key: cord-0037590-et66r6p8 authors: Zhou, Jiaju; Xie, Guirong; Yan, Xinjian title: Volume 3 Isolated Compounds (H-M) date: 2010-11-15 journal: Encyclopedia of Traditional Chinese Medicines - Molecular Structures, Pharmacological Activities, Natural Sources and Applications DOI: 10.1007/978-3-642-16747-8_1 sha: 499119b9b702d2cbae9abb3515e597a9a633108b doc_id: 37590 cord_uid: et66r6p8 Hemanthamine [466-75-1] C17H19NO4 (301.35). mp 203~203.5ºC, [a]D 25 = +19.7º (c = 3.8, methanol), [a]D 25 = +33 (c = 1.25, CHCl3). Pharm: Antihypertensive (mild); antiretroviral and cytotoxic (ID50 = 0.8µg/mL, TC50 = 1.0µg/mL, TI50 (TC50/ID50) = 1.3)[5026]. antibacterial inactive (various tested bacteria) [5175] ; antifungal inactive (various tested fungi) [5175] ; LD 50 (mus, ip) = 705mg/kg, (mus, iv) = 135mg/kg. Source [5876-17-5] C 13 H 11 NO 4 (245.24) . mp 203~204ºC. Pharm: Phototoxic (yeast, Saccharomyces cerevisiae); photo-activated antibacterial (Staphylococcus aureus) [4989] ; photo-activated antifungal (Candida albicans weak) [4989] ; photo-activated DNA binding (Asc I and Sma I with restriction sequences consisting only of G and C was very weak) [4989] ; cytotoxic (P 388 cell line, ED 50 = 7.6μg/mL, control Mithramycin, ED 50 = 0.06μg/mL; HT29, ED 50 = 13.1μg/mL, Mithramycin, ED 50 = 0.07μg/mL; A549, ED 50 = 3.3μg/mL, Mithramycin, ED 50 = 0.08μg/mL) [5405] . Source [525-57-5] C 12 H 12 N 2 O (200.24) . Trihydrate, red acicular crystals (C 2 H 5 OH aq.), absolute substance mp 212ºC (dec). Pharm: Causes progressive paralysis of CNS (animal model); inhibits transport of active sodium (in bladder); monoamine oxidase inhibitor; Na + ,K + -ATP inhibitor; antihypertensive; Slows heart rate and enhances myocardial contractility Hederagenin-3-O-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside C 41 H 66 O 12 (750.98) . mp 228~230ºC. Pharm: Anti-inflammatory (male ICR mus, orl, dose = 50mg/kg) [4212] ; anti-inflammatory (modulator of cytokine network: prevents 50 = 5μmol/L) [4416] ; antioxidant (75μg/mL, total antioxidant activity ( 6, 7, 8, 8a, 9, 10 Isorhodeasapogenin 3-O-β-D-glucopyranosyl-(1→3)-[β-D-xylopyranosyl- (1→2) ]-β-D-glucopyranosyl-(1→4)-β-D-galactopyra-noside C 50 Pharm: Anti-inflammatory (COX-1 inhibitor, 1000μmol/L, InRt = (52±2)%, positive control Indomethacin, 1.7μmol/L, InRt = (43±3)%) [4413] [α] D 25 CHCl 3 43.3μg/mL, control Mitomycin C, IC 50 = 1.7μg/mL) [4092] . Source [3850] ; cytotoxic (XTT assay, HL-60 cells, IC 50 > 50.0μg/mL; control NDGA, IC 50 = (2.6±0.2)μg/mL, Vitamin C, IC 50 > 10.0μg/mL, Trolox, IC 50 > 10.0μg/mL) [3850] . Source (−)-4-Hydroxymethyl-2- (1',2',2'-trimethylcyclopentyl) 2', 19 H 19 NO 5 (341.37) . Pharm: Anti-HIV-1 inactive IC 50 > 100μmol/L, positive control Suramin, IC 50 = 2.4μmol/L) [4224] (modulator of cytokine network: inhibits LPS-stimulated TNF-α release in 3.10%) [5508] , ZHI SHI Citrus aurantium (dried ripe pericarp: content = 0.99%) [5508] . Ref: 2, 4, 658, 660, 4752, 5041, 5501, 5508 . Paeonia lactiflora] (fresh fruit: yield = 0.010%fw) [4695] , HU TAO REN Juglans regia. Ref: 3065, 3408, 4695 . Leonurus artemisia] (aerial parts). Ref: 4493, 4534 . antitussive (dispels phlegm); platelet aggregation inhibitor; binding activity to benzodiazepine receptor (IC 50 = (1.3±0.2)μmol/L, control Diazepam, IC 50 = (0.05±0.01)μmol/L) [5366] ; PFTase inhibitor (100μg/mL, InRt = 75%) [5378] ; cytotoxic (strongly inhibits growth of ZR-75-1 cells, GI 50 = 1.2μg/mL) [5378] ; cytotoxic inactive (hmn breast cancer cell lines: MDA-MB-231, MCF7, T47D, 20μg/mL) [5378] ; angiogenesis inhibitor inactive (chicken embryo chorioallantoic membrane (CAM) assay, 10μg) [5378] . Source [4747] . Source [71-00-1] C 6 H 9 N 3 O 2 (155.16). Pharm: An essential amino acid for children; promotes ulcer healing. Source: BAN XIA Pinellia ternata (dried tuber: content scope of 4 origins = 0.22%~2.33%, mean content = 0.88%) [5521] , HU LU BA Trigonella foenum-graecum [658] , YI YE JIA FAN LV Pseudostellaria heterophylla (tuberoid: mean content of 5 origins = 0.0456%) [5508] . Ref: 658, 5508, 5521 1, [4661] ; NO production inhibitor (IC 50 = 43.5μmol/L, control L-NMMA, IC 50 = 28.5μmol/L) [5407] . Source (inhibits cellular leakage of LDH and AST, and cell death, induced by 1.5μmol/L tBH for 1h, effective dose = 20μmol/L, 40μmol/L; induced by 30μmol/L GalN, effective dose = 1μmol/L, 5μmol/L, and 20μmol/L) [5344] ; hepatoprotective (inhibits tBH-induced lipid peroxidation, primary cultured rat hepatocytes, thiobarbituric acid reactive substance (TBARS) assay, effective dose = 5, 20 and 40μmol/L) [5344] ; hepatoprotective (inhibits GSH depletion, GSH concentration in tBH-treated hepatocytes was significantly reduced to 17 % of that of normal hepatocytes, effective dose = 5μmol/L, 20μmol/L, and 40μmol/L; induced by GalN, effective dose = 1μmol/L, 5μmol/L and 20μmol/L) [5344] ; antioxidant (protects rat heart and liver mitochondria against lipidperoxidation; hydroxyl radical scavenger) [5362] ; platelet aggregation inhibitor [5362] ; antiarrhythmic [5362] ; anti-ischemia myocardial (myocardial ischemia-reperfusion injury) [5362] ; anti-myocardial infarction (rat, reduces area of coronary artery infarction) [5362] ; increases tolerance to anoxia (rat, no significant hemodynamic change after intravenous infusion of honokiol at the dosages of 0.01μg/kg, 0.1μg/kg and 1.0μg/kg, however significantly reduces total volume of infarction at 0.1μg/kg or 1.0μg/kg) [5362] ; antibacterial (gram-negative bacteria and acid-fast bacteria); anticaries 6S-(1R-Hydroxy-2R-cinnamyloxyphenethyl)-5,6-dihydro-5S-hydroxy-2-pyr one [190848-69-2] C 22 H 20 O 6 (380.40) . White acicular crystals, mp 176~178ºC, [α] D = +97.6º (c = 0.087, chloroform). Pharm: Antineoplastic (hmn tumor, in vivo and in vitro, cell proliferation inhibitor, blocks cell from G 1 to S phase, increases fluidity of L 1210 cell membrane) [2442] . Source 50 = 11 .1μmol/L, mus P 388 , ED 50 = 9 .8μmol/L); platelet aggregation inhibitor (rbt, 100μg/mL, due to arachidonic acid, InRt = 100%, due to collagen, InRt = 83.9%, due to PAF, InRt = 100%). Source (85±5)μmol/L; control Etoposide, GI 50 < 1.5μmol/L, Chlorambucil, GI 50 < 50μmol/L; induces decrease in cellular GSH content and increases ROS production) [ 0.05U/mL thrombin induced, InRt = 6.8%) [4654] ; antioxidant (inhibits superoxide anion generation, fMLP/CB, IC 50 control DPI, IC 50 [4950] . Source (2-methylpropanoyl)-3β, 15α,16α,21β,22α,28-hexahydroxyolean-12-ene C 48 H 76 O 19 (957.13 pyranosyl- (1→2)-β-D-glucopyranosyl-22-O-acetyl-21-O-(2-methylpropanoyl )-3β,15α,16α,21β,22α,28-hexahydroxyolean-12-ene C 59 H 96 O 27 (1237.41 (1'S, 6'R, 2Z, [3042] , ZHONG GUO XIU QIU Hydrangea chinensis (root) [3069] . Ref: 2, 660, 3042, 3069, 4488, 4502, 4676, 4722, 4747, 4758, 4789 [5508] , occurs in many plants. Ref: 2, 415, 544, 562, 594, 658, 660, 2529, 3423, 3802, 4233, 4473, 4488, 4502, 4544, 4706, 4722, 4733, 4758, 5508 . '-β-D -glucosyl)-cyclohex-2'-en-1'-yl]-3-methyl-penta-2, Anticancer Flavonoid PMV70P691-019 C 20 (4S)-5-Hydroxy-4-methoxy-α-tetralone C 11 H 12 O 3 (192.22 Acid 6-hydroxy-1,7(11)-humuladienyl-10-yl ester [ ; DPPH scavenger inactive [5371] ; antidepressant [1521] ; inhibits reuptake of neurotransmitters (synapses) [1521] ; cytochrome P450 (CYP3A4) inducer (hepatocytes) [1521] ; antibacterial (gram-positive and gram-negative bacteria) [1521] . Source: BIAN DI JIN Hypericum wightianum (dried whole herb: content = 0.0375%) [5508] , DI ER CAO Hypericum japonicum (dried whole herb: content = 0.0897%) [5508] , GUAN reversing MDR of KBV200 cells (obviously) [2787] ; PGE 2 production inhibitor (rat peritoneal macrophages, LPS-induced, 0.1μmol/L; inhibits LPS-induced expression of COX-2 and mPGES, not directly inhibits COX-1 and COX-2) [5392] ; T-cell Proliferation inhibitor [4071] ; cytotoxic (24h: 1-[2,4-Dihydroxy-3-(4-hydroxy-3-methyl-2-butenyl)-6-methoxyphenyl]-3-(4- hydroxyphenyl)-2-propen-1-one C Quercetin-3-O-(2''-galloyl)-β-D- HL-60, IC 50 tumor, mus tumor U14, 3~7mg/kg ip, InRt = (44.0~55.5)%, mus lymphatic sarcoma, 3mg/kg, InRt = 33.3%, liver cancer in solid tumor, 7mg/kg, InRt = 38%, liver cancer with ascites, 5mg/kg, biotic prolonged rate = 150%, EAC, 5mg/kg, biotic prolonged rate = 38%); immunoenhancer; cytotoxic (radiosensitizing agent, in vitro, U 14 , S-180V, HeLa, mus Ma7373 breast cancer cell, hmn intestinal mucoadenocarcinoma in nude mouse, mechanism was considered to be an inhibition of oxygen consumption and depletion of glutathione in tumor cells) [5369] ; antineoplastic (mus tumor xenografts, U 14 cervical cancer and Ehrlich carcinoma, ip, lymphosarcoma, ip and oral administration, inhibits cancer growth) [5369] ; antineoplastic (mus bearing U 14 tumor, orl 100mg/kg or iv 5mg/kg, once every other day for 5 cycles, starting 24h after implantation of the tumor, tumor inhibition rate = (35~55)%) [5369] ; antineoplastic (clinical trial, given orl to 558 patients with cancer of lung and esophagus, or with superficial metastatic cancer during radiotherapy, significantly reduction of tumor size and prolongation of survival time of the patients) [5369] ; LD 50 (mus, ip) = 28mg/kg (25.4mg rel-(7''E)- (7α, 8β, 7'α, 4, 9, 9', 7:3'', 4':8', rel-(7''E)- (7α, 8β, 7'β, 4, 9, 9', 7:3'', 4':8', nerve (10μmol/L, increases activity of choline acetyltransferase in rat rel-(7''E)- (7α, 8β, 7'α, 4, 9, 9', 7:3'', 3':8', rel-(7''E)- (7α, 8β, 7'β, 4, 9, 9', 7:3'', 3':8', [5253] ; cytotoxic (in vitro, A549, ED 50 = 16.3μg/mL, control Adriamycin, ED 50 = 0.0322μg/mL; MCF7, ED 50 = 9.3μg/mL, Adriamycin, ED 50 = 0.0204μg/mL; HT29, ED 50 = 3.5μg/mL, Adriamycin, ED 50 = 0.0421μg/mL; A498, ED 50 = 3.9μg/mL, Adriamycin, ED 50 = 0.00348μg/mL; PC3, ED 50 = 4.8μg/mL, Adriamycin, ED 50 = 0.241μg/mL; PACA-2, ED 50 = 2.2μg/mL, Adriamycin, ED 50 = 0.0120μg/mL) [5253] [26833-86-3] C 28 H 37 NO 9 (531.61). Pharm: Antineoplastic (mus L 1210 , 7.5mg/kg ip, biotic prolonged rate = 26%, P 388, biotic prolonged rate = 172%). ((7α, 7'α, 8α, 8'α, 7''α, 7'':7, 9':7', 3'', 4, 4'', 7'α, 8α, 8'α, 7''β, 7'':7, 9':7', 3'', 4, 4'', Ref: 2, 658, 660, 1521 Ref: 2, 658, 660, , 2080 Ref: 2, 658, 660, , 2489 Ref: 2, 658, 660, , 2548 3, 4, 4a, 5, 6, 6a, 7, 11, 11a, 4, 3, 4, 4a, 5, 6, 6a, 7, 11, 11a, 4, 7, 3, 4, 4a, 5, 6, 4, 7, [4337] ; cytotoxic (quinone reductase induction assay in cultured Hepa1c1c7 mouse hepatoma cells, IC 50 = 0.16μg/mL) [5038] ; cytotoxic (soft agar transformation assay with JB6 cells, IC 50 = 0.13μg/mL) [5038] ; cytotoxic (mouse mammary organ culture assay, ca. 60% at 10μg/mL, a promising lead as potential cancer chemopreventive agents) [5038] , 4, 279, 283, 397, 463, 468, 552, 573, 658, 660, 1521, 3014, 3015, 3522, 4187, 4205, 4247, 4416, 4454, 4483, 4500, 4722, 4723, 5501, 5508, 5519, 5527, 5529 . [4669] ; NO production inhibitor (LPS-induced, concentration-dependent manner, IC 50 = 8.9μmol/L or 6.6μmol/L) [4918] ; PGE 2 production inhibitor (LPS-induced, concentration-dependent manner, IC 50 = 9.6μmol/L or 5.1μmol/L) [4918] Antioxidant (6.25μg/mL, superoxide radical scavenging activity = 5.5 %, control Curcumin 16.1%; 6.25μg/mL, DPPH radical scavenging activity = 9.4 %, control Curcumin 50.0%) [4535] ; hepatoprotective (primary cultures of rat hepatocytes, H 2 O 2 -induced toxicity, 50μmol/L, relative protection = 50.8% Glycyrrhetic acid-3-O-β-D-6''-n-methyl-glucuronopyranosyl-(1→2)-β-D-6'- n-butyl-glucuronopyranoside C Insularoside-3'-O-β-D-11121 Ioniceroside C 3-O-β-D-Glucopyranosyl hederagenin 28-O-α-L-rhamnopyranosyl (1→2)- [β-D-xylopyranosyl(1→6)]-β-D-22-Oxo-23-hydroxyiridal-3-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside]-16-β- D-glucopyranoside C3-[rel-(2S,3R)-5-Hydroxy-6-(3α-isopropenyl-2,2-dimethylcyclobutyl-β-methy l)-2,3-dimethyl-6-(3-methylbut-2-enyl)-4,7-dioxo-3, (−)-(1S,2S,3S)-1-Ethenyl-1-methyl-2,3-di(1-methylethenyl)-8-(3'''-methylbut-2'''-enyl)-6-(2''-hydroxy-3''-methylbut-3''e nyl) isoflavone21-O-Tigloyl-28-O-acetylprotoaescigenin-3-O-[β-D-glucopyranosyl(1→2)] [β-D-glucopyranosyl(1→4)]-β-D-21-O-Angeloyl-28-O-acetylprotoaescigenin-3-O-[β-D-glucopyranosyl(1→2)] [β-D-glucopyranosyl(1→4)]-β-D- A (+)-(S)-1,5-Dimethyl-7-(1-methylethenyl)-cyclodeca-1E, 2-(3,4-dihydroxyphenyl)-ethyl-O-β-D-glucopyranosyl-(1→6)-3-O-trans-caffeoy l-β-D- Isorhamnetin 3-O-(6''-O-α-L-rhamnopyranosyl)-β-D-O O O O O OH O O H OH O O O O H O O 11671 Isorhamnetin 3-O-β-D-xylopyranosyl-(1''''→3''')-α-L-rhamno- pyranosyl-(1'''→6'')-β-D- 3'-Methoxyisovitexin 2''-O-(6'''-(E)-p-coumaroyl)-β- Isovitexin 2''-O-(6'''-(E)-feruloyl)-β-glucopyranoside-4'-O-β-3-O-α-L-Rhamnopyranosyl-(1→3)-β-D-glucopyranosyl-(1→3)-α-L-rhamnop yranosyl-(1→2)-α-L-arabinopyranosyl-hederagenin 28-O-β-D- (H 2 O 2 -treated, relative protection = 0.0%, control, relative protection = 100%), positive control Silibinin, Relative protection = 74.9%) [4996] ; CYP3A4 inhibitor inactive (IC 50 > 100μmol/L, control Ketoconazole, IC 50 = 0.245μmol/L) [4669] ; CYP2D6 inhibitor inactive (IC 50 > 100μmol/L, control Quinidine, IC 50 = 0.078μmol/L) [4669] 3-O-[α-L-Rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl]-hedragenin-28-[α- L-rhamnopyranosyl-(1→2)-β-D-glucopyranosyl(1→6)-β-D- [23740-25-2] C 18 H 11 NO 4 (305.29). mp 302~303ºC (dec). Pharm: Platelet aggregation inhibitor inactive (rat blood: 2~5μmol/L ADP-induced, IC 50 > 1000μmol/L, control Acetylsalicylic acid, IC 50 > 1000μmol/L; 2~5μg/mL collagen-induced, IC 50 > 500μmol/L, Acetylsalicylic acid, IC 50 cruzi, strain Y, IC 50 > 250μg/mL, IC 90 > 250μg/mL) [3976] [α] D = +29.90º (c = 0.7, chloroform). Pharm: Analgesic (hot plate model, murine writhing model and murine tail-swing model); antiarrhythmic (rat, caused by 0.07mg/kg 3-acetylaconitine, ED = 0.5mg/kg); anti-inflammatory (rat, caused by formaldehyde); antipyretic (mus with artificial fever by triad-vaccine); local anesthetic; anti-inflammatory (modified assay of Berridge, 100μg/mL, InRt = 29.34%) [5271] ; tyrosinase inhibitor (IC 50 = (93.33±0.16)μmol/L, control Kojic acid, IC 50 = (16.67±0.52)μmol/L, L-Mimosine, IC 50 = (3.68±0.02)μmol/L) [5271] ; antioxidant (DPPH scavenger, 1μmol/L, ScRt = 12.0%; control 3-t-Butyl-4-hydroxyanisole, 1μmol/L, ScRt = 92.5%) [5271] ; LD 50 (mus, iv) = 6.9mg/kg, (mus, ip) = 9.1mg/kg, (mus, orl) = (25R)-3β-Hydroxy-5α-spirostan-6-one 3-O-[O-α-L-arabinopyranosyl-(1→6)- 6α, 16β, 6α, 16β, 6α, 16β, 591, 1521, 1679, 1681, 1690, 1691, 1692, 1693, 1694, 1695, 1696, 4470 C 30 H 24 O 6 (480.52 C 40 H 40 O 6 (616.76). Yellow needles (MeOH), mp 86~89ºC. Pharm: MAO-A inhibitor (rat brain mitochondrial enzyme, IC 50 > 100μg/mol/L); MAO-B inhibitor (rat brain mitochondrial enzyme, IC 50 5, 5'', 7, 7'', ,29-dihydroxy-24,25,26,27-t etranorlanost-8-en-17α,23- -hydroxy-15-oxo-24,25,26,27-tetranorlanost-8-en-17α,23-olide C 54 H 84 O 27 (1165.26 A 3-O-β-D-Xylopyranosyl (1→2)-α-L-rhamnopyranosyl-6α-O-β-D-xylopyra- nosyl-22-O-β-D-glucopyranosyl-16β- syl-(1→6)-β-D-glucopyranosyl)oxy]-29-hydroxy-15-oxo- 24,25,26,27-tetranor lanost-8-en-17α,23-olide C 59 H 92 O 31 (1297.37 Bacillus termo); antifungal (Candida albicans); cytotoxic (NK/LY ascites cancer in vitro); anti-inflammatory (rat, caused by woolball-embedding, 20mg/(kg⋅d), 7 days); antispasmodic (rbt intestine in vitro, gpg trachea smooth muscle and ileum); antitussive (inhibits coughing center); dispels phlegm (rat capillary tube method, mus P.S.P. method); antiviral (H. suis virus); enhances arterial tension and lowers intravenous tension (dog heart in vitro, 5~10mg); enhances blood capillary permeability (rat, 0.5g/kg sc); immunoenhancer; increases coronary flow; dihydrocoenzyme I (NADH) oxidase inhibitor; iodine-induced thyronine deiodinase inhibitor; aldose reductase inhibitor (eye lens, IC 50 50 = 0.072μmol/L) [4214, 4530] ; protein kinase C inhibitor; succinic oxidase inhibitor; antihypercholesterolemic (rbt, reduces the level of cholesterol and triglyceride in serum); anti-inflammatory (modulator of cytokine network: inhibits 50 < 1μmol/L) [4416] decreases both PMA and oxazolone-induced allergic ear oedema) [4416] ; anti-inflammatory (significantly reduces LPS-stimulated ICAM-1 expression in liver of LPS-treated mouse) [4416] ; anti-inflammatory (treatment of airway bronchoconstriction and bronchial hyperreactivity, reduces level of both IL-4 and IL-5, a suggested lead compound to treat asthma) [4416] ; anti-inflammatory (IL-5 inhibitor, concentration-dependent manner, mean IC 50 = 18.7μmol/L) [4416] ; anti-inflammatory (COX-2 inhibitor, rat renal medulla, moderate activity) [4415] ; 15-lipoxygenase inhibitor [4415] ; anti-inflammatory (NO production inhibitor) [4415] ; anti-HIV; LD 50 Apiaceae spp., Scrophulariaceae spp., Asteraceae spp., Cistaceae spp. and Passifloraceae spp.). Ref: 2, 4, 369, 602, 658, 660, 1521, 3029, 4214, 4415, 4416, 4530, 4664, 4689, 4752, 5400, 5501, 5508, 5535 . 20 O 11 (448.39) . mp 168~178ºC. Pharm: Anti-inflammatory (IL-5 inhibitor, concentration-dependent manner, mean IC 50 = 3.7μmol/L) [4416] ; Xanthinoxidase inhibitor (IC 50 = 2.0μmol/L); cAMP phosphodiesterase inhibitor (IC 50 = 79μmol/L); aldose reductase inhibitor (IC 50 = 4.8μmol/L, control Epalrestat, IC 50 = 0.072μmol/L) [4530] Luteolin 7-O-β-D-glucopyranosiduronic acid C 21 H 18 O 12 (462.37 Methyl-1-cyclohexen-1-yl-1, 3,5,7,9,11,13-tetradecaheptaene [26000-17-9 Margetine [19622-83-4 antifungal (Candida albicans, IZD = 40mm, MIC = 39μg/mL) [3829] ; toxin (in genus Narcissus plants); LD 50 (dog) = 41mg/kg, (mouse, orl) = 230mg/kg, (mouse, sc) = 145mg/kg, (mouse, ip) = 117mg/kg, (mouse, iv) = 123mg/kg. 2-(4-Methoxyphenyl)-1-nitroethane C 9 H 11 NO 3 (181.19) . Pale yellow oil. Pharm: Antifungal (TLC, Candida albicans, 31.4μg/cm 2 , IZD = 0mm; Fusarium oxysporum, 31.4μg/cm 2 , IZD = 9mm, 15.7μg/cm 2 , IZD = 9mm, 7.9μg/cm 2 , slight inhibition; Cladosporium herbarum, 31.4μg/cm 2 , IZD < 9mm, 15.7μg/cm 2 , IZD < 9mm, 7.9μg/cm 2 , slight inhibition); antibacterial inactive (TLC, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, ; CYP3A4 inhibitor (hmn CYP3A4, enzyme activity was monitored by nifedipine oxidation, IC 50 = 120μmol/L) [ 12 O 5 (284.27) . mp (−) 195~196ºC, (±) 199~200ºC. Pharm: Antifungal (EC = 10μg/mL); hepatoprotective (mus primary cultured hepatocytes, antihepatotoxin induced by D-galactosamine (GalN), 100μmol/L, InRt = (35.2±3.0)%, weak, control Silybin, 100μmol/L, InRt = (77.0±5.5)%) [4095] ; antibacterial (Staphylococcus aureus ATCC 25923, MIC > 512μg/mL, Vancomycin, MIC = 0.5μg/mL; MRSA SK1, MIC > 512μg/mL, Vancomycin, MIC = 1.0μg/mL) [3810] ; increases blood pressure (anesthetized rats, increases in mean arterial blood pressure, 0.4mg/kg, 8.3mmHg) [3810] . Pharm: Antibacterial (Streptococcus sp., MIC = 0.63μg/mL); antiulcerative (rat, prevents stress ulcer due to waterlogging, 5~20mg/kg); muscle relaxant (MED = 90mg/kg); hepatoprotective (inhibits cellular leakage of LDH and AST, and cell death, induced by 1.5μmol/L tBH for 1h, effective dose = 40μmol/L; induced by 30μmol/L GalN, effective dose = 1, 5, and 20μmol/L) [5344] ; Hepatoprotective (inhibits tBH-induced lipid peroxidation, primary cultured rat hepatocytes, thiobarbituric acid reactive substance (TBARS) assay, effective dose = 20 and 40μmol/L) [5344] ; Hepatoprotective (inhibits GSH depletion, GSH concentration in tBH-treated hepatocytes was significantly reduced to 17 % of that of normal hepatocytes, effective dose = 20, and 40μmol/L; induced by GalN, effective dose = 5 and 20μmol/L) [5344] . Quinidine, CYP2D6, IC 50 = 0.082μmol/L) [4797] Dammar-23 (24) (iNOS) gene expression; downregulates cyclooxygenase-2 (COX-2) gene expression; downregulates interleukin-6 (IL-6) gene expression; downregulates gene expression; downregulates cyclooxygenase-2 (COX-2) gene expression; downregulates interleukin-6 (IL-6) gene expression; downregulates interleukin-1b expression; downregulates cyclooxygenase-2 (COX-2) gene expression; downregulates interleukin-6 (IL-6) gene expression; downregulates [Syn. Panax schinseng] (rhizome: content = 0.42% [5508] ), XI YANG SHEN Panax quinquefolium (rhizome: content = 0.21%) [5508] 7a,10a-Dihydro-5-hydroxy-8,8-dimethyl-6-(2-methyl-1-oxobutyl)-4-phenyl-2 H-8H- [1,2]-dioxolano[4'',5'':4',5'] furo [2',3':5,6] benzo [1,2-b] , ED 50 = 2.53μg/mL, control Ellipticine ED 50 = 0.61μg/mL; KB, ED 50 = 2.48μg/mL, Ellipticine ED 50 = 0.54μg/mL; Col2, ED 50 = 3.42μg/mL, Ellipticine ED 50 = 0.60μg/mL; Lu1, ED 50 = 2.33μg/mL, Ellipticine ED 50 = 0.61μg/mL; BCA-1, ED 50 = 6.51μg/mL, Ellipticine ED 50 = 0.52μg/mL) [5478] Angelica porphyrocaulis], DU HUI MAO DOU Tephrosia toxicaria (stem: yield = 0.00023%dw) [4718] , GOU SHU Broussonetia papyrifera [3090] (7S,8R)- 3, 9, [24, 25, 26, 1, 14, 20(22 24, 25, 26, 20, C 26 H 34 O 11 (522.55 Epoxypseudoisoeugenyl 2 7, 2', 4':2'', 3'') [ 4-Methoxy-3-methyl-5-[(2Z,11aS)-8t-((1R)-1-methoxypropyl)-1c-methyl-(11 ar,11bc) -1,2,5,6,8,9,10,11,11a,11b-decahydrofuro[3,2-c] pyrido [1,2-a] C 13 H 13 NO (199.25 5 (270.24) . Pharm: β-Hexosaminidase release inhibitor (RBL-2H3 cells, 100μmol/L, InRt = (82.3±0.7)%, p<0.01) [4347] ; cytotoxic (KB, ED 50 > 25μg/mL, control Doxorubicin, ED 50 = 0.12μg/mL; Hep3B, ED 50 = 1.7μg/mL, control Doxorubicin, ED 50 = 0.14μg/mL; Colon205, ED 50 = 1.16μg/mL, control Doxorubicin, ED 50 = 0.10μg/mL; HeLa, ED 50 = 12.3μg/mL, control Doxorubicin, ED 50 = 0.11μg/mL) [4369] ; NO production inhibitor (in vitro, LPS-activated mouse peritoneal macrophages, 3μmol/L, 10μmol/L, 30μmol/L, 100μmol/L, InRt = 7.9%, 37.5%, 99.5%, 99.6%, respectively; control L-NMMA, 3μmol/L, 10μmol/L, 30μmol/L, 100μmol/L, InRt = 10.3%, 15%, 34.1%, 63.1%, respectively) [ 26-O-β-D-Glucopyranosyl-22-methoxy-3β,26-dihydroxy-25(R)-furost-5-en-3- O-α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)-[α-L-rhamnopy ranosyl-(1→2)]-β-D- (1'E)-(1R*,5R*,9S*)-9-Hydroxy-1-(2,6-dimethylhepta-1,5-dienyl)-3,6-dioxo- ; cytotoxic (cyclooxygenase-1 inhibitor) [5038] ; aromatase inhibitor inactive (in vitro, IC 50 > 40μmol/L; control Aminoglutethimide, IC 50 = 6.4μmol/L) [3090] [5507] Pharm: Bidirectional action to drowsiness (excitation in low dose and inhibition in high dose); coronary vasodilator (increases coronary flow); increases tolerance to anoxia (mus, cardiac muscles, 100mg/kg ip); LD 50 (mus, iv) = 152~172mg/kg, (mus, ip) = 270~290mg/kg. Source: SHE XIANG Moschus moschiferus; Moschus berezovskii; Moschus sifanicus (dried secretion obtained from musk gland of musk deer: content scope = 0.50%~5.00% [5501] ; content scope of 9 batch samples = 0.37%∼5.30%, mean content = 2.91% [5508] O (208.35) . Pharm: Cytotoxic (A549, ED 50 = 3.2μmol/L, ED 50 = 14.7μg/mL, control Adriamycin, ED 50 = 0.01μmol/L, ED 50 = 0.02μg/mL; MCF7, ED 50 = 0.6μmol/L, ED 50 = 2.7μg/mL, Adriamycin, ED 50 = 0.1μmol/L, ED 50 = 0.1μg/mL; HT29, ED 50 = 1.8μmol/L, ED 50 = 8.0μg/mL, Adriamycin, ED 50 = 0.1μmol/L, ED 50 = 0.1μg/mL) [5088] 1, 1, 1a, 2, 3, 3a, 3b, 4, 6, 3] anti-gonadotropin; cytotoxic (KB in vitro, EC = 15μg/mL); antitussive (dispels phlegm); diuretic; inhibits release and metabolism of arachidonic acid; aldose reductase inhibitor (mus eye lens, 100μmol/L, InRt = 100%); ∆(5)-lipoxygenase inhibitor; NADH oxidase inhibitor; succinic oxidase inhibitor; inhibits degranulation and release of β-hexosaminidase (RBL-2H3 cells, IC 50 50 = 82μmol/L, p<0.01, did not affect the enzyme activity of β-hexosaminidase) [4163] ; DPPH scavenger (IC 50 = (16.0±0.4)μmol/L, control Trolox, IC 50 = (25.4±0.8)μmol/L) [4244] ; LD (rbt, sc) = 8~10g/kg. Source (62.6±1.0)%, did not affect the enzyme activity of β-hexosaminidase) [4163] ; hepatoprotective (primary cultures of rat hepatocytes, H 2 O 2 -induced toxicity, 50μmol/L, relative protection = 24.6% (H 2 O 2 -treated, relative protection = 0.0%, control, relative protection = 100%), positive control Silibinin, Relative protection = 74.9%) [4996] ; inhibits cell proliferation of PBMC (activated by phytohemagglutinin (PHA), IC 50 = 75.6μmol/L, inhibitory mechanism may involve the blocking of IL-2 and IFN-γ production) [4100] [607-91-0] C 11 H 12 O 3 (192.22) . bp 157ºC/21mmHg, 149.5ºC/15mm; 95~97ºC/0.2mmHg. Pharm: Antineoplastic (mus lung tumor, InRt = 65%, stomach tumor InRt = 31%); antifungal (Cladosporium cucumerinum in vitro, MED = 20μg); hallucinogen (normal hmn); induces activity of cytochrome system (rat, ip, 500μmol/kg, improves liver P450-1A1/2, 2B1/2 and 2E1 activity by 2~20 times); antioxidant (mus liver, inhibits lipid peroxidization); platelet aggregation inhibitor (rbt, in vitro); monoamine oxidase inhibitor (in vitro); larvacide (larva of Stegomyia calopus, 100% killed in 24h, 25mg/L); teratogen. Source: DA CAO KOU Alpinia speciosa, GAO BEN Ligusticum sinense (root and rhizome: content = 11.31%) [ Colorless amorphous powder Colorless amorphous powder Source: KU DING CHA DONG QING Ilex kudingcha. Ref: 5504. (6R)-6-Hydroxyl-7-octenoic acid 6-O-β-D-xylopyranosyl-(1'''-→6'')-O-β-D-glucopyranosyl-(1''→2')-O-β-D-glu Streptococcus mutans, MIC > 125μg/mL Pale yellow amorphous powder. Pharm: Antioxidant (DPPH scavenger, IC 50 = 17.9μg/mL, control Gallic acid Cytochrome-C reduction, IC 50 = 17.5μg/mL, control Gallic acid Source: BAI GUO YE Ginkgo biloba. Ref: 5239 (1→6)-β-D-glucopyran osyl]-21-O-{(6S)-2-trans-2-hydroxymethyl-6-methyl-6-O-(2-O-[(6S)-2-trans-2,6-dimethyl-6-O-β-D-quinovopyranosyl-2,7-octadienoyl]-β-D-quinovopyranosyl-2,7-octadienoyl)-acacic acid 28-O-β-D-glucopyranosyl Source: GE GEN Pueraria lobata Pueraria thunbergiana Colorless needles (petroleum ether-acetone), mp (776.84). Colorless needles (petroleum ether-ethyl acetate), mp (657.72). Colorless needles (petroleum ether-ethyl acetate) Pharm: cAMP phosphodiesterase inhibitor (in vitro, IC 50 = 31μmol/L) Ref: 2, 972, 1007, 1135, 1156, 5409 Ref: 2 Crystals (CHCl -MeOH), mp 207~209ºC, [α] Off-white amorphous powder Source: (rat, sc, strengthens ephedrine-induced spontaneous motion) Source: HAI BIN LIU CHUAN YU Linaria japonica. Ref: 652. nosyl-(1→4)-β-D-digitoxopyranosyl-(1→4)-β-D-digitoxopyranoside C 46 H 74 O 17 (899.09). Amorphous powder Ref: 3925. 3α-Hydroxy-5β-cholan-24-oic acid [434-13aq.), mp 186ºC Pharm: Antibacterial (Staphylococcus aureus, MIC = 12.5μg/mL Source: CHANG GUAN XIANG CHA CAI C 36 H 58 O 9 (634.86). Amorphous powder, mp 198~202ºC InRt = 70.45%); cell viability (hmn isolated neutrophils, 12.5μg/mL, cell viability = 78.81%, 50μg/mL, cell viability = 100%, 200μg/mL, cell viability = 68.85%). Source: SONG LUO Usnea longissima Amorphous powder Amorphous powder Pharm: Cytotoxic (inhibition growth of hmn tumor cell lines, MCF7 (breast) Source: MAO GUO SUAN PAN ZI Glochidion eriocarpum (root and stem wood) 2º (c = 0.06, MeOH); colorless prisms (Me 2 CO-CH 3 OH), mp 216~218ºC 1→3)-α-L-rhamnopyranosyl(1→2)-α-L-arabinopyra nosyl hederagenin 28-O-β-D-glucopyranosyl(1→6)-β-D-glucopyranosyl ester C 59 H 96 O 27 (1237.41). White clustered crystals, mp 229~232ºC white granular Crystals (methanol), mp 218~220ºC Source: QIN JIAO Gentiana macrophylla. (25R)-26-O-β-D-Glucopyranosyl-22-methoxy-5β-furost-2β White amorphous powder, mp 206~208ºC. Source: XIE BAI Allium macrostemon Pharm: Induces gene expression changes (hmn fibroblast, IC 90 > 400μg/mL) Ref: 2, 6, 1521 Source: JIN ZHAN JU Calendula officinalis (flower) 2-{4-[1-(1H-Indol-2-yl)-vinyl]-1-methyl-piperidin-3-ylidene}ethanol C 18 H 22 N 2 O (282.39) Crystals (dichloromethane-ether), mp C 30 H 48 O 3 (456.72). Pharm: DPPH scavenger inactive (for 40μmol/L DPPH radical Ref: 4378. 3β-Acetoxy-6α,15β,17-trihydroxy-11β,16β-epoxy-ent-kaurane C 22 H 34 O 6 (394.51). Colorless crystals, mp 124~126ºC Colorless crystals (acetone), mp 115~118ºC Antitrypanosomal (in vitro, epimastigotes of Trypanosoma cruzi, MLC = 3.1μmol/L vitro, epimastigotes of Trypanosoma cruzi, MLC = Antitrypanosomal (in vitro, epimastigotes of Trypanosoma cruzi Amorphous powder isolated from the plant for the first biserrata Pharm: Antifungal (plant pathogenic fungus Pyricularia oryzae Source SU MU Caesalpinia sappan (heartwood) Pharm: Cytotoxic (P 388 cell line ED 50 = 0.08μg/mL) [5405] ; cytotoxic (Colon26-L5, ED 50 = 84.2μmol/L; HT1080, ED 50 > 100μmol/L) [3042] ; cytotoxic inactive (in vitro, HONE-1 and NUGC cancer cell lines Source: HUANG GUA Cucumis sativus (leaf) [4727] , JIA BAI HE Notholirion hyacinthinum Pharm: Antiproliferative and cytotoxic (in vitro, L-929 3'-di-O-acetyl)-3'-α-rhamnoside C 25 H 22 O 14 (546.45). Needles (MeOH), mp 217~218ºC yellow amorphous solid ); antibacterial (in vitro, Babesia gibsoni, IC 50 = 28.5μg/mL 60μg/mL Source: DU HUO Angelica pubescens f. biserrata Pale yellow needle-shaped crystals MLC = 0.2mg/L). kaur-16-en-19-oate C 26 H 38 O 6 (446.59). Colorless needles, mp 108ºC Pharm: Leukotriene biosynthesis Inhibitor (in vitro 68±0.44)μmol/L, control Kojic acid, = (97.61±1.73)μmol/L, control Eserine = (3.68±0.02)μmol/L) 69±0.13)μmol/L, control Eserine Colorless needles (CHCl ), mp 124~125ºC vitro Plasmodium falciparum: D6, IC = 11.67ng/mL Source: DU HUO Angelica pubescens f. biserrata C 58 H 96 O 28 (1241.40). White powder, mp 234ºC (dec) dioeca (herbaceous twigs: mean content = trace mp 175~176ºC. Source: DAN SHEN Salvia miltiorrhiza Pharm: Antineoplastic (ox brain, tubulin (484.46). Off-white amorphous powder Source: DU HUO Angelica pubescens f. biserrata Crystals (CH Cl -Et O) Source: Miliusa balansae (branch and leaf: yield = 0.00065%dw) Source: SU MI CAO Mollugo pentaphylla C 16 H 22 O 11 (290.35). mp 175ºC (dec) Pharm: Antidiarrheal (mus Colorless waxy solid ED 50 > 20μg/mL; U-87-MG, ED 50 > 20μg/mL; CAKI, ED 50 > 20μg/mL; PC3, ED 50 > 20μg/mL; 1A9 (3 day), ED 50 > 10μg/mL Ca 2+ from CaCl 2 , in vitro: A549, ED 50 = 7.4μg/mL; MCF7, ED 50 = 5.5μg/mL; HCT8, ED 50 = 12.3μg/mL ED 50 = 13.9μg/mL; U-87-MG, ED 50 = 14.2μg/mL; CAKI, ED 50 = 14.2μg/mL ED 50 = 4.5μg/mL; PTX10 (6 day), ED 50 = 2.8μg/mL). Source: SHAN 0.36μg/mL). Source: SHAN FAN LI ZHI Annona montana (seed) Source: SHAN FAN LI ZHI Annona montana (seed) Source: SHAN FAN LI ZHI Annona montana (seed) Pharm: Antioxidant (DPPH scavenger, 10μmol/L, ScRt = 51%, control BHT, 10μmol/L, ScRt = 43%) antibacterial (Staphylococcus aureus ATCC 25923, MIC > 128μg/mL, control Vancomycin, MIC = 2μg/mL Ref: 6, 4422, 5319. O O O OH crystals, mp 254ºC, [α] inhibits cytokines formation, including TNF-α, IL-4, IL-2 and IFN-γ in hmn O (428.48). Colorless crystals, mp 180~183ºC VSE) (= ATCC19434), MIC = 6.25μg/mL, control Linezolid VanA), MIC = 3.13μg/mL, Linezolid, MIC = 0.78μg/mL 13μg/mL, Linezolid, MIC = 0.78μg/mL; Enterococcus faecium JCM5804 (VSE) (= ATCC 29212), MIC = 6.25μg/mL 56μg/mL; Enterococcus faecium JU1858 (VRE, VanA), MIC = 6.25μg/mL, Linezolid, MIC = 0.78μg/mL 13μg/mL, Linezolid, MIC = 1.56μg/mL 56μg/mL 56μg/mL Pharm: Laxative (mus, ED 50 = 30mg/kg, a large intestine laxative agent similar to sennoside A) Cerasus japonica Source: GUANG JING QIAN CAO Rubia wallichiana (stem) 135ºC. Pharm: Platelet aggregation inhibitor (washed rabbit platelets 0±3.1)%, control, AggRt = (77.0±1.5)%; collagen = 10μg/mL PAF = 1ng/mL, AggRt = (77.0±2.9)%, control, AggRt = (82.5±1.5)%) [5417] . Source: JIU LI XIANG Murraya paniculata Pharm: Antitussive (mouse, fog-ammonia method, 800mg/kg, perfusion in stomach, cough time of half the animals increased by 135%); dispels phlegm (mus, phenol red method, 400mg/kg and 800mg/kg, perfusion in stomach LD 50 (mus, orl) ≥ 4.8g/kg. Source: CHAI HU Bupleurum HUANG HAO Artemisia scoparia MU XU Medicago sativa, TAI WAN CUI BAI Calocedrus macrolepis var. formosana (leaf) Ref: 4174. (202.34). Colorless oil. chinense, DU HUO Angelica pubescens f. biserrata LUO XIAO 15μmol/L, control Epalrestat .9±1.4)%, control Curcumin, 100μmol/L, InRt = 100μmol/L, InRt = (−13.1±3.6)%, control Curcumin, 100μmol/L, InRt = = 23μmol/L, control Curcumin, IC . Source: YANG MEI SHU PI Myrica rubra (bark: β-hexosaminidase Colorless plates (CH Cl ), mp 141~143ºC C 17 H 21 NO 3 (287.36