忍冬之本草學簡介

忍冬藥用歷史久遠，始載於梁 陶弘景名醫別錄^17,20-22，書 云：”今處處皆有，似藤生，凌冬不凋，故名忍冬……，十二月 採，陰乾。可見當時僅用忍冬的莖葉入藥，並非忍冬的花，因忍冬 是在初夏開花，不可能在十二月採，且凌冬不凋，由此可知當時以 帶葉的藤入藥。唐 蘇敬唐本草首次記載忍冬花為花白蕊紫，但均未 有金銀花名稱出現；而宋代蘇軾等所著蘇沉良方裡頭才有對忍冬花 的詳細描述²¹，並首次提出”金銀花”這一名詞及其解釋，書 云：”……四月開花，極芬，香聞數步，初開白色，數日則變黃，

每黃白相間，故名金銀花。”

唐 陳藏器本草拾遺云¹⁷：”忍冬，主熱毒、血痢，濃煎服。北 宋嘉佑補注神農本草仍襲”忍冬”之名。南宋 王玠履鑱岩本草雖然 出現金銀花這一名詞，但其內容記述的仍是忍冬的藤。由此可見宋 代以前諸家本草所記載的忍冬，都是使用藤葉，而沒有單獨用花。

明代地方性醫藥名著滇南本草收載：金銀花，性寒味苦，清熱 解諸瘡、痈疽發背、無名腫毒、丹流瘰病。杆能寬中下氣，消疾，

去風熱，清咽喉熱痛。杆即是藤。明 李時珍本草綱目云:忍冬莖葉 及花功用皆同。昔人稱其治風、除脹、解痢為要藥..，後世稱其消 腫，散毒、治瘡為要藥。其所引附方也是莖葉花均入藥。根據上 述，可知明代醫家會依臨床所需，採用忍冬的莖葉，或用其花，屬 莖葉及花並用階段。

明代之後，由於溫病學的發展及對金銀花的效用認識更加全 面，尤其強調用花，忍冬莖葉的應用比較少。如清 汪昂本草備要 云：散熱、補虛、療風、養血止渴，並謂花葉同被，花香為佳。

張壽熙本草正義對歷代本草所載的忍冬及花的功能做一總結，

並將花與葉的療效進行比較，書中寫道^17,22“忍冬……，今人多用其 花，實則花性輕揚，力量甚弱，不如枝蔓之氣味俱厚。古人只稱忍 冬，不言其花，則並不用花入藥，自可於言外得之。……壽熙已謂 不如藤葉之力厚，且不僅煎劑之必須，即外用煎湯洗滌亦大

良………”。忍冬之本草系統圖如Figure 1所示。

Figure 1 忍冬之本草系統圖

有消炎防腐作用，芳樟醇有平喘鎮咳和治療小兒肺炎及扁桃體炎的 藥理作用。在解熱、消炎、免疫等實驗研究結果表明，其水煮液，

口服液和注射液對角叉菜膠、三聯菌苗致熱有不同程度的退熱作 用，對蛋清、交叉菜膠、二甲苯所致水腫有不同程度的抑制作用，

另外，還能提高鼠腹腔巨噬細胞吞噬巨紅細胞的吞噬百分率和吞噬 指數，從而證明臨床作用透過調節機體免疫功能，達到清熱解毒來 治療感染性疾病。

2. 保肝利膽作用

在動物實驗當中，金銀花中的三萜皂苷對CCl4引起的小鼠肝損 傷有明顯的保護作用，並明顯減輕肝臟病理損傷程度。其所含綠原 酸能增進大鼠膽汁分泌；黃褐毛忍冬總皂甙對實驗性肝損傷有保護 作用，其皮下注射能顯著對抗四氯化碳，撲熱息痛及 D-半乳糖胺所 致肝中毒小鼠血清穀丙轉氨酶升高，降低肝臟甘油三酯含量，而減 輕肝臟損傷程度。而總皂苷中α-常春藤皂苷和無患子皂苷 B 的混合 物對因乙醯氨基酸(paracetamol)所引起小鼠肝臟毒性有保護作用。

3. 抗病原微生物

金銀花所含的有機酸成分-綠原酸、異綠原酸，黃酮類成分-木 樨草素和揮發油類成分-芳樟醇等皆有抗菌作用。金銀花爲廣泛抗菌 藥物，在體外試驗中發現對痢疾桿菌、金黃色葡萄球菌、傷寒桿 菌、副傷寒桿菌、霍亂弧菌、大腸桿菌、變形桿菌、綠膿桿菌、α-溶血鏈球菌、β-溶血鏈球菌、肺炎雙球菌和百日咳桿菌等，有較強 抗菌作用；其酒精浸劑在1：100000 濃度下仍能抑制人型結核桿菌 生長，減輕該菌所致肺部病變。單味金銀花對小白鼠試驗結核病有 療效。

其水浸劑比煎劑作用強，葉煎劑比花煎劑作用強。金銀花對變 形鏈球菌，具有較好的抑菌和殺菌作用，金銀花與青黴素合用，能 加強青黴素對耐藥金黃色葡萄球菌的抗菌作用，兩者具有協同作 用。金銀花對鐵銹色小芽孢癬菌、星形奴卡氏菌等皮膚黴菌產生綠 暈現象。金銀花對流感病毒、孤兒病毒、皰疹病毒、猴免疫缺陷病 毒(SIV) 等多種病毒均有抑制作用，金銀花注射液對綠膿桿菌內毒素 有一定的對抗作用。對傷寒桿菌內毒素有減毒作用。此外，試管試 驗表明，金銀花及其藤煎劑對鉤端螺旋體有抑制作用。

4. 抗生育

浙江産金銀花經乙醇提取後之水煎液浸膏，在臨用前用蒸餾水 配製成所需濃度，對小鼠、狗、猴等多種動物有明顯的終止妊娠作 用，尤其對小鼠、狗有顯著的抗早孕作用，並觀察了金銀花提取物 對妊娠小、大鼠不同孕期的影響，初步探討了其抗早孕作用的機

理。

5. 止血

金銀花炭水煎液、混懸液具有顯著的止血作用，且混懸液的作 用強於水煎液。金銀花炭中鞣質的含量僅為生品的一半，但其止血 作用明顯優於生品。

6. 降血脂

金銀花能顯著降低小鼠血清膽固醇(Tc)及動脈粥樣硬化指數 (AI)， 提高高密度脂蛋白-膽固醇(HDL2c)含量，保護胰腺 β 細胞及 弱降糖作用。銀花露抑制腸道吸收膽固醇，而降低血脂，具有保護 心腦血管的作用；其有效成分能在體外與膽固醇結合，進而減少家 兔腸道膽固醇的吸收。

7. 免疫調節

金銀花具有促進白細胞的吞噬功能，促進炎性細胞吞噬功能。

8. 抗氧化

金銀花水提物在體外對於H2O2具有直接的消除作用，且呈線性 量效關係。而金銀花對燙傷小鼠中性粒細胞釋放過氧化氫有一定程 度的改善作用，能使燙傷小鼠中性粒細胞合成和釋放溶酶體酶的能 力相應減少，說明其具有抗氧化反應的作用。

9. 中樞興奮

綠原酸對大鼠、小鼠的中樞神經系統有興奮作用，口服可刺激 胃液分泌。

10. 抗病毒作用

金銀花腹腔注射可明顯減少綠膿桿菌內毒素所致小鼠死亡，金 銀花對上呼吸道感染致病病毒有抑制和延緩細胞病變作用。其複方 能滅活PR8株甲型流行性感冒病毒，防治繼發細菌感染。木樨草素 能抑制皰疹病毒。

11. 抗腫瘤

金銀花中黃酮類化合物木樨草素對 NK/LY 腹水癌細胞體外培 養有抑制生長的作用。金銀花及酒浸液對肉瘤S180 及艾氏腹水癌有 明顯細胞毒作用。

12. 其他作用

金銀花提取液口服對大鼠實驗性胃潰瘍有輕度預防效果。此外, 綠原酸還能輕微增強腎上腺素及去甲腎上腺素對貓與鼠的升壓作 用。

13. 毒副作用

金銀花水浸液灌服對家兔、犬等無明顯毒性反應，對呼吸、血 壓、尿量均無影響，小鼠皮下注射金銀花浸膏的LD50為53 g/kg。灰

毡毛忍冬蒸曬品無溶血性，而生曬品有溶血性。實驗研究表明，綠 原酸具有致敏原作用，可引起變態反應。

第五節 忍冬屬之化學成分考察 (一) 國外的研究現況

依據梁曉天的常用中藥基礎研究⁴¹，將忍冬屬植物的化學成分 分為揮發油（volatile oil）、黃酮（flavonoids）、三萜及三萜皂苷類

（triterpenoids＆triterpenoidal saponin）、iridoid、苯丙素類

（penylpropanoids）、有機酸衍生物（organic acid derivatives）和其 他類（others）等七大類。 Lonicera caerulea L.var. emphyllocalyx N^AKAI.

fresh leaves quercetin (1)

quercetin-3-rhamnoside (2) quercetin-3-O-β-D-glucoside (3) eriodictyol-7-glucoside (4)

42

Lonicera confusa DC.

flower buds rutin (5) quercetin(1)

luteolin-7-O-β-D-galactoside (6)

lonicerin (luteolin 7-O-neohesperidoside) (7) luteolin (8)

tricin-7-O-β-D-glucopyranoside (9) chrysoeirol-7-O-neohesperidoside (10) tricin-7-O-neohesperidoside (11)

43 44

Lonicera gracilipes var. glandulosa M^AXIM.

fresh leaves apigenin -7-O-( 2^G-rhamnosyl )- gentiobioside (12)

cosmosiin

(apigenin 7-O-β-D-glucopyranoside) (13) rhoifolin (14)

(apigenin-7-O-neohesperidoside) apigenin-7-O-gentiobioside (15) apigenin-7-O-sophoroside (16) luteolin-7-O-glucoside (17) luteolin-7-O-neohesperidoside (7) luteolin-7-O-gentiobioside (18)

45

Lonicera implexa A^ITON.

leaves implexaflavone (19)^* madreselvin A (20)^* madreselvin B (21)^* ochnaflavone (22) rhoifolin (14) luteolin (8)

luteolin-7-O-β-D-glucopyranoside (23) apigenin-7-O-primeveroside (24)

46

apigenin-7-O-β-D-glucopyranoside (13) apigenin-7-O-rutinoside (25)

3-methoxyquercetin-7-O-β-D-glucopyranoside (26)

fresh aerial

parts hydnocarpin (27) quercetin (1) ochnaflavone (22)

ochnaflavone-4^’-O-methyl ether (28) astragalin (29)

isoquercetin (30) rhoiflon (14)

47 Lonicera japonica

THUNB.

flower buds luteolin-7-O-D-glucoside (17) luteolin-7-O-β-D-galactoside (6) quercetin-3-O-β-D-glucoside (3) hyperoside (31)

luteolin (8) corymbosin (32)

5-hydroxy-7, 3^’, 4^’-trimethoxy flavone (33) 5-hydroxy-7, 3^’-dimethoxy flavone (34) quercetin (1)

lonicerin (7)

48

49

Lonicera similis H^EMSL.

flower buds luteolin (8) quercetin (1)

50 Triterpenoids & Triterpenoidal saponins

Lonicera angustifolia leaves oleanolic acid (35) ursolic acid (36)

51 Lonicera burnei

H^EMSL.

flower buds oleanolic acid (35) bourneioside A (37) bourneioside B (38) bourneioside C (39) bourneioside D (40) bourneioside E (41)

52 53 54 55

Lonicera confusa DC.

flower buds hederagenin-28-O-β-D-glucopyranosyl (6→1)-O-β-D-glucopyranosyl ester (42)

hederagenin-3-O-α-L-arabinopyranosyl (2→1)-O-α-L-rhamnopyranoside (43)

macranthoside A (44) macranthoside B (45) dipsacoside B (46) macranthoidin A (47) macranthoidin B (48)

56

Lonicera fulvotomentosa H^SUETS.C. C^HENG

flower buds fulvotomentoside A (49)^* α-hederin (50)

sapindoside B (51)

57

Lonicera gracilipes var. glandulosa MAXIM.

fresh leaves ferna-7, 9 (11)-diene-3α, 16α-diol (52)

3α, 16α-dihydroxyferna-7, 9 (11)-dien-12-one (53)

58

ferna-7, 9 (11)-diene-3α, 16α, 19α-triol (54) 3α, 16α-dihydroxyfern-8-en-11-one (55) 3α, 16α-dihydroxyferna-8-ene-7,11-dione (56) Lonicera implexa

A^ITON.

leaves hederagenin-3-O-α-L-arabinopyranoside (57) 46 fresh aerial

parts

saponin 1-12(58-69) 63^*,66^*,68^*,69^* loniceroside A (70)^* loniceroside B (71)^*

59

60 fresh leaves saponin 1-4 (72-75)

74^*, 75^*

61 Lonicera japonica

T^HUNB.

flower buds 3-O-α-L-rhamnopyranosyl (1→2)-α- L-arabinopyranosyl hederagenin 28-O-β-D- xylpyranosyl (1→6)-β-D- glucopyranosyl ester (76)

3-O-L-arabinopyranosyl hederagenin 28-O- α-L- rhamnopyranosyl (1→2) [β-D-xylpyrano syl(1→6)]-β-D-glucopyranosyl ester (77) 3-O-α-rhamnopyranosyl (1→2)-α-L-arabino pyranosyl hederagenin 28-O-α-L- rhamno pyranosyl (1→2) [β-D- xylpyranosyl (1→6)]-β-D- glucopyranosyl ester (78)

3-O-[α-L-rhamnopyranosyl (1→2)-α-L-arabi nopyranosyl]-28-O-[β-D-glucopyranosyl (1→

6)-β-D-glucopyranosyl] oleanolic acid (79)

62

flowers dipsacoside B (46) macranthoidin A (47)^* macranthoidin B (48)^*

64

Lonicera nigra L. fruit

(berries) monodesmosidic saponins 1-5 (80-84)

bidesmosidic saponin (85-87) 65 Monoterpene

Lonicera nitida E. H. WILSON

fresh twigs leaves

lonitoside (88)^* 66

Lonicera xylosteum

L. leaves xylostosidine (89)

loxylostosidine A (90^*) loxylostosidine B (91)^*

67 68 69 Iridoid

Lonicera alpigena L.

fruits morroniside (92) kingiside (93)

alpigenoside (94)^*

70 68 Lonicera angustifolia leaves sweroside (95)

6^’-O-β-apiofuranosylsweroside (96)^* loganin (97)

52

Lonicera caerulea L.var.emphyllocalyx

fresh leaves 7-ketologanin (98) epi-vogeloside (99)

42

NAKAI. (6R, 9R)-3-oxo-α-ionol-β-D-glucoside (100) caeruleoside A (101)^*

caeruleoside B (102)^*

caeruleoside C (103)^* 71

Lonicera coerulea

L. fresh leaves

and stem bark

sweroside (95) loganin (97) secologanin (104) secologanic acid (105) loganic acid (106)

periclymenosidic acid (107)^*

72

Lonicera gracilipes var. glandulosa M^AXIM.

fresh leaves erythritol-1-O-(6-O-trans-caffeoyl) -β-D-glucopyranoside (108)

1,2,3,4-tetrahydroxy-2-methylbutane -4-O-(6-O-trans-caffeoyl)-β-D- glucopyranoside (109)

arabitiol-5-O-(6-O-trans-caffeoyl)- β-D-glucopyranoside (110)

73

Lonicera implexa A^ITON.

leaves sweroside (95) loganic acid (106) grandifloroside (111) vogeloside (112) epi- vogeloside (99)

74

fresh aerial

parts secologanin dimethyl acetal (113) vogeloside (112)

epi- vogeloside (99) loganin (97)

secologanin (104)

7-O-butylsecologanic acid (114) secologanin dibutylacetal (115) secologanic acid (105)

sweroside (95)

74

75 Lonicera japonica

THUNB.

young shoots

secoxyloganin (116) 76

flower buds loniceracetalides A (117) loniceracetalides B (118) loganin (97)

secologanin (104)

secologanin dimethyl acetal (113) secologanoside 7-methyl ester (119) sweroside (95)

vogeloside (112) 8-epiloganin (120) kingiside (93) morroniside (92) epi-vogeloside (99) dehydromorroniside (121)

77

78

stems＆

leaves

L-phenylalaninosecologanin (122) 7-O-(4-β-glucopyranosyloxy-3-methoxy benzoyl) secologanic acid (123)

6^’-O-(7α-hydroxyswerosyloxy)loganin (124) (E)-aldosecologanin (125)

(Z)-aldosecologanin (126)

79

Lonicera korolkovii S^TAPF.

young plants

korolkoside(127)^* 80

fresh fruits

morroniside (92) kingiside (93) loganin (97) 7-ketologanin (98) secoxyloganin (116)

secologanin dimethyl acetal (113)

81

secologanin (loniceroside) (104) sweroside (95)

83 68 Lonicera

morrowii A. G^RAY.

stems kinginoside﹝sweroside-6^’-O-(4^” -O-feruloyl)-α-L-rhamnoside﹞(128)

84

Lonicera

periclymenum L.

stems morroniside (92) secologanin (104) loganic acid (106) secoxyloganin (116) secologanoside (129) periclymenoside (130) loganin (97)

sweroside (95)

85 68

86

Lonicera

quinquelocularis

roots loganin (97) sweroside (93)

6^’-O-β-apiofuranosylsweroside (96)^*

86

Lonicera tatarica L. leaves loganin (97) secologanin (104)

50 Penylpropanoids

Lonicera gracilipes var. glandulosa MAXIM.

fresh leaves aseculetin-6-O-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside (131)

4,9,9^’-trihydroxy-3,3^’-dimethoxy-8- O-4’^'- neolignan-7-O-β-D-glucopyranoside (7S,8S-threo form) (132)^*

4,9,9’-trihydroxy-3,3^’-dimethoxy-8- O-4^’-neolignan-7-O-β-D-glucopyranoside (7S,8R-erythro form) (133)^*

7R,8R-threo-4,7,9,9’ -tetrahydroxy-3- methoxy-8-O-4^’-neolignan-3^’ -O-β-D-glucopyranoside (134)^*

7S,8R-erythro-7,9,9^’-trihydroxy-3,3^’- dimethoxy -8-O-4^’-neolignan-4-O-β-D-glucopyranoside (135)^*

4,7,9-trihydroxy-3,3^’-dimethoxy-8-O-4^’ -neolignan-9’^'-O-β-D-glucopyranoside (7R,8R-threo form) (136)

4,7,9-trihydroxy-3,3^’-dimethoxy-8-O-4^’ -neolignan-9’^'-O-β-D-glucopyranoside (7R,8R-erythro form) (137)

(6R,7E,9R)-9-hydroxy-4,7- megastigmadien -3-one-9-O-〔α-L-arabinopyranosyl-

Lonicera hypoleuca aerial parts 4-hydroxy-2,6-di-(4^'-hydroxy-3^'-methoxy)-

phenyl-3,7-dioxabicyclo-(3,3,0)octane (140) 90 Organic acid derivatives

Lonicera angustifolia leaves methyl-4-hydroxy benzoate(141) 51

Lonicera burnei HEMSL.

flower buds chlorogenic acid ethyl ester (142) bis (5-formylfurfuryl) ether (143) 5-hydroxymethyl-2-furaldehyde (144)

52 91

Lonicera caerulea L.var.emphyllocalyx N^AKAI.

fresh leaves protocatechuic acid (145) methyl chlorogenate (146)

42

Lonicera confusa DC.

flower buds chlorogenic acid (147) caffeic acid (148)

methyl chlorogenate (146)

5-O-caffeoyl quinic acid butyl ester (149)

43 92

Lonicera hypoleuca aerial parts syringic acid (150) 90 Lonicera implexa

AITON. leaves chlorogenic acid (147) macranthoin G

(3,5-dicaffeoylquinic acid methyl ester) (151)

74

Lonicera japonica

THUNB. flower buds chlorogenic acid (147) 3-caffeoyl-quinic acid (152)

3-caffeoyl-quinic acid methyl ester (153) 3,5-dicaffeoylquinic acid (154)

3,5-dicaffeoylquinic acid methyl ester (151) 3,5-dicaffeoylquinic acid butyl ester (155)^*

93 49

Lonicera macranthoid H^AND.-M^AZZ.

flowers macranthoidin F (156) macranthoidin G (157)

94

chlorogenic acid (147) 84

Lonicera similis H^EMSL.

flower buds caffeic acid (148)

3, 5-dicaffeoylquinic acid (154) chlorogenic acid (147)

95

Others

Lonicera angustifolia leaves β-sitosterol 51

Lonicera burnei H^EMSL.

flower buds β-sitosterol 52

Lonicera confusa DC.

flower buds β-sitosterol tetratriacontane

43 Lonicera hypoleuca aerial parts β-sitosterol

β- sitosterol glucoside n-nonacosanol

scopeletin

90

Lonicera implexa AITON.

leaves myoinositol 74

fresh leaves venoterpine 96

Lonicera japonica

THUNB. flower buds daucosterol sucrose

49

Lonicera

quinquelocularis

aerial parts β-sitosterol 1-inositol hexacosanol n-triacontanol nonacosane

95

Lonicera similis H^EMSL.

flower buds β-sitosterol nonacosanol nonacosane

95

* new compound

(二) 國內忍冬屬之研究現況

將國內現況分類為天然物化學研究(成分分離、結構鑑定)、品 質評估(藥材與複方)、藥理活性探討及藥品動力學探討；然而國內 對於忍冬屬之研究多以 Lonicera japonica THUNBERG為主，本文針對 忍冬屬天然物化學成分相關研究作整理，如Table2 所列：

Table 2 國內研究之忍冬屬植物化學成分

學名 部位 化學成分 來

源 Lonicera acuminata

WALLICH

(銳葉忍冬)

stems Long chain fatty acid and ester:

octacosanyl hexadecanoate Steroid:

phytosterol (campesterol, stigmasterol, β-sitosterol)

stigmast-5-ene-3β,7α-diol

stigmast-5-ene-3β,7β-diol sitosterol-3β-D-glucoside

sitosterol-3-β-D-glucoside-6'-acetate sitosterol-3-β-D-glucoside

Flavonoid:

isorhamnetin ochnaflavone quercetin

97

Organic acid derivative:

protocatechuic acid methyl caffeate chlorogenic acid methyl chlorogenate

3, 5-di-O-caffeoylquinic acid methyl 3, 5-di-O-caffeoulquinate 3, 4-di-O-caffeoylquinic acid methyl 3, 4-di-O-caffeoylquinate Flavonoid:

3, 5-di-O-caffeoylquinic acid methyl 3, 5-di-O-caffeoulquinate 3, 4-di-O-caffeoylquinic acid methyl 3, 4-di-O-caffeoylquinate Flavonoid:

在文檔中 紅腺忍冬葉部之化學成分研究; Studies on the Chemical constituents of the Leaves of Lonicera hypoglauca MIQUEL (頁 10-0)