Study of anti-inflammatory,analgesic and antipyretic activities of seeds of Hyoscyamus niger and isolation of a new coumarinolignan

A chemical and biological validation of the traditional use of Hyoscyamus niger seeds as anti-inflammatory drug has been established. The methanolic extract of seeds of H. niger (MHN) was evaluated for its analgesic, anti-inflammatory and antipyretic activities in experimental animal models at different doses. MHN produced significant increase in hot plate reaction time, while decreasing writhing response in a dose-dependent manner indicating its analgesic activity. It was also effective in both acute and chronic inflammation evaluated through carrageenin-induced paw oedema and cotton pellet granuloma methods. In addition to its analgesic and anti-inflammatory activity, it also exhibited antipyretic activity in yeast-induced pyrexia model. Furthermore, the bioactive MHN under chemical investigation showed the presence of coumarinolignans as major chemical constituent and yielded a new coumarinolignan, cleomiscosin A methyl ether (1) along with four known coumarinolignans, cleomiscosin A (2), cleomiscosin B (3), cleomiscosin A-9′-acetate (4) and cleomiscosin B-9′-acetate (5). The structure elucidation of 1 was done by spectroscopic data interpretation and comparative HPLC analysis. Cleomiscosin A, but not its isomer cleomiscosin B, reduced dry and wet weight of cotton pellet granuloma in mice. This suggests that cleomiscosin A is an important constituent of MHN responsible for anti-inflammatory activity.     

Four new fluorenone alkaloids and one new dihydroazafluoranthene alkaloid from Caulophyllum robustum Maxim

Four new fluorenone alkaloids, caulophylline A-D (1-4), and one new dihydroazafluoranthene alkaloid, caulophylline E (5) were isolated from the roots of Caulophyllum robustum Maxim. Their structures were elucidated by spectroscopic analysis. Among the isolated alkaloids, Caulophylline E showed good scavenging effects against DPPH radical with IC₅₀ of 39 μM.     

Biologically active components of a Papua New Guinea analgesic and anti-inflammatory lichen preparation

A traditional preparation of Parmotrema saccatilobum (Taylor) Hale (Family: Parmeliaceae) is being considered for inclusion into the PNG national drug formulary by the Ministry of Health Taskforce on Traditional Medicines. The lichen preparation is traditionally used in the Milne Bay province of Papua New Guinea for analgesic and anti-inflammatory activities. A hexane extract of P. saccatilobum yielded the principle components atranorin and chloroatranorin. Atranorin and chloroatranorin were tested in a COX-1 and -2 enzyme inhibition assay, which showed that atranorin inhibited COX-1 in a dose dependent manner and suggests partial inhibition by atranorin and chloroatranorin of COX-2 and COX-1, respectively.     

Two pregnane derivatives and a quinolone alkaloid from Helicteres angustifolia

Phytochemical investigation of the ethanol extract from roots of Helicteres angustifolia led to the isolation of two new pregnane derivatives, heligenin A–B (1–2), and a new quinolone alkaloid, helicterone A (3), along with thirteen known compounds (4–16). The structures of new compounds were established by analysis of extensive spectroscopic data. The absolute configuration of 1 was determined by application of the modified Mosher's method. All of the isolates were evaluated for their anti-proliferative activities against HT-29 human colon cancer cells and OVCA 429 ovarian cancer cells by MTT assay.     

Antiinflammatory and analgesic activities of Zizyphus lotus root barks

The root barks of Zizyphus lotus were extracted with water, chloroform, ethyl acetate and methanol to determine their antiinflammatory and analgesic activities. Aqueous extract (50, 100 and 200 mg/kg) given intraperitoneally (i.p.) showed a significant and dose-dependent antiinflammatory and analgesic activity.     

Millaurine A, a new guanidine alkaloid from seeds of Millettia laurentii

A new guanidine alkaloid, millaurine A (1), was isolated from the methanol extract of the seeds of Millettia laurentii. The structure of the new compound was elucidated on the basis of spectral analysis.     

Antinociceptive and anti-inflammatory activities of ethyl acetate fraction from Zanthoxylum armatum in mice

Zanthoxylum armatum DC. is a traditional Chinese medicine that is prescribed to alleviate pain and treat inflammatory disorders. This species is distributed mainly in the southeast and southwest regions of China. In the present study, we found that ethyl acetate fraction of ethanolic extract of Z. armatum could significantly decrease acetic acid-induced writhing numbers, and suppress formalin induced licking times in the first phase at the highest dose and in the second phase at all tested doses. This observation revealed that Z. armatum extract possessed powerful antinociceptive activity. The mechanisms of the antinociceptive effect might be mainly involved in the periphery inflammatory analgesic. In addition, the ethyl acetate fraction also inhibited xylene-induced ear swelling in a dose-dependent manner in mice. Eight lignans [eudesmin, horsfieldin, fargesin, kobusin, sesamin, asarinin, planispine A, and pinoresinol-di-3,3-dimethylallyl] were identified as major components of the ethyl acetate fraction. Considering related studies reporting the anti-inflammatory activity for the identified lignans, lignan might be responsible for its anti-inflammatory activity. Our results confirm that the traditional use of Z. armatum in the treatment of inflammation and pain is warranted.     

The studies of anti-inflammatory and analgesic activities and pharmacokinetics of Oxytropis falcate Bunge extraction after transdermal administration in rats

The aim of this study was to evaluate the activities of anti-inflammatory and analgesic of the total flavonoids extraction from Oxytropis falcate Bunge (FEO) after transdermal administration. The pharmacokinetics and absolute bioavailability of FEO in rat, furthermore, was studied. Firstly, the anti-inflammatory and analgesic effects of the FEO were studied by xylene-induced ear edema, adjuvant-induced joint inflammation law in rats, acetic acid-induced writhing and hot-plate tests in mice. Secondly, we developed a sensitive and specific HPLC method to analyze 2′, 4′-dihydroxychalcone (TFC, the mainly ingredient of FEO) in rat plasma to study the pharmacokinetic of TEC. The results showed FEO has anti-inflammatory and analgesic property in a dose-dependent manner, and that the high dose group (90.6 mg/kg) of FEO appeared more significantly effective than the positive drug. From the pharmacokinetic studies of TFC in rats, we got the main pharmacokinetic parameters of TFC, providing a basis for the future studies in clinic.     

A novel aporphine alkaloid from Magnolia officinalis

A novel aporphine alkaloid, magnofficine (1), has been isolated from the root barks of the Chinese medicinal plant Magnolia officinalis, along with seven known compounds. Elucidations of their structures were achieved by spectroscopic methods. Magnofficine is the first example of an adduct of aporphine alkaloid and 4-hydroxyphenethylamino bridged by a methylene.     

New amide alkaloid from the aerial part of Piper capense L.f. (Piperaceae)

Together with apigenine dimethylether and piperchabamide A, a new amide alkaloid, Kaousine and the Z form of antiepilepsirine were isolated from the aerial part of Piper capense L.f (Piperaceae). Their structures were elucidated by spectrometric methods and their in vitro antiparasitic activities were evaluated on Plasmodium falciparum.     

A new indole alkaloid from Ervatamia yunnanensis

The stems of Ervatamia yunnanensis have afforded a new indole alkaloid, ervataine (1), whose structure was determined by spectroscopic analysis. Five known compounds, ibogaine (2) coronaridine (3), heyneanine (4), voacangine hydroxyindolenine (5) and coronaridine hydroxyindolenine (6), were also isolated.     

In vitro antifungal activities of Allium cepa, Allium sativum and ketoconazole against some pathogenic yeasts and dermatophytes

By using an agar dilution assay, the antifungal activity of aqueous extracts prepared from Allium cepa (onion; AOE) and Allium sativum (garlic; AGE) were evaluated against Malassezia furfur (25 strains), Candida albicans (18 strains), other Candida sp. (12 strains) as well as 35 strains of various dermatophyte species and compared with the activity of a known antifungal drug, ketoconazole (KTZ). All the AOE, AGE and KTZ were found to be able to inhibit growth of all fungi tested in a dose-dependent manner with maximum of 100% at defined concentrations. The results indicate that onion and garlic might be promising in treatment of fungal-associated diseases from important pathogenic genera Candida, Malassezia and the dermatophytes.     

Analgesic, anti-inflammatory, and CNS depressant activities of new constituents of Nepeta clarkei

Two new pentacyclic triterpenes named kirmanoic acid (1) and kurramanoic acid (2) have been isolated from the chloroform-soluble portion of the whole plant of Nepeta clarkei Hook. The structures of the two new compounds were assigned on the basis of their 1H and 13C NMR spectra including two-dimensional NMR techniques such as COSY, HMQC, and HMBC experiments. Kirmanoic acid (1) was investigated for analgesic, anti-inflammatory, and CNS depressant activities. Interestingly kirmanoic acid (1) showed strong analgesic activity than standard drug in acetic induced writhing and formalin tests. Similarly kirmanoic acid (1) also showed strong anti-inflammatory activity than its standard drug. The gross behavioral study of kirmanoic acid (1) revealed that it exhibited mild CNS stimulant and muscle relaxant in the mice. Compound 1 showed a slight increase in Locomotor activity and possesses the antidepressant effect.     

Antinociceptive and anti-inflammatory activities of iridoid glycosides extract of Lamiophlomis rotata (Benth.) Kudo

Lamiophlomis rotata (Benth.) Kudo is a perennial herb (Labiatae) used as the Tibetan traditional medicine with the effects of alleviating pain, detumescence, hemostasis, promoting blood circulation to remove blood stasis and reinforcing marrow. In this study, we investigated the antinociceptive and anti-inflammatory activities of iridoid glycosides extract of L. rotata (IGLR) in mice. Our results showed that the iridoid glycosides extract could decrease acetic-acid-induced writhings times and formalin-induced lickings times, inhibit carrageenan-induced hind paw edema and xylene-induced ear swelling, and suppress peritoneal capillary permeability and leukocyte infiltration also induced by acetic acid in mice. All of these results suggested that the iridoid glycosides extract possesses the significant antinociceptive and anti-inflammatory activities.     

Anthelmintic activities of three medicinal plants from Nigeria

Aqueous extracts of the leaf, stem bark and root bark from Canna bidentata, Spondias mombin and Commiphora africana were examined for anthelmintic activity against earthworm. All the extracts demonstrated a concentration-dependent activity at tested concentrations of 10-80 mg/ml. Higher activities were observed at the higher concentrations, 40-80 mg/ml for all the plant extracts. C. bidentata with a paralysis time of 3-5 min and death time of 5-18 min at these concentrations for the stem bark, and S. mombin which exhibited comparatively higher efficacy (34-44 min paralysis time and 105 min death time for the leaf) at lower concentrations of 10-20 mg/ml were adjudged the outstanding anthelmintics of plant origin accordingly.     

New isocoumarins and alkaloid from Chinese insect medicine, Eupolyphaga sinensis Walker

Two new isocoumarins (1 and 2), a new alkaloid (3), and a known N-acetyldopamine dimer (4) were isolated from the ethyl acetate extract of Chinese insect medicine Eupolyphaga sinensis. Their structures were elucidated on the basis of detailed spectroscopic investigations, such as 1D- and 2D NMR spectroscopy, as well as by means of HR-MS. The structure of 1 was firmly confirmed by X-ray crystallography, and the absolute configuration was revealed by experimental and computational optical rotation analyses. Cytotoxicities of 1-4 were measured in vitro against 10 selected cancer cell lines.     

Investigation of in vitro anthelmintic activities of Pycnanthus angolensis and Sphenocentrum jollyanum

Extracts from Pycnanthus angolensis stem bark, and fruits and seeds of Sphenocentrum jollyanum, when tested in vitro, showed potent anthelmintic activity on the earthworm, Eudrilus eugeniae. Methanolic extract of P. angolensis was more active than its chloroform extract (P<0.001), while fruit ethanolic extract of S. jollyanum was also more potent than the seed extract. When compared with other worms, S. jollyanum fruit extract showed the greatest activity on wireworms when tested at 80 mg/ml.     

Determination of chemical profile, antioxidant, DNA damage protection and antiamoebic activities of Teucrium polium and Stachys iberica

This work deals with the evaluation of in vitro antioxidant, DNA preventing and antiamoebic activities of the water extracts of Teucrium polium and Stachys iberica. In all systems, T. polium extract exhibited excellent activity potential than that of S. iberica. The amount of total phenolics and flavonoids were high in this extract. In the presence of 40 mg/ml T. polium extract, a significant protection was observed for native super coiled DNA of pBR322 plasmid DNA. In the presence of 32 mg/ml of T. polium extract, no trophozoite was after the 24th hour.     

Evaluation of analgesic, anti-inflammatory and hepatoprotective effects of lycorine from Sternbergia fisheriana (Herbert) Rupr

The present study reports the potential antinociceptive, anti-inflammatory and hepatoprotective activities of lycorine from Sternbergia fischeriana (Herbert) Rupr. (Amaryllidaceae). Lycorine was evaluated on mice by using acetic-acid induced writhing and tail-flick tests. Lycorine exhibited stronger inhibition than aspirin in acetic-acid induced abdominal stretching at 1.0 mg/kg dose. Lycorine also showed antinociceptive activity at 1.0 mg/kg dose in tail-flick test. The anti-inflammatory activity of lycorine was not found to be significant at dose of 0.5 mg/kg. However, at doses of 1.0 mg/kg and 1.5 mg/kg, i.p. showed a significant reduction with 53.45% and 36.42%, respectively in rat paw oedema induced by carrageenan against the reference anti-inflammatory drug indomethacin (3 mg/kg, i.p.) (95.70%). The ED₅₀ of lycorine was determined as 0.514 mg/kg. Hepatoprotective activity of lycorine on carbon tetrachloride (CCl₄) induced acute liver toxicity following biochemical parameters were also evaluated. Rats were treated with lycorine at doses of 1.0 mg/kg and 2.0 mg/kg, i.p. Results of biochemical tests were confirmed by histopathological examination. Lycorine exhibited significant hepatoprotective effect at dose of 2.0 mg/kg i.p. dose.     

油茶树体对氮磷钾元素年吸收和积累规律的研究

以5年生油茶为试材,研究了树体对大量矿质元素氮、磷、钾元素的年吸收和积累规律。结果表明:油茶年发育周期中对氮、磷、钾元素的吸收量分别为44.05、5.50、23.31 g.株-1,吸收比例约为8∶1∶4。抽梢期(4月)至果实发育期(7月)是油茶吸收氮、钾元素的活跃时期,该段时期内的积累量超过了年积累量的50.00%,其中的氮、钾元素分别有43.64%和26.97%被根系所利用;植株对磷元素的积累量在4月至10月没有明显的起伏,从果实发育期(7月)至成熟期(10月)这段时间内,植株磷元素的积累量达到2.63 g,其中35.36%保留在根系中。油茶叶片、枝干和根系中氮、磷、钾元素含量高低顺序为氮>钾>磷,成熟果实中为钾>氮>磷;在新梢期(4月),根系中的磷、钾元素向叶片和新梢进行了部分转运,而在果实膨大、成熟期,钾元素从枝干和叶片转运至果实中。