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Anticonvulsant activity of aqueous extract of Leonotis leonurus.

Water extract of Leonotis leonurus was tested for anticonvulsant activity against seizures produced in mice by pentylenetetrazole, picrotoxin, bicuculline and N-methyl-DL-aspartic acid (intraperitoneal injections). L. leonurus extract in the doses of 200 and 400 mg/kg respectively protected 37.5% and 50% of animals used and significantly (p < 0.05; Student's t-test) delayed pentylenetetrazole (90 mg/kg)-induced tonic seizures. Similarly, the same doses of L. leonurus extract significantly (p < 0.05; Student's t-test) delayed the onset of tonic seizures produced by picrotoxin (8 mg/kg) and N-methyl-DL-aspartic acid (400 mg/kg). However, all the doses of aqueous extract of L leonurus used did not alter the seizures induced by bicuculline (20 mg/kg) to any significant extent. The data suggest that the extract of L. leonurus has anticonvulsant activity and may probably be acting through non-specific mechanisms, since it affects both gabaergic and glutaminergic systems. High performance liquid chromatography (HPLC) and phytochemical tests carried out respectively show a spectrum profile, characteristic of L. leonurus and the presence of alkaloids, saponins and tannins in the extract.

Animals↗

New labdane-type diterpenoids from Leonurus heterophyllus SW.

Five new natural labdane-type diterpenoids (5-9), designated leoheteronins A-E, together with four known diterpenoids (1-4), two phytosterols as a mixture of beta-sitosterol and stigmasterol, and the flavone genkwanin (10) were isolated from the aerial parts of Leonurus heterophyllus SW. (Lamiaceae) collected in northern Vietnam. Compound 1 was isolated for the first time from a Leonurus species, and 10 is considered to be a chemotaxonomic marker of the Leonurus genus. Their structures were determined using spectroscopic analyses.

Chromatography, High Pressure Liquid↗

Antinociceptive, antiinflammatory and antidiabetic effects of Leonotis leonurus (L.) R. BR. [Lamiaceae] leaf aqueous extract in mice and rats.

The present study was undertaken to investigate the antinociceptive, antiinflammatory, and antidiabetic properties of the aqueous leaf extract of Leonotis leonurus (L.) R. BR. (Lamiaceae) in mice and rats, to scientifically appraise some of the plant's ethnomedical uses, and its safety and efficacy. The leaf powder of the plant was Soxhlet extracted with distilled water and used. The antinociceptive effect of the plant's extract was evaluated by the "hot-plate" and "acetic acid" test models of pain in mice, while the antiinflammatory and antidiabetic effects of the leaf extract were investigated in rats, using fresh egg albumin-induced paw edema, and streptozotocin (STZ)-induced diabetes mellitus, respectively. Morphine (MPN, 10 mg/kg i.p.), diclofenac (DIC, 100 mg/kg i.p.), and chlorpropamide (250 mg/kg p.o.) were used, respectively, as reference analgesic, antiinflammatory, and hypoglycemic agents for comparison. L. leonurus leaf aqueous extract (LLE, 50-800 mg/kg i.p.) produced dose-dependent and significant (p < 0.05-0.001) antinociceptive effects against thermally and chemically induced nociceptive pain stimuli in mice. LLE (50-800 mg/kg i.p.) also significantly (p < 0.05-0.001) inhibited fresh egg albumin-induced paw edema, and caused significant (p < 0.05-0.001) hypoglycemic effects in rats. It is suggested that the analgesic effects of LLE (50-800 mg/kg i.p.) may be peripherally and centrally mediated. The different flavonoids, diterpenoids, polyphenolics, and other chemical constituents of the plant may be involved in the observed antinociceptive, antiinflammatory, and antidiabetic effects of the plant's extract. However, the results of this experimental animal study suggest that the aqueous leaf extract of L. leonurus possesses antinociceptive, antiinflammatory, and hypoglycemic properties, and thus lend pharmacological credence to the suggested folkloric uses of the herb in the management and/or control of painful, arthritic, and other inflammatory conditions, as well as for adult-onset, type-2 diabetes mellitus in some communities of South Africa.

Acetic Acid↗

[Nuclear ribosomal DNA internal transcribed spacer 1 sequences of 4 Leonurus species].

OBJECTIVE: To analyze the nuclear ribosome DNA (nrDNA) internal transcribed spacer (ITS) sequences of 4 Leonurus species, and the possibility of using them for molecular authentication of the crude drugs from the genus. METHODS: The nrDNA ITS sequence (including ITS1, 5.8S rDNA, ITS2, and partial 18S rDNA and 26S rDNA) of L. japonicus and its 3 adulterant species were amplified and sequenced, and CLUSTRAL X and MEGA software was employed for analysis. RESULTS: The variation of ITS1 and ITS2 between L. japonicus and its adulterant species ranged between 7.2% and 18.8% and between 14.2% and 27%, respectively. The phylogenic tree derived from the dendrograms based on the ITS sequence data contained some discrepancy from the traditional classification. CONCLUSION: The nrDNA ITS sequences can be used potentially as efficient markers for identification of L. japonicus and its adulterants, and further study is needed for studying the phylogeny of Leonurus.

DNA, Plant↗

Isolation of the uterotonic principle from Leonurus artemisia, the Chinese motherwort.

A search in ancient Chinese medicinal literature and modern phytochemical references indicates that the therapeutic value of Leonurus artemisia (I-mu ts'ao, the Chinese motherwort) might reside in a uterotonic principle present in leaves. Leonurine (4-guanidino-n-butyl syringate) was isolated from fresh and dry leaves of Leonurus artemisia. The uterotonic effect of leonurine was demonstrated in rat uterus in vitro. Results from this study suggest that functional phytochemistry based on ethnobotanical experience could lead to development of new and effective drugs from Chinese medicine.

China↗

Analgesic and anti-inflammatory activity of Leonurus sibiricus.

The methanolic extract of Leonurus sibiricus aerial parts injected intraperitoneally at dose of 250 and 500 mg/kg showed a significant analgesic effect in acetic acid-induced writhing in mice. Moreover, when given orally to rats at dose of 200 and 400 mg/kg, it showed a significant anti-inflammatory activity against carrageenin induced rat paw edema in rats.

Animals↗

Antibacterial activity of Leonurus sibiricus aerial parts.

Different solvent extracts (carbon tetrachloride, chloroform, acetone and methanol) of Leonurus sibiricus were studied for their antibacterial activity. Carbon tetrachloride and chloroform extracts showed a broad spectrum of antibacterial activity.

Anti-Bacterial Agents↗

Isolation and characterization of a novel thermostable non-specific lipid transfer protein-like antimicrobial protein from motherwort (Leonurus japonicus Houtt) seeds.

In screening for potent antimicrobial proteins from plant seeds, a novel heat-stable antimicrobial protein, designated LJAMP2, was purified from seeds of the motherwort (Leonurus japonicus Houtt), a medicine herb, with a procedure involving cation exchange chromatography on a CM FF column, and reverse phase HPLCs on C8 column and C18 column. LJAMP2 exhibited a molecular mass of 6.2 kDa determined. Automated Edman degradation determined the partial N-terminal sequence of LJAMP2 to be NH2-AIGCNTVASKMAPCLPYVTGKGPLGGCCGGVKGLIDAARTTPDRQAVCNCLKTLAKSYSG, which displays homology with plant non-specific lipid transfer proteins (nsLTPs). In vitro bioassays showed that LJAMP2 inhibits the growth of a variety of microbes, including filamentous fungi, bacteria and yeast. The growth of three phytopathogenic fungi, Alternaria brassicae, Botrytis maydis, and Rhizoctonia cerealis, are inhibited at 7.5 microM of LJAMP2, whereas Bacillus subtilis is about 15 microM. The IC(50) of LJAMP2 for Aspergillus niger, B. maydis, Fusarium oxysporum, Penicillium digitatum and Saccharomyces cerevisiae are 5.5, 6.1, 9.3, 40.0, and 76.0 microM, respectively.

Amino Acid Sequence↗

Labdane diterpenes from Leonurus japonicus leaves.

Three labdane diterpenes 15,16-epoxy-6-hydroxylabda-5,8,13(16),14-tretraen-7-one (leojaponin), (9alpha,13S);15,16-diepoxy-7beta-hydroxylabd-14-en-6-one (13-epi-preleoheterin), and (9alpha,13R);15,16-diepoxy-6beta-hydroxylabd-14-en-7-one (iso-preleoheterin) were isolated from the leaves of Leonurus japonicus, in addition to the previously reported preleoheterin. The structure elucidations were made based on analysis of their spectroscopic data.

Diterpenes↗

Labdane diterpenes of Leonurus sibiricus.

Seven new labdane diterpenes, sibiricinones A-E (1-4, 6) and 15-epi-sibiricinones D and E (5 and 7), and the flavone genkwanin were isolated from the aerial parts of Leonurus sibiricus. Sibiricinone D (4) and 15-epi-sibiricinone D (5), and sibiricinone E (6) and 15-epi-sibiricinone E (7), respectively, were isolated as C-15 epimeric pairs. These secondary metabolites were identified on the basis of 1D and 2D NMR including (1)H-(1)H COSY, HSQC, and HMBC spectroscopic techniques. The stereochemical configurations of compounds 4-7 were assigned through 2D T-ROESY and selective NOE experiments.

Barbados↗

A new flavonoside from Leonurus heterophyllus.

In a chemical investigation on the flavone composition of Leonurus heterophyllus a new flavonoside has been isolated. By means of physico-chemical evidences and spectral analysis its structure has been established as quercetin-3-O-[3-(4-hydroxy-3,5-dimethoxybenzyl)-alpha-L-rhamnopyranosyl]-(1-->6)-beta-D-galactopyranoside (1).

Flavones↗

A new labdane diterpene from Leonurus heterophyllus.

A new labdane diterpene, heteronone B (1), together with a known labdane diterpene, heteronone A (2), have been isolated from the aerial part of Leonurus heterophyllus. Their structures were established mainly by 1D and 2D NMR analysis and the stereochemistry of 2 was confirmed by single-crystal X-ray diffraction analysis.

China↗

In vitro anticancer activities of Leonurus heterophyllus sweet (Chinese motherwort herb).

OBJECTIVES: To investigate the anticancer activities of Chinese motherwort herb (Leonurus heterophyllus Sweet; LHS). DESIGN: Dried LHS was extracted and reconstituted in phosphate-buffered saline. The in vitro antiproliferation activities of the extract were tested against seven human cancer cell lines. The DNA ladder assay and cell morphologic studies were performed to verify the drug's apoptotic activities. The possible pathway by which LHS induced apoptosis was also explored by examining mitochondrial depolarization, cytochrome c release, and caspase-3 activation. RESULTS: The LHS extract was effective in inhibiting the growth of all seven cancer cell lines tested. The IC(50) (50% inhibition concentrations, milligrams of raw material per milliliter) were in the range of 8.0-40.0 when the drug exposure time was 48 hours. The inhibitory action of the herbal extract was time- and dose-dependent. A significant decrease in activity was seen when the drug exposure time was shortened. Microscopic examination of the LN CaP and other cancer cell lines after treatment with LHS revealed morphologic changes that are typical of cells undergoing apoptosis. DNA fragmentation was obvious in the DNA latter assay and this confirmed the induction of apoptosis of the cancer cells by LHS. The mitochondria of the LHS-treated cells were found to undergo depolarization. Cytochrome c was released into the cytosol from the LHS-treated cells but not from the control cells. Cells treated with LHS showed cleavage of the full-length poly[ADP(ribose)] polymerase (PARP; 112 kd) to generate the 85-kd cleaved PARP fragment indicating the activation of caspase-3. CONCLUSIONS: LHS was able to induce apoptosis of all the tumor cell lines tested. The antiproliferation effect was dose- and time-dependent. The mitochondrion was found to be involved in the apoptosis induced by the LHS extract.

Antineoplastic Agents, Phytogenic↗

Expression of a novel small antimicrobial protein from the seeds of motherwort (Leonurus japonicus) confers disease resistance in tobacco.

Medicinal plants are valuable resources of natural antimicrobial materials. A novel small protein with antimicrobial activities, designated LJAMP1, was purified from the seeds of a medicinal herb, motherwort (Leonurus japonicus Houtt). LJAMP1 is a heat-stable protein with a molecular mass of 7.8 kDa and a determined isoelectric point of 8.2. In vitro assays showed that LJAMP1 inhibits the growth of an array of fungi and bacteria. The hyphal growth inhibition by LJAMP1 was more evident against hyphomycete fungi, such as Alternaria alternata, Cercospora personata, and Aspergillus niger. The N-terminal amino acid sequence of LJAMP1 was determined, and its coding gene was consequently cloned by the rapid amplification of cDNA ends. The gene LJAMP1 has no intron and encodes a polypeptide of 95 amino acids, in which the first 27 residues was deduced as a signal peptide. The mature LJAMP1 shows relatively low identity to plant napin-like storage proteins. Northern blot assays revealed that LJAMP1 is expressed preferentially in seeds. Bioassays in transgenic tobacco demonstrated that that overexpression of LJAMP1 significantly enhanced the resistance of tobacco against not only the fungal pathogen A. alternata but also the bacterial pathogen Ralstonia solanacearum, while no visible alteration in plant growth and development was observed.

Amino Acid Sequence↗

Studies on the constituents of Leonurus sibiricus L.

Two new furanoditerpene-lactones, LS-1 (1) and LS-2 (2), were isolated along with four known furanoditerpene-lactones 3, 4, 5 and 6 from the aerial part of Leonurus sibiricus L. The structures of the new compounds were determined by spectroscopic means. Compounds 1-6 isolated here exhibited moderate cytotoxic activity (IC(50)=50-60 microg/ml) against leukemia cells (L 1210) in tissue culture.

Leonurus↗

New bis-spirolabdane-type diterpenoids from Leonurus heterophyllus Sw.

Twelve natural bis-spirolabdane-type diterpenoids, including eight new, named leoheteronones A-E, 15-epileoheteronones B, D, and E, and four known leopersin B, 15-epileopersin B, leopersin C, and 15-epileopersin C, together with hispanone and galeopsin were isolated from the aerial parts of the medicinal plant Leonurus heterophyllus SW. (Lamiaceae) grown in Vietnam. Their structures were determined by spectroscopic analyses. The current study emphasized the accumulation of C-15 oxygenated bis-spirolabdane-type diterpenoids of both 13R and 13S configurations in L. heterophyllus.

Chromatography, Thin Layer↗

[Identification on crude drugs from genus Leonurus: II. Leaf and flower surface characters].

OBJECTIVE: To identify the crude drugs originated from 9 species and 1 variety of genus Leonurus (called Yimucao) through leaf and flower surface characters. METHOD: Routine slide processing and the characters under microscope were observed and compared. RESULTS: Obvious characteristics for identification were revealed. CONCLUSION: The shape and length of non-glandular hairs are useful in identifying this sort of crude drugs. Leaf constants and cluster crystals are also useful as reference. However, pollen grains and secretory tissues are worthless.

Leonurus↗

[Regulation on growth and accumulation of total alkaloid in Leonurus artemisia (Lour.)S.Y. Hu by various microfertilizers].

OBJECTIVE: To trace the effects of various microfertilizers on the growth and accumulation of total alkaloid in Leonurus artemisia. METHOD: The total alkaloid was determined by spectrophotometry. RESULT: Microfertilizers of different concentrations could facilitate the growth of L. artemisia in various degrees and Mn-fertilizer of standard concentration and Cu-fertilizer of excessive concentration could help raise the output of the plant markedly by up to 43.6% and 55.2% respectively. Microfertilizers of different concentrations could improve the content of total alkaloid in L. artemisia: Mn-fertilizer of standard concentration and B-fertilizer of excessive concentration could enhance the contents of total alkaloid up to 2.15% and 2.09% respectively. Mn-fertilizer and Cu-fertilizer of standard concentration have been proved very useful in improving the resistibility and ability of the plant to survive summer safely, and Fe-fertilizer of standard concentration could bring the plant an obvious increase of output after surviving summer. CONCLUSION: Application of Mn-fertilizer of standard concentration is very important for cultivating L. artemisia of excellent quality and high output.

Alkaloids↗