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The structure in cross section of stem and lamina of 9 species and 1 variety from genus Leonurus, whose herb used as Yimu Cao, were reported. Diagnostic characteristics were listed out in a key for identification.
Two new phenylpropanoid glycosides, leonosides A and B, and two known glycosides lavandulifolioside and verbascoside, were isolated from the aerial parts of Leonurus glaucescens. On the basis of chemical and spectral evidence, leonosides A and B were shown to be beta-(3,4-dihydroxyphenyl)-ethyl-O-alpha-L-arabinopyranosyl-(1---- 2)-alpha-L- rhamnopyranosyl-(1----3)-4-O-feruloyl-beta-D-glucopyranoside and beta-(3-hydroxy, 4-methoxyphenyl)-ethyl-O-alpha-L-arabinopyranosyl-(1----2)- alpha-L-rhamnopyranosyl-(1----3)-4-O-feruloyl-beta-D-glucopyranosi de, respectively.
Lavandulifolioside was detected for the first time in Leonurus cardiaca var. vulgaris [Moench] Briquet (Lamiaceae). The isolation was performed from the butanolic extract of the aerial parts and the identification by NMR and MS. The pharmacological properties of lavandulifolioside consist of significant negative chronotropism, prolongation of the P-Q, Q-T intervals and QRS complex, and decrease of blood pressure. Contrary to the butanolic extract lavandulifolioside did not reduce the spontaneous locomotor activity. In conclusion, the pharmacological pattern of lavandulifolioside did not explain the pharmacological effects of L. cardiaca L. alone.
Two new cyclic nonapeptides, cycloleonuripeptide E, cyclo (-Ala-Pro-Ile-Val-Ala-Ala-Phe-Thr-Pro-), and cycloleonuripeptide F, cyclo (-Gly-Tyr-Pro-Leu-Pro-Phe-Tyr-Pro-Pro-), have been isolated from the fruits of Leonurus heterophyllus, and their structures were elucidated by 2D NMR analysis and chemical degradation. Cycloleonuripeptides E (1) and F (2) showed moderate vasorelaxant effects on rat aorta.
Two new iridoid glucosides, 6-O-acetylajugol (1) and 7, 8-epoxy-8-epi-loganic acid (2), together with five known iridoid glucosides, galiridoside (3), ajugoside (4), 10-deoxygeniposidic acid (5), 7-deoxy-8-epi-loganic acid (6), and 8-O-acetylharpagide (7), have been isolated from the aerial parts of Leonurus persicus. Leucosceptoside A (8), eugenyl beta-rutinoside (9), and kaempferol 3-O-glucoside (10) were also isolated. The structures of 1 and 2 were elucidated by extensive 1D- and 2D-NMR spectroscopy and molecular modeling. The structure of 3 was confirmed by single-crystal X-ray diffraction. Antimicrobial activity of compounds (1-10) was also evaluated against a panel of gram-positive and gram-negative bacteria and two strains of fungi.
A predominantly Cad-specific lectin is present in the seeds of Leonurus cardiaca. Extracts of these seeds makes a valuable addition to reagents used in the elucidation of red cell polyagglutinability.
1. Using an in vitro radioligand binding assay for the platelet activating factor (PAF) receptor, we have identified a novel, specific PAF antagonist, prehispanolone, from a Chinese medicinal herb Leonurus heterophyllus. 2. The presence of sodium ions inhibited specific [3H]-PAF binding to rabbit platelet membrane with an IC50 of 5.2 mM, decreased the inhibitory potency of PAF but increased the inhibitory potency of prehispanolone. 3. Prehispanolone and several of its derivatives inhibited the binding of [3H]-PAF to rabbit platelets with potencies closely resembling that of inhibition of PAF-induced aggregation. 4. The integrity of the tetrahydrofuran ring of prehispanolone is critical for its interaction with the PAF receptor. 5. By hydrogenating the dihydrofuran ring and replacing the keto group of prehispanolone with a hydroxyl group, we obtained a compound, LC5507, that is more stable and more active than prehispanolone as a PAF receptor antagonist.
Leonurus hereterophyllus Sweet is a traditional Chinese herbal medicine used to treat menstrual disturbances in woman. A new labdane diterpene, prehispanolone LC-5504, namely 9 alpha, 13R,15,16-diepoxy-labdane-14-en-7-one, had been isolated. The authors studied the synergism of labdane diterpene, prehispanolone LC-5504 and Con A and LPS on T cells and B cells proliferation of BALB/c female mice in vitro. They showed that: (1) proliferation of T cells was demonstrated by administration of LC-5504 of various concentrations together with Con A. This proliferation was 5-8 times stronger than that observed when Con A was used alone. Such effect on T cells was not observed when LC-5504 was used alone. (2) Proliferation of B cells was not observed whether LC-5504 was used alone or together with LPS.
To evaluate further the chemopreventive role of motherwort (Leonurus sibiricus L; MW) in lesions of the mammary gland and uterus of GR/A mice, the effects on these lesions of the adsorbed (MW1) and unadsorbed (MW2) fractions of MW separated by ion-exchange resins were studied. The incidence of palpable mammary tumours was suppressed and their growth was retarded by both MW1 and MW2, between whose effects no apparent difference was seen. However, neither of them showed effects on pregnancy-dependent mammary tumours (PDMT), mammary hyperplastic alveolar nodules (HAN) or uterine adenomyosis, whereas MW promoted PDMT and inhibited HAN and adenomyosis. All these findings indicate the importance of the synergistic action of several components, specified and unspecified, for the full manifestation of the effects of Chinese medicine.
Chronic ingestion of methanol extract of the above-ground part of motherwort (Leonurus sibiricus L) in drinking water at the concentration of 0.5% enhanced the development of both pregnancy-dependent mammary tumours (PDMT) and mammary cancers originated from PDMT. By contrast, the treatment markedly suppressed the development of mammary cancers that originated from hyperplastic alveolar nodules (HAN) associated with the decreased formation of HAN. The incidence of uterine adenomyosis was also inhibited in mice given motherwort. The urinary excretion of allantoin, creatine and creatinine and glucose tolerance were stimulated by motherwort. The cause of discrepancy of the effects of motherwort on mammary cancers due to their origins is not clear at present. However, the stimulation by the agent of the excretion of any carcinogenic factors may at least partly contribute to its inhibition of mammary cancers originating from HAN.
The experimental results indicate that the decoction of Chinese drugs Carthamus tinctorius, Angelica sinensis and Leonurus sibiricus has stimulating action on the uterus of mouse in vitro. The stimulating action of Carthamus tinctorius and Leomurus sibiricus has been found related to stimulating H1-receptor and alpha-adrenergic receptor of uterus, but the action of Angelica sinensis to stimulating H1-receptor of uterus only.
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