.

Aim

This study evaluated he topical effects of crude extract of leaves (CE) and its active constituents in 12-O-tetradecanoilforbol acetate (TPA)-induced ear oedema.

Methodology

CE and compounds effects were tested in commonly used models of TPA-, arachidonic acid (AA)- and capsaicin-ear oedema. Polymorphonuclear (PMN) cell migration was evaluated by mieloperoxidase and analyzed histologically.

Results

CE (0.1–1 mg/ear) caused a dose-related inhibition of TPA-induced ear oedema and PMN influx similarly to that produced by topical application of the steroidal anti-inflammatory drug dexamethasone. The active constituents of the AcOEt fraction kaurenoic acid, α-spinasterol, oleanolic acid and baurenol also inhibited TPA-induced ear edema. Histological analysis of the ear of CE-treated animals confirmed the reduction of edema and of PMN infiltration. Both CE and the nosteroidal anti-inflammatory drug indomethacin inhibited the AA-induced ear oedema, but did not change capsaicin-induced oedema.

Conclusion

These results indicate that the CE and the active constituents have a topical anti-inflammatory effect and the possible mechanisms for the pharmacological effects are discussed.     

Evaluation of the antioedematogenic, free radical scavenging and antimicrobial activities of aerial parts of Tillandsiastreptocarpa Baker-Bromeliaceae

The crude methanolic extract of the aerial parts of Tillandsiastreptocarpa was investigated for their acute toxicity and antioedematogenic, antioxidant and antimicrobial activities. Also, the antioedematogenic activity of the hexane fraction resulting from the partition of the crude methanolic extract was evaluated. The methanolic extract and the hexane fraction showed significant (P < 0.05) inhibition of ear oedema, observed at 2 mg/ear in the croton oil-induced mice ear oedema test. In the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging test, a high reactivity and potent antioxidant effect (IC(50) = 0.0056%, w/v) were observed for the methanolic extract. The antimicrobial activity assay showed that the crude methanolic extract was inactive toward Escherichiacoli, Staphylococcusaureus, Pseudomonasaeruginosa, Bacillussubtilis, Candidaalbicans, C. parapsilosis, C. krusei and C. tropicalis (MIC > 500 microg/ml). The methanolic extract showed no toxic effect on mice at a single dose of 2000 mg/kg (p.o). Common side effects including mild diarrhoea, loss of weight and depression were not recorded. The compounds cycloartenol, 4',5-dihydroxy-3',7-dimethoxyflavanone and a mixture of the steroids stigmasterol, beta-sitosterol and campesterol, were isolated from the hexane fraction and identified by spectroscopic methods.     

Anti-inflammatory and analgesic effects of Daphne retusa Hemsl

Daphne retusa Hemsl. belongs to the genus Daphne, a member of Thymelaeaceae family. The barks and stems of Daphne retusa are used as a folkloric medicine 'Zhu Shi Ma' in Western China because of its effects of detumescence and acesodyne. In this paper, we investigate the anti-inflammatory and analgesic effects of the 75% ethanol extract of the stems and barks of Daphne retusa and different fractions partitioned with petroleum ether, methylene chloride, ethyl acetate and n-butanol, respectively. The anti-inflammatory effects were evaluated using xylene-induced ear oedema in mice and carrageenan-induced paw oedema in rats, while the acetic acid-induced writhing test and hot-plate test as models for evaluating the centrally and peripherally analgesic activity. The results showed the plant has significant anti-inflammatory and analgesic effects (P<0.05-0.01). Meanwhile, the result of the acute toxicity test at which the MTD was above 5g/kg indicates that the plant extract is relatively safe in, and/or non-toxic to, mice. The findings of these experimental animal studies indicate that the Daphne retusa ethanol extract possesses anti-inflammatory and analgesic properties, and thus provide pharmacological support to folkloric, ethnomedical uses of 'Zhu shima' in the treatment and/of management of anti-inflammatory and painful conditions in China.     

Anti-inflammatory effects of crude methanolic extract and fractions of Alchornea cordifolia leaves

The leaves of Alchornea cordifolia were collected, identified, dried, and reduced to coarse powder and extracted with aqueous methanol. Using various solvent treatments, the powdered dried leaf was fractionated into five fractions, A1, A2, B, C, D and E. The fractions were subjected to phytochemical analysis to identify the biologically active constituents. The anti-inflammatory effects of crude methanolic extract (ME) of Alchornea cordifolia leaves and the five fractions were evaluated using egg-albumen-induced rat hind paw oedema as a model of inflammation. The crude extract was also subjected to acute toxicity test. Fraction A2, which exhibited the most promising anti-inflammatory effect, was also subjected to analgesic and ulcerogenic tests. Phytochemical analysis of the extracts showed the presence of terpenes, sterols, flavonoids, tannins, carbohydrates, glycosides, saponins and traces of alkaloids. The LD(50) of the aqueous ME was found to be 1131.4 mg/kg. The crude ME (50 mg/kg) gave anti-inflammatory activity which was significant (P<0.05) at all the observation times (1-3h). The different solvent fractions exhibited varying degrees of anti-inflammatory activities, with terpenoid fraction (A2) and the tannin-containing multi-component fraction (D) showing very high and significant (P<0.01) activity at 100mg/kg, with percentage inhibition of oedema value of 87.69 each. In conclusion, the aqueous ME of Alchornea cordifolia leaves could be beneficial in the management of different inflammatory disease states. Its anti-inflammatory activity may not be attributed only to the terpenoid content.     

Evaluation of the analgesic and topical anti-inflammatory effects of Hypericum reflexum L. fil

The present study investigates the analgesic and topical anti-inflammatory effects of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum reflexum L. fil. in mice. The acetic acid-induced writhing test, formalin test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of all extracts tested from this species significantly inhibit acetic acid-induced writhing in mice. Only the methanol extract and chloroform fraction were significantly active in both phases of formalin-induced pain and in the tail flick assays, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of methanol extract, butanol and chloroform fractions of this species significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.     

Antibacterial and anti-inflammatory activities of extract and fractions from Pyrrosia petiolosa (Christ et Bar.) Ching

Ethnopharmacological relevance

Pyrrosia petiolosa is commonly used as a traditional Chinese medicine for treatment of acute pyelonephritis, chronic bronchitis and bronchial asthma. This study aims to evaluate the antibacterial activity of the ethanol extract and its derived fractions of Pyrrosia petiolosa obtained with solvents of different polarities and to perform the anti-inflammatory screening.

Materials and methods

The powdered aerial parts of Pyrrosia petiolosa were used to extract various fractions with ethanol, petroleum ether, ethyl acetate, N-butanol and aqueous. Qualitative phytochemical screening was performed on the ethanol extract, petroleum ether fraction, ethyl acetate fraction, N-butanol fraction and aqueous fraction. The agar diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were employed to evaluate antibacterial activity of the ethanol extract and fractions. The in vitro cytotoxicity of ethanol extract and fractions was determined using MTT assay. The anti-inflammatory activity was analyzed using the mouse ear swelling induced by xylene.

Results

The phytochemical screening revealed the presence of anthraquinones, flavonoids, terpenoids, steroids, saponins, phenols and reducing sugars in the extract and fractions. Antibacterial results showed that petroleum ether fraction and N-butanol fraction inhibited all the tested microorganisms with the maximum inhibition zone of 15.25±0.35 mm. Ethyl acetate fraction also exhibited good antibacterial activity except Pseudomonas aeruginosa ATCC 27853, while extract and aqueous fraction inhibited 8 out of 13 (61.5%) of the tested microorganisms. The MIC values of ethanol extract and fractions ranged from 1.25 to 10.00 mg/mL and most of the MBC values were equal or twice as high as the corresponding MIC values. The in vitro cytotoxicity showed the ethanol extract and fractions exhibited non-toxic or low toxic activity against lung cancer cell lines A549 and mouse spleen cells. In anti-inflammatory experiment, ethanol extract at 5.0 and 10.0 mg/kg exhibited significant anti-inflammatory activity against the mouse ear swelling induced by xylene and the maximum inhibition rate reached as high as 67%.

Conclusions

Pyrrosia petiolosa could be a potential candidate for future development of a novel antibacterial and anti-inflammatory agent.     

Comparative evaluation of the anti-inflammatory and antinociceptive activity of Turkish Eryngium species

Extracts obtained from the root and aerial parts of various Eryngium (Apiaceae) species are used as folk remedy worldwide for the treatment of various inflammatory disorders. Ethanolic and aqueous extracts obtained from either aerial parts or roots of eight Eryngium species growing in Turkey, i.e., were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Eryngium campestre, Eryngium creticum, Eryngium davisii, Eryngium falcatum, Eryngium isauricum, Eryngium kotschyi, Eryngium maritimum, and Eryngium trisectum. For the antinociceptive activity assessment p-benzoquinone-induced writhing test, and for anti-inflammatory activity carrageenan-induced hind paw oedema and TPA-induced ear oedema tests were employed in mice. According to the results of investigations, except Eryngium falcatum extracts, ethanol extracts either from the aerial parts or roots of Eryngium species showed apparent anti-inflammatory and antinociceptive activity. In spite of potent activity of the ethanol extract from Eryngium isauricum aerial parts was induced gastric damage. Aerial parts and roots of Eryngium maritimum and Eryngium kotschyi were found to possess most promising activities without including any apparent gastric damage.     

Pharmacological assay of Cordia verbenacea. III: Oral and topical antiinflammatory activity and gastrotoxicity of a crude leaf extract

The antiinflammatory effects and gastrotoxicity of a lyophilized 70% ethanol extract of the leaves of Cordia verbenacea were investigated through experimental models in rats and mice. The oral administration of 1.24 mg/kg of the extract significantly inhibited nystatin-induced oedema. Topical application of the extract at a dose of 0.09 mg/ear in mice was clearly more effective than 1.0 mg/ear of naproxen in the reduction of the ear oedema induced by corton oil. At antiinflammatory doses, the extract showed an important protective effect on the gastric mucosa, reducing significantly the number of gastric lesions.     

不同来源黄芩醇提物与水提物抗炎作用比较研究

目的：探讨不同产地（河北、山西、大连）黄芩醇提物与水提物抗炎药效差异。方法：建立干酵母致大鼠足跖肿胀动物模型和二甲苯致小鼠耳肿胀动物模型,观察不同产地黄芩醇提物与水提物对炎症模型肿胀度的影响。结果：小鼠耳肿实验,大连水提物抑制小鼠耳廓炎症优于醇提物（P〈0.05）,山西、河北醇提物抗炎药效优于水提物（P〈0.05）,且山西、河北醇提物在所有提取物中表现出较好的抑制耳廓炎症作用。大鼠足肿实验总体抗炎疗效比较,各个产地的黄芩醇提物均较同产地的水提物表现出较优的抑制肿胀作用（P〈0.05）,河北醇提物具有较好抑制炎症作用（P〈0.01）。结论：3个产地黄芩醇提物和水提物均有一定的抑制炎症作用,产地为河北的黄芩醇提液在3种产地中具有较强的抑制急性炎症作用。     

狭叶荨麻根、茎、叶的抗炎镇痛作用

目的研究狭叶荨麻Urticaangustifolia根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物的抗炎、镇痛作用。方法二甲苯致小鼠耳廓肿胀实验;冰醋酸致小鼠扭体反应实验。结果狭叶荨麻根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物能明显对抗二甲苯致小鼠耳廓肿胀,并显著抑制0.5%醋酸致小鼠扭体反应。结论狭叶荨麻根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物具有显著的抗炎、镇痛活性。     

短葶山麦冬水提物及其主要有效部位和成的抗炎活性(英文)

目的:研究短葶山麦冬水提物((Lm-a)、总皂苷(Lm-s)及主要成分Lm-3的抗炎活性,为其临床应用于治疗炎性疾病提供药理学依据。方法:采用二甲苯诱导小鼠耳廓肿胀和角叉菜胶或组胺诱导小鼠足跖肿胀模型,评价Lm-a,Lm-s和Lm-3灌胃给药的体内抗炎活性;采用肿瘤坏死因子(TNF-α)或佛波酯(PMA)诱导的髓样白血病细胞(HL-60)与人脐静脉内皮细胞(ECV304)黏附模型,考察Lm-3的体外抗炎活性。结果:单次灌胃给予Lm-a(336和672mg.kg-1)明显抑制二甲苯致小鼠耳廓肿胀和角叉菜胶致小鼠足跖肿胀;Lm-s和Lm-3(23.2和4.6mg.kg-1,相当于Lm-a672mg.kg-1)对上述炎症模型显示相似的抗炎活性;相当于短亭山麦冬4g.kg-1生药量的Lm-a、Lm-s及Lm-3均明显抑制组胺致小鼠足跖肿胀;Lm-3(0.01、0.1和1μmol.L-1)体外显著抑制TNF-α或PMA诱导的HL-60与ECV304细胞的粘附作用,提示其抗炎机制可能与调节蛋白激酶C通路等有关。结论:短葶山麦冬具有显著体内外抗炎活性,其主要活性部位和成分为总皂苷和Lm-3,为其临床应用于治疗炎性疾病提供药...     

Appraisal of anti-inflammatory potential of the clubmoss, Lycopodium clavatum L

Studies on four extracts prepared with petroleum ether, chloroform, ethyl acetate and methanol as well as the alkaloid fraction from the aerial parts of Lycopodium clavatum L. of Turkish origin using acetic acid-induced increase in capillary permeability assessment in mice revealed that only the chloroform extract and the alkaloid fraction displayed marked anti-inflammatory effect at a dose of 500mg/kg having percentage of inhibition 24.3 and 32.1, respectively, as compared to indomethacin, which exhibited 44.6% of inhibition at 10mg/kg dose. Bioassay-guided fractionation of the alkaloid fraction of Lycopodium clavatum revealed that the alkaloidal-type of compounds might possibly be responsible for the anti-inflammatory activity of the extract, which supports the folk medicinal utilization of the plant. Gas chromatographic-mass spectrophotometric analysis of the active alkaloid fraction revealed that lycopodine (84.5%) is the major component.     

Antimicrobial and anti-inflammatory activity of folklore: Mallotus peltatus leaf extract

Since ages Mallotus peltatus (Geist) Muell. Arg. var acuminatus (Euphorbiaceae) leaf and stem bark is used in folk medicine to cure intestinal ailments and skin infections. In several intestinal ailments, localized inflammation is of common occurrence and hence we have evaluated the antimicrobial as well as anti-inflammatory activity of M. peltatus leaf extract. The crude methanol extract of M. peltatus leaves was found to be active against Staphylococcus aureus, Staphylococcus saprophyticus, Streptococcus faecalis, Bacillus subtilis, Escherichia coli and Proteus mirabilis and the dermatophytic fungi Microsporum gypseum. The minimum inhibitory concentration (MIC) ranges from 128 to 2000 microg ml(-1) for bacteria and 128 mg ml(-1) for fungi, while the minimum bactericidal concentration (MBC) was 2-4-fold higher than MIC. The methanol-water fraction of the extract showed similar activity against Staphylococcus, Streptococcus, Bacillus and Proteus isolates. The anti-inflammatory activity of the extract against carrageenan (acute model) and dextran-induced (subacute model) rat paw oedema and cotton pellet-induced granuloma (chronic model) in rats were studied using indomethacin (10 mg kg(-1)), a nonsteroid anti-inflammatory drug, as standard. The methanol extract at 200 and 400 mg kg(-1), and the n-butanol fractions A and B at 25 mg kg(-1), exhibited significant anti-inflammatory activity in Albino rats, compared with indomethacin. Phytochemical study revealed the presence of tannins, saponins, terpenoids, steroids and reducing sugars in the crude extract while the n-butanol fractions showed the presence of ursolic acid, beta-sitosterol and some fatty acids as major compounds. Further study with fractions showed that the antibacterial and anti-inflammatory activity is due to either fraction A (ursolic acid) alone or the combination of fractions A and B (beta-sitosterol and fatty acids) of the extract.     

Analgesic and topical anti-inflammatory activity of Hypericum canariense L. and Hypericum glandulosum Ait

The present study investigates the analgesic and topical anti-inflammatory activities of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum canariense L. and Hypericum glandulosum Ait. in mice. The acetic acid-induced writhing test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of methanol extracts, and the aqueous, butanol and chloroform fractions of both species and the infusions of Hypericum glandulosum significantly inhibit acetic acid-induced writhing in mice. Only the infusion, methanol extract and butanol and chloroform fractions of Hypericum glandulosum were significantly active in the tail flick assay, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of all extracts tested from both species, with the exception of the infusions and the Hypericum canariense aqueous fraction, significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.     

药理效应法对藏药熏倒牛不同提取工艺的评价

目的:研究藏药熏倒牛的提取工艺。方法:采用小鼠耳廓二甲苯致炎、小鼠热板法致痛实验,观察熏倒牛不同工艺提取物对抗炎、镇痛作用的影响。结果:熏倒牛传统水煎工艺提取物、传统水煎醇沉工艺提取物、醇提工艺提取物均有抑制二甲苯致小鼠耳肿胀的作用,均可提高小鼠热板法致痛的痛阈(P<0.01),但醇提取物的抗炎、镇痛效果明显优于水煎提取物和水煎醇沉提取物(P<0.01)。结论:熏倒牛乙醇提取物的抗炎、镇痛作用显著,其药理效应明显优于水煎和水煎醇沉工艺。     

两种不同挥发油含量柴胡制剂药效作用研究

目的:对比两种不同挥发油含量柴胡制剂的抗炎、镇痛、解热作用。方法:分别采用二甲苯致炎剂所致小鼠耳廓肿胀实验,醋酸引起小鼠疼痛扭体实验,干酵母致大鼠发热实验,观察两种柴胡制剂的抗炎、镇痛、解热作用,并比较二者差异。结果:采用抗炎、镇痛、解热三种动物模型研究表明,普通柴胡浸膏5g生药/kg、10g生药/kg,富集挥发油的柴胡浸膏5g生药/kg、10g生药/kg均可显著减轻二甲苯所致的小鼠耳肿胀,减少醋酸所致的小鼠扭体反应次数,降低干酵母引起的大鼠体温升高,其中富集挥发油的柴胡浸膏的抗炎活性优于普通柴胡浸膏,但镇痛和解热活性两种浸膏无显著性差异。结论:两种不同挥发油含量柴胡浸膏均具有明显的抗炎、镇痛和解热作用,但柴胡挥发油抗炎活性较高。     

Anti-inflammatory activities of the methanol extracts and an isolated furanoditerpene constituent of Sphenocentrum jollyanum Pierre (Menispermaceae)

Sphenocentrum jollyanum crude extracts and an isolated constituent were evaluated for anti-inflammatory activity using the carrageenan-induced hind paw oedema of healthy adult albino rats and utilizing the oral route of administration. The fruit methanol extract (79.58% inhibition at 200 mg kg(-1)) gave a higher anti-inflammatory activity than the root extract (53.75% inhibition at 200 mg ml(-1)). Further purification of the most active fruit methanol extract (MFE) led to the isolation of three furanoditerpenes identified as columbin, isocolumbin, fibleucin (uv, ir, nmr and ms) as well as a flavonoid-rich fraction (FDE). Both columbin (67.08% inhibition at 20 mg kg(-1), p<0.05) and FDE (76.25% inhibition at 200 mg kg(-1); p<0.05) gave significant anti-inflammatory activities in comparable range with reference acetylsalicylic acid (72.5% inhibition at 100 mg kg(-1)). The results provide some justification for the folkloric uses of Sphenocentrum jollyanum in the treatment of inflammatory-based diseases across the West African sub-region.