狮耳花的药学研究进展

王晓玲，袁绿益

(西南民族大学药学院，四川 成都 610041)

狮耳花的药学研究进展

王晓玲，袁绿益

(西南民族大学药学院，四川 成都 610041)

目的综合报道狮耳花在植物学，药理学，植物化学，生物活性，毒理学及其商业方面的研究.方法对1900年～2015年的文献进行广泛查阅，包括电子数据库Scopus，SciFinder，Pubmed，Google Scholar中的摘要，全文文章和相关书籍.结果狮耳花中主要含萜类化合物，尤其是半日花烷型二萜类.还有很多化学成分被认为并非来自狮耳花，比如，具有轻度神经兴奋性的益母草碱，从未出现在狮耳花提取物中.结论尽管对狮耳花的研究和应用已有很多报道，但是仍需要对该植物中的未知成分进行深入研究，尤其对有神经性作用的相关成分进行系统分离和鉴定，具有重要的学术价值.

狮耳花；半日花烷型二萜类；药理活性

狮耳花Leonotis leonurus(L.)R.Br.系唇形科狮耳花属常绿灌木，浅棕色方茎，全株密被柔毛，幼株茎纤细，灰绿色.单叶对生，叶片纸质或亚革质，通常镰状椭圆形，有时为长圆状披针形或倒披针形，具粗锯齿，表面绿色，背面淡绿色，气味刺鼻，花丛生于茎上部叶腋处，长40至70毫米，花序柄圆柱形，花萼12到16毫米长，直径4毫米，筒状花冠40至49毫米长，橙色并且覆盖橙色毛[1-2].

狮耳花的名字起源于希腊文，“leon”译为狮子，“otis”译为耳朵，并因其花瓣长得像狮子的耳朵，故取名为狮耳花(如图1)[3].

图1 狮耳花Fig.1 Leonotis leonurus

2 民间应用

2.1 人类疾病治疗

狮耳花，俗称野生大麻，同时具有药用价值和神经兴奋作用，广泛用于如痔疮、湿疹、皮疹、疖子、瘙痒、肌肉痉挛、头痛，癫痫，胸部感染，便秘，蜘蛛和蛇咬伤的治疗[4].详细的用药过程是取一汤匙切碎的干叶子(约10g)，加入三杯开水煎煮10分钟，冷却一夜，过滤后清洗伤口[5].煎煮后的狮耳花还可以作为治疗咳嗽，感冒和支气管炎的口服药.狮耳花的粉末可做成药膏，局部使用可缓解眼部疼痛[6].狮耳花干粉或种子煎煮后可作为缓解痔核的口服药物，局部使用可缓解头部和腿部溃烂.根据Watt和Breyer-Brandwijk报道，狮耳花叶煎煮后可用作泻药和调经剂[7].狮耳花的茎、叶和花通过煎煮或吸食可治疗普通感冒、癫痫、麻风、高血压[8].

狮耳花的叶和花在非洲南部常用于治疗胸部感染、流感、发烧、痢疾、便秘、头痛、癫痫、蜘蛛和蛇咬伤、月经推迟、肠道蠕虫、高血压、蝎子刺[6，9-12].在治疗蛇咬伤时，经常将狮耳花的根部与其他植物混合使用，如狮耳花与马钱子刺混合，趁热口服作催吐剂[9].在南非，祖鲁人用热水浸泡后的茎和叶子治疗咳嗽和感冒，用冷水浸泡后的叶子冲洗鼻腔来缓解高烧引起的头痛.浸泡后的叶子还被报道可治疗哮喘和缓解病毒性肝炎[7].Maroyi在2013年发表的对津巴布韦中南部地区传统药用植物综述中表明，咀嚼吞咽狮耳花的叶可治疗溃疡[12].吸食狮耳花的叶和花可治疗癫痫和局部麻痹[7，11].狮耳花叶经常被用作薄荷茶杯冲泡使用，有助于利尿和治疗肥胖[6-7，11].狮耳花的民间应用详见表1.

除了表1中的民间应用外，狮耳花由于具有神经兴奋活性还可以用作商品销售[6，11].据报道，吸食狮耳花的干燥花、叶具有减轻癫痫的作用，吸食过程中会产生一种类似大麻的作用，不过十分轻微[20].

2.2 传统兽药应用

在许多发展中国家，畜牧农民经常使用本地植物来治疗患病牲畜[21].草药对动物的常见疾病，如轻度腹泻、肠道寄生虫、伤口和皮肤感染都有很好的疗效，而且价廉易得，是农民的首选方法.Masika和Afolayan等人发现，狮耳花叶的汁液滴入动物的眼睛可治疗眼部炎症[15-17].捣碎的根和叶添加于家禽的饮用水中可以预防疾病，治疗牛边虫病[18].狮耳花也可以用来防止牲畜蠕虫感染[19]，其水提物可以有效预防山羊胃肠道寄生虫.

2.3 娱乐性使用

在21世纪初，许多草药在互联网上被宣传为大麻的合法代替品[22].狮耳花就是其中的一种，其他如埃及蓝睡莲，透纳树叶.虽然这些都自称是“纯”草药产品，但在2008年发现它们被掺入合成大麻类化合物.这些芳香植物实质是作为帮助合成大麻类产品销售的“绿色飞机”，这种做法会严重危害到公众的健康[23].

表1 狮耳草的民间应用Table 1 Traditional uses，preparation and mode of administration of Leonotis leonurus

3 化学成分

狮耳花中提取到的主要化合物有单萜类，倍半萜类和半日花烷型二萜类化合物[24～34]，见图2.

图2 狮耳花半日花烷型二萜类化合物基本结构Fig.2 General structure of labdane diterpene

以半日花烷型为母核的二萜类化合物见表2，除二萜类化合物的其它化合物见表3.

表2 狮耳花半日花烷型二萜类化合物Table 2 Labdane diterpenoids from Leonotis leonurus

表3 狮耳花中的杂环化合物(除二萜类化合物)Table 3 Miscellaneous compounds，other than diterpenes，from Leonotis leonurus

4 药理活性

狮耳花具有多方面的药理活性，如抗惊厥、抗菌、抗感染、抗疟、抗氧化、抗HIV等，狮耳花化学成分的药理活性见表2和3.

5 总结

虽然关于狮耳花的化学成分及药理活性已有大量报道，但是有很多成分仍需要权威的研究和阐明，包括狮耳花中的生物碱和精油，以及其它部位化学成分，比如传统医药学中广泛研究的根部.研究已证明狮耳花的粗提物中具有神经性作用，所以对具有神经性作用的成分进行分离和鉴定就显得尤为重要.在南非，狮耳花作为传统民间草药被广泛使用，如果要为患者提供安全有效的产品，尚需在质量控制方面做大量的工作.

[1]IWARSSON M，HARVEY Y.Monograph of the genus Leonotis[J].Kew Bulletin，2003，58:597-645.

[2]HURINANTHAN V.Immune Modulatory Effect of Dichrostachys cinerea，Carpobrotus dimidiatus，Capparis tomentosa and Leonotis leonurus [D].Durban:Durban University of Technology，2009.

[3]BAUDRY N N，GILL E，ALVARO V.“Wild cannabis”:A review of the traditional use and phytochemistry of Leonotis leonurus[J].Journal of Ethnopharmacology，2015，174:520-539.

[4]SCOTT G，SPRINGELD E P，COLDREY N.A pharmacognostical study of 26 South African plant species used as traditional medicines[J]. Pharmaceutical Biology，2004，42:186-213.

[5]MUGABO P，KHAN F，BURGER A.Effect of Leonotis leonurus aqueous extract on the isolated perfused rat heart[J].Journal of Medicinal and Aromatic Plant Sciences，2012，Plants 2:281-292.

[6]HUTCHINGS A，SCOTT A H，LEWIS G，et al.An Inventory[M].Natal，South Africa:University of Natal Press，1996:266-267.

[7]WATT J M，BREYER-BR，WIJK B N.Medicinal and poisonous plantsof Southern and Eastern Africa[M].2nd ed.Churchill Livingstone，Edinburgh，1962:514-520.

[8]DUKE J A.Handbook of medicinal herbs[M].2nd ed.London，New York，Washington D C，Boca Raton:CRC press，2001.

[9]BRYANT A T.Zulu medicine and medicine Men[M].Struik，Cape Town，1909.

[10]JÄGER A K，HUTCHINGS A，VAN STADEN J.Screening of Zulu medicinal plants for prostagladin-synthesis inhibitors[J].Journal of Ethnopharmacology，1996，52:95-100.

[11]VAN WYK B E，VAN OUDSHOORN B，GERICKE，N.Medicinal Plants of South Africa[M].2nd edition.Briza Publications Pretoria，South Africa，2000.

[12]STAFFORD G I，PEDERSEN M E，VAN STADEN J，et al.Review on plants with CNS effects used in traditional South African medicine against mental diseases[J].Journal of Ethnopharmacology，2008，119: 513-537.

[13]MAROYI A.Traditional use of medicinal plants in south-central Zimbabwe:review and perspectives[J].Journal of Ethnobiology and Ethnomedicine，2013，9:31.

[14]MABONA U，VAN VUUREN S F.South African medicinal plants used to treat skin diseases.S.Afr[J].Pakistan Journal of Botany，2013，87: 175-193.

[15]MASIKA P J，SONANDI A，et al.Perceived causes，diagnosis and treatment of babesiosis and anaplasmosis in cattle by livestock farmers in communal areas of the central Eastern Cape Province，South Africa [J].Journal of the South African Veterinary Association，1997，68:40-44.

[16]MASIKA P J，VAN AVERBEEKE W，SONANDI A.Use of herbal remedies by smallscale farmers to treat livestock diseases in central Eastren Cape province，South Africa[J].Journal of the South African Veterinary Association，2000，71:87-91.

[17]MASIKA P J，AFOLAYAN A J.An ethnobotanical study of plants used for thetreatment of livestock diseases in the Eastern Cape Province，South Africa[J].Pharmaceutical Biology，2003，41:16-21.

[18]HULME M M.Wild Flowers of Natal[M].Shuter＆Shooter，Pietermaritzburg，1954.

[19]MAPHOSA V，MASIKA P J.In vivo validation of Aloe ferox(Mill) .Elephantorrhiza elephantina Bruch.Skeels.and Leonotis leonurus(L) R.Br as potential anthelmintics and antiprotozoals against mixed infections of gastrointestinal nematodes in goats[J].Parasitology Research，2011，110:103-108.

[20]WU H，LI J，FRONCZEK F R，et al.Labdane diterpenoids from Leonurus leonurus[J].Phytochemstry，2013，91:229-235.

[21]MCGAW L.J，ELOFF J N.Ethnoveterinary use of Southern African plants andscientific evaluation of their medicinal properties[J].Journal of Ethnopharmacology，2008，119:559-574.

[22]ZUBA D，GEPPERT B，SEKULA K，et al.[1-(Tetrahydropyran-4-ylmethyl)-1H-indol-30yl]-(2，2，3，3，-tetramethylcyclopropyl)methanone:a new synthetic cannabinoid identified on the drug market[J]. Forensic Toxicology，2013，31:281-291.

[23]CORNARA L，BORGHESI B，CANALI C，et al.Smart drugs:green shuttle or real drug[J].Journal of Legal Medicine，2013，127:1109-1123.

[24]DEMETZOS C，DIMAS S.Labdane-type diterpenes:chemistry and biological activity[J].Studies in Natural Products Chemistry，2001，35: 235-292.

[25]PURUSHOTHAMAN K K，VASANTH S.Chemical studies on Leonotis–a review[J].Indian Drugs，1988，25:484-491.

[26]PEDRO L G，BARROSO J G，MARQUES N T，et al.Composition of the essential oil from sepals of Leonotis leonurus R Br J Essent[J]. Journal of Essential Oil Research，1991，3:451-453.

[27]CRAGG G M L，LITTLE G E.The extractives of Leonotis leonurus [J].South African Journal of Chemistry，1962，15:29-30.

[28]RIVETT D E A.Isolation of marrubiin from Leonotis leonurus[J]. Chemical Society，1964:1857-1858.

[29]KAPLAN E R，RIVETT D E A.Structures of compounds X and Y，two labdane diterpenoids，from Leonotis leonurus[J].Chemical Society，1968:262-266.

[30]LAONIGRO G，LANZETTA R，PARRILLI M，et al.The conguration of the diterpene spiroethers from Marrubium vulgare and from Leonotis leonurus[J].Gazzella Chimica，1979，109:145-150.

[31]KRUGER G J，RIVETT D E A.Diterpenoids of Leonotis species.Part 7.The crystal and molecular structure of compound X a labdane from Leonotis leonurus[J].South African Journal of Chemistry，1988，41: 124-125.

[32]MCKENZIE J M，GREEN I R，MUGABO P.Leonurun，a novel labdane diterpenoid from Leonotis leonurus[J].South African Journal of Chemistry，2006，59:114-116.

[33]OBIKEZE K C，MCKENZIE J M，GREEN I R，et al.Characterization and cardiovascular effects of(13S)-9α，13α-epoxylabda-6β(19)，15 (14)diol dilactone，a diterpenoid isolated from Leonotis leonurus[J]. South African Journal of Chemistry，2009，61:119-122.

[34]NAIDOO D，MAHARAJ V，CROUCH N R，et al.New labdane-type diterpenoids from Leonotis leonurus support circumscription of Lamiaceae s.l.Biochemstry[J].Biochemical Systematics and Ecology，2011，39:216-219.

[35]BIENVENU E，AMABEOKU G J，EAGLES P K，et al.Anticonvulsant activity of aqueous extract of Leonotis leonurus[J].Journal Phytomedicine，2002，9:217-223.

[36]HE F，LINDQVIST C，HARDING W.Leonurenones A–C:labdane diterpenes from Leonotis leonurus[J].Journal Phytochemdicine，2012，83:168-172.

[37]VON DREELE R B，PETTIT G R，ODE R H，et al.The crystal and molecular structure of the unusual spiro dihydrofuran diterpene，nepe-taefolin[J].Journal of the American Chemical Society，1975，97:6236-6240.

[38]MNONOPI N，LEVENDAL R A，COLEMAN M，et al.The cardioprotectiveeffects of marrubiin，a diterpenoid found in Leonotis leonurus extracts[J].Journal of Ethnopharmacology，2011，138:67-75.

[39]MNONOPI N，LEVENDAL R A，MZILIKAZI N，et al.Marrubiin，a constituent of Leonotis leonurus，alleviates diabetic symptoms[J].Journal Phytomedicin，2012，19:488-493.

[40]POPOOLA K，ELBAGORY M，AMEER F，et al.Marrubiin:a review [J].Molecules，2013，18:9049-9060.

[41]NARUKAWA Y，KOMORI M，NIIMURA A，et al.Two new diterpenoids from Leonotis leonurus R Br[J].Nature Medicine，2015，69:130-134.

[42]CHEN C X，KWAN C Y.Endothelium-independent vasorelaxation by leonurine，a plant alkaloid purified from Chinese motherwort[J].Life Sciences，2001，68:953-960.

[43]KUCHTA K，ORTWEIN J，RAU W，et al.Leonurus japonicus，Leonurus cardiaca，Leonotis leonurus:a novel HPLC study on the occurrenceand content of the pharmacologically active guanidino derivative leonurine[J].Pharmazie，2012，67(12):973-979.

[44]LÓPEZ L..Distribution and biological activities of the avonoid luteolin [J].Medical Chemical，2009，9:31-59.

[45]AGNIHOTRI V K，ELSOHLY H N，SMILLIE T J，et al.Constituents of Leonotis leonurus Flowering tops[J].Phytochemistry Letter，1991，2: 103-105.

[46]EL-ANSARI M A，ABOUTABL E A，FARRAG A R H，et al.Phytochemical and pharmacological studies on Leonotis leonurus[J].Pharmaceutical Biology，1991，47:894-902.

[47]NISHIMURA H，SASAKI H，INAGAKI N，et al.Nine phenethyl alcohol glycosides from Stachys sieboldii[J].Phytochemistry，2001，30: 965-969.

[48]PEDERSEN J A.Distribution and taxonomic im plications of some phenolics in the family Lamiaceae determined by ESR spectroscopy [J].Biochemical Systematics and Ecology，2000，28:229-253.

[49]TADAHIRO T，YUJI N，NORIYASU H.Studies on the constituents of Leonotis nepetifolia[J].Chemical and Pharmaceutical Bulletin，1999，47:284-286.

[50]DE SARRO A，CECCHETTI V，FRAVOLINI V，et al.Effects of novel 6-des uoroquinolones and classic quinolones on pentylenetetrazole-induced seizures in mice.Antimicrob[J].Antimicrobial Agents and Chemotherapy，1999，43:1729-1736.

(责任编辑:李建忠，付强，张阳，罗敏；英文编辑:周序林，郑玉才)

Progress in pharmacieticul research of Leonotis leonurus

WANG Xiao-ling，YUAN lv-yi
(School of Pharmacy，Southwest University for Nationalities，Chengdu 610041，P.R.C.)

Objective To summarize the botanical aspects，ethnopharmacology，phytochemistry，biological activity，toxicity and commercial aspects of L.leonurus.Methods An extensive review of the literature from 1900 to 2015 was carried out.Electronic databases including Scopus，Sci Finder，Pubmed，Google Scholar were used as data sources.All abstracts，full-text articles and books written in English were considered.Result L.leonurus contains mainly terpenoids，particularly labdane diterpenes.Other compounds reported by some authors have been isolated from the plant，including the mildly psychoactive alkaloid.Leonurine has however，never been reported in the extracts of L.leonurus.Conclusion Despite the publication of various papers on L.leonurus，there is still demand for definitive research and clarification of other compounds.Research has proven the psychoactive effects of the crude extract of L.leonurus，but confirmation of the presence of psychoactive compounds，as well as isolation and characterization，is still required.

Leonotis Leonurus；labdane diterpenes；pharmacological activities

R28；R29

A

2095-4271(2016)05-0484-08

10.11920/xnmdzk.2016.05.003

2016-07-25

王晓玲(1969—)，女，汉族，四川资阳人，教授，博士，研究方向:天然药物化学.E-mail:wxl3232＠sina.com

四川省科技厅科技支撑项目(2015SZ0040)