Fagaronine,a novel antileukaemic alkaloid

A review is presented about fagaronine, a benzophenanthridine alkaloid responsible for antitumoural activity. Plant source, extraction, biosynthesis, medicinal properties, especially antileukaemic activity, are described.     

石椒草化学成分研究

采用硅胶、ODS、Sephadex LH-20和制备型高效液相等色谱方法对石椒草属植物石椒草Boenninghausenia sessilicarpa全草乙醇提取物的石油醚萃取部位进行分离纯化,同时根据化合物波谱数据对单体化合物进行结构鉴定。从石油醚萃取部位共分离鉴定了15个香豆素类化合物,结构鉴定分别为：欧芹烯酮酚甲醚（1）、九里香素（2）、3-(1,1-二甲基烯丙基)-8-羟基-7-甲氧基香豆素（3）、花椒毒素（4）、异茴芹素（5）、状芸香素（6）、异去甲基呋喃羽叶芸香素（7）、欧前胡素（8）、珊瑚菜内脂（9）、白芷脑素（10）、白当归素（11）、新比克白芷内酯（12）、chalepin(13)、鲁望桔内酯（14）、3-(1,1-二甲基烯丙基)-花椒内酯（15）。化合物1～3、6～10和14～15均首次从石椒草中分离得到。     

酸橙中一个新的香豆素苷

目的：对中药枳实化学成分进行研究。方法：采用色谱技术进行分离，应用波谱技术、化学手段及文献对照方法，对分离得到的化合物进行结构鉴定。结果：自枳实乙醇提取物中分离得到10个化合物，分别为5，7-二羟基香豆素5—O-β-D-吡喃葡萄糖苷(Ⅰ)、3，5-二羟基苯基1-O-β-D-吡喃葡萄糖苷(phlorin，Ⅱ)、新橙皮苷(neohesperidin，Ⅲ)、柚皮苷(naringin，Ⅳ)、异樱花素7-O-β-D-新橙皮糖苷(poncirin，Ⅴ)、红橘素(tageritin，Ⅵ)、柚皮素(naringenin，Ⅶ)、马尔敏(marmin，Ⅷ)、橙皮素7-O-β-D-吡喃葡萄糖苷(hesperetin 7—O-glucoside，Ⅸ)、腺苷(adenosine，Ⅹ)。结论：化合物Ⅰ为新化合物，化合物Ⅱ、Ⅹ为首次从该植物果实中分离得到。     

Antinociceptive,Anti-Inflammatory and Antipyretic Activities of the Leaf Methanol Extract of Ruta Graveolens L. (Rutaceae) in Mice and Rats

Background

Ruta graveolens has been used to treat toothache, earache, rheumatism and fever with little scientific evidence corroborating these uses.

Materials and Methods

The leaf methanol extract of Ruta graveolens was evaluated for antinociceptive activity using the acetic acid writhing and hot-plate tests in mice, also anti-inflammatory and antipyretic activities using the carrageenan-induced oedema and E. coli-induced pyrexia tests in rats, respectively.

Results

R. graveolens (100 mg/kg, i.p.), significantly reduced the number of acetic acid-induced writhes by 54 %. R. graveolens (400 mg/kg, i.p.), significantly delayed the reaction time in mice to thermal stimulation 15, 30, 45, and 60 min after treatment. Combined treatment of the lowest and sub-effective doses of the leaf methanol extract (25 mg/kg, i.p.), and indomethacin (10 mg/kg, i.p.) significantly reduced the number of acetic acid-induced writhes in mice. The leaf methanol extract of R. graveolens (50 – 400 mg/kg, i.p.), significantly reduced carrageenan-induced oedema over the 4 h period of testing. Combined treatment of the lowest doses of R. graveolens (25 mg/kg, i.p.) and indomethacin (2 mg/kg, i.p.) produced a significant reduction in carrageenan-induced oedema over the 4 h period of testing. R. graveolens (100 -400 mg/kg, i.p.) significantly reduced E. coli-induced pyrexia over the 5 h period of testing. Given together, the lowest dose of R. graveolens (25 mg/kg, i.p.) and pentoxifylline (10 mg/kg, i.p.) produced a significant reduction in pyrexia induced by E. coli (50 µg/kg, i.m.) over the 5 h period of measurement. The LD₅₀ value obtained for R. graveolens was greater than 4000mg/kg (p.o), suggesting that the plant species may be safe in or nontoxic to mice.

Conclusion

The data obtained indicate that R. graveolens has antinociceptive, anti-inflammatory and antipyretic activities, justifying the use of the plant species by traditional medicine practitioners in the management and treatment of pain, inflammation and fever.     

Anxiolytic properties of botanical extracts in the chick social separation-stress procedure

RATIONALE: The recent growth in sales of natural products labeled as dietary supplements in the United States has renewed scientific interest in the study of the therapeutic effects of multi-component botanical products. OBJECTIVES: This study sought to determine whether botanical extracts derived from the Rutaceae family, Acori graminei, the Magnoliaceae family, Alchemilla vulgaris and Primula veris, which had previously been identified in bioassays as having potential anxiolytic activity, were active in the chick social separation-stress procedure. METHODS: Eight-day-old chicks received IP injections of test articles 30 min before being tested in the presence of two social companions or in isolation for a 3-min observation period. Dependent measures were: a) latency to adopt a ventral recumbent posture to index sedation, b) number of vocalizations to index separation-distress and c) a composite pain score (comprised of footlift frequency and footlift duration in response to 50 microl of 0.10% formalin injected into the plantar surface of the foot) to index stress-induced analgesia. RESULTS: Proprietal extracts NPS00033 from the Rutaceae plant family and NPS00039 (Relora) from the Magnoliaceae plant family screened positive in this chick model without causing sedation. CONCLUSIONS: These results suggest that botanical extracts Relora and NPS00033 may be useful in modulating anxiety states.     

翼叶九里香叶挥发油化学成分的研究

 目的:对海南三亚产翼叶九里香叶中挥发油成分进行了定性和定量研究。方法:采用水蒸汽蒸馏法提取翼叶九里香叶挥发油;Finnigan MAT 17D 800石英毛细管气相色谱-质谱-计算机联用技术,对化学成分进行分离和鉴定。并通过核对标准谱库,确定化合物名称。结果:共分离鉴定出24个化合物。主要成分为3,4-二乙烯基-3-甲基环己烷(35.686%)、十氢-1,1,7-三甲基-4-甲烯基-1H-环丙[e] (19.668%)、石竹烯(6.707%)、十氢-4α-甲基-1-甲烯基-7-(1-甲乙烯基)萘(3.697%)和1,5-二乙烯基-3-甲基-2-甲乙烯基环己烷(3.554%)等。结论:主要成分3,4-二乙烯基-3-甲基环己烷在本属其它种未见报道。     

Inhibitory effect of oxycoumarins isolated from the Thai medicinal plant <Emphasis Type="Italic">Clausena guillauminii</Emphasis> on the inflammation mediators,iNOS, TNF-α, and COX-2 expression in mouse macrophage RAW 264.7

In the present study, we investigated the inhibitory effect of the known oxycoumarins poncitrin (3), osthol (4), and xanthoxyletin (5), newly isolated from Clausena guillauminii (Rutaceae), together with the known carbazoles heptaphylline (1) and 7-methoxyheptaphylline (2) on inducible-nitric oxide synthase (iNOS) expression induced by lipopolysaccharide (LPS) and the NO generation in RAW 264.7 mouse macrophages. Isolation of active oxycoumarins was guided by Western blot analysis of iNOS protein expression. These oxycoumarins showed an inhibitory effect on iNOS protein expression at 10 μM. Further examination of the inhibitory effects of these compounds on inflammation mediators revealed that the synthesis of nitric oxide (NO) and the protein expression of tumor necrosis factor-α (TNF-α) and cyclooxygenase-2 (COX-2) were inhibited by 5. It was expected that these compounds show anti-inflammatory activities.     

Beneficial effect of the leaves of Murraya koenigii (Linn.) Spreng (Rutaceae) on diabetes-induced renal damage in vivo

Ethnopharmacological relevance

Murraya koenigii (Linn.) Spreng (curry leaf) is widely used as a nephroprotective agent in kidney's infirmities among diabetics by the traditional practitioners in Malaysia. However, the latter role of curry leaf has been grossly under reported and is yet to receive proper scientific evaluation.

Aim of the study

The present study was designed to investigate the beneficial effect of the leaves of Murraya koenigii (Linn.) on diabetes-induced renal damage in vivo with regard to prove its efficacy by local traditional practitioners in the treatment of kidney frailties in diabetics.

Materials and methods

Aqueous (AQ) extract of the leaves of Murraya koenigii (Linn.) was administered to both normal and streptozotocin (STZ) induced diabetic male rats (Sprague-Dawley strain). Animals were divided into six groups (n = 6) and treated with variable dose levels of AQ extract (200 and 400 mg/kg body weight/day) for 30 days. At the end of 30 days, animals were sacrificed, blood was collected, processed and stored at −70 °C for the zestimation of serum urea and creatinine, changes in plasma antioxidant capacity by FRAP assay, and glutathione peroxidase levels, in the normal and STZ-induced diabetic rats. Histological changes of the kidneys of these animals were also evaluated by light microscopy to determine the beneficial effect of the leaves.

Results

Daily oral administration of variable dose levels of the AQ extract for 30 days, produced significant dose dependant decrease in serum urea and creatinine levels (p < 0.001), and marked increase in the levels of plasma antioxidant capacity (p < 0.01) in diabetic treated rats, compared to the control (non-diabetic) subjects. However, the normal treated rats showed minimal variation in these parameters in comparison to normal controls. Histological studies of the kidneys of these animals showed comparable tissue regeneration by the AQ extract.

Conclusion

The results of our study scientifically support the traditional belief for using the leaves of Murraya koenigii (Linn.) as adjuvant, in the treatment of pain disorders related to renal impairments among diabetics.     

中药海桐皮的生药鉴别

报道市售中药海桐皮来源于6种不同植物:豆科植物刺桐Erythrina variegata L.var.orientalis(L.)Merr.,芸香科植物樗叶花椒Zanthoxylum ailanthoides Sieb.et Zucc.,朵椒Z.molle Rehd.,凹头花椒Z.kemsleyanum Makino.,五加科植物刺楸Kalopanax septemlobus(Thunb.)Koidz.和木棉科植物木棉Gossampinus malabarica(DC.)Merr.。对6种树皮的生药性状、组织构造和粉末特征进行了比较鉴定。     

Monoamine oxidase inhibitory coumarins from the aerial parts ofDictamnus albus

The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with IC50 values of 0.7 and 1.7 microM, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B (IC50 0.5 and 0.6 microM, respectively) compared to MAO-A (IC50 1.3 and 34.6 microM, respectively). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.