General

Scientific Names: Scutellaria baicalensis Georgi.

Common Names: Huang Qin, Huang Jin Cha, Shan Cha Gen, Lan Xin Cao.

 

BOTANICAL:

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来 源： 为唇形科植物黄芩Scutellaria baicalensis Georgi 的干燥根。

植物特征： 多年生草本。茎丛生，具细条纹，近无毛或被上曲至开展的微柔毛。叶对生，披针形至条状披针形，全缘，下面密被下陷的腺点。总状花序顶生，花偏生于花序一侧；花萼二唇形，盾片高约1.5mm，果时增大；花冠紫色、紫红色至蓝紫色，花冠筒近基部明显膝曲；雄蕊4，二强。小坚果卵球形，黑褐色，具瘤。花期7～8月，果期8～9月。

资源分布:生于向阳草地山坡及休荒地上。主产河北、山西、内蒙古。

生药材鉴定： 干燥根呈倒圆锥形，扭曲不直。表面深黄色或黄棕色。上部皮较粗糙而下部皮细，上下均有稀疏的疣状支根痕。质硬而脆，易折断；断面深黄色，中间有棕红色圆心。以条粗长、质坚实、色黄、除净外皮者为佳。

 

 

Pharmacology

化学成分: 根含黄芩甙（baicalin）4.0％－5.0％、黄芩素（baicalein）、汉黄芩甙（wogonoside）、汉黄芩素（wogonin）、黄芩新素(neobaicalein)、7－甲氧基黄芩素（7-methoxybaicalein）、 7－甲氧基去甲基汉黄芩素（7-methoxynorwogonin）、木蝴蝶素A(oroxylin A)、黄芩黄酮 Ⅰ(skullcapflavoneⅠ,5,2ˊ-二羟基-6,8-二甲氧基黄酮)、 黄芩黄酮Ⅱ(skullcapflavone Ⅱ,5,2ˊ-二羟基-6,7，8，6ˊ-四甲氧基黄酮)。黄芩黄酮Ⅰ结构现修订为黄芩黄酮Ⅰ5,2ˊ -二羟基-7,8-二甲氧基黄酮。另报道尚含木蝴蝶素A葡萄糖醛酸甙、5,7-二羟基-6,8，2ˊ， 3ˊ-四甲氧基黄酮、5,8，2ˊ-三羟基-7-甲氧基黄酮（5,8，2ˊ-trihydroxy-7- methoxyflavone）、5,8，2ˊ-三羟基-6，7-二甲氧基黄酮（5,8，2ˊ-trihydroxy-6,7- dimethoxyfla-vone）、5,7，4ˊ-三羟基-6-甲氧基黄酮（5,7，4ˊ-trihydroxy-6- methoxyflavone）、二氢木蝴蝶素A（dihydroorox-ylin A）和白杨素（chrysin）。此外。尚含β-谷甾醇、豆甾醇、菜油甾醇和苯甲酸。

 

 

Efficacy

Scutellaria baicalensis is a widely used Chinese herbal medicine that has been used historically in anti-inflammatory and anticancer therapy. The purpose of this study is to verify its anticancer activity on head and neck squamous cell carcinoma (HNSCC) in vitro and in vivo and to investigate its effect on cyclooxygenase-2 (COX-2), which converts arachidonic acid to prostaglandin E(2) (PGE(2)) and is highly expressed in HNSCC. Two human HNSCC cell lines (SCC-25 and KB) and a nontumorigenic cell line (HaCaT) were tested in vitro for growth inhibition, proliferation cell nuclear antigen expression, and COX-2 activity and expression after treatment with Scutellaria baicalensis extract. Its effects were compared with those of baicalein (a flavonoid isolated from Scutellaria baicalensis), indomethacin (a nonselective COX inhibitor), and celecoxib (a selective COX-2 inhibitor). Four nude mice with s.c. inoculation of KB cells were tested for its anticancer activity in vivo by oral administration of Scutellaria baicalensis at a dose of 1.5 mg/mouse (75 mg/kg), five times/week for 7 weeks. Scutellaria baicalensis and other agents demonstrated a strong growth inhibition in both tested human HNSCC cell lines. No growth inhibition of HaCaT cells was observed with Scutellaria baicalensis. The IC(50)s were 150 micro g/ml for Scutellaria baicalensis, 25 micro M for celecoxib, and 75 micro M for baicalein and indomethacin. Scutellaria baicalensis, as well as celecoxib and indomethacin, but not baicalein, suppressed proliferation cell nuclear antigen expression and PGE(2) synthesis in both cell types. Scutellaria baicalensis inhibited COX-2 expression, whereas celecoxib inhibited COX-2 activity directly. A 66% reduction in tumor mass was observed in the nude mice. Scutellaria baicalensis selectively and effectively inhibits cancer cell growth in vitro and in vivo and can be an effective chemotherapeutic agent for HNSCC. Inhibition of PGE(2) synthesis via suppression of COX-2 expression may be responsible for its anticancer activity. Differences in biological effects of Scutellaria baicalensis compared with baicalein suggest the synergistic effects among components in Scutellaria baicalensis. (source)

Baicalein is a flavonoid extracted from the root of Scutellaria baicalensis Georgi, a medicinal plant traditionally used in Oriental medicine. Baicalein exerts either proapoptotic or anti-apoptotic effects in different cell types. Baicalein prevented loss of cell viability and apoptosis induced by cisplatin in a dose-dependent fashion over the concentrations of 2-10 microM. Exposure of cells to baicalein without cisplatin did not affect cell viability. Western blot analysis demonstrated that cisplatin induced activation of extracellular signal-regulated kinase (ERK), which was not affected by baicalein. Baicalein prevented Bax expression, mitochondrial depolarization, cytochrome c release from mitochondria, and caspase activation induced by cisplatin. Taken together, these findings suggest that baicalein prevents cisplatin-induced apoptosis through inhibition of the mitochondrial depolarization in human glioma cells. (source)

We used high-performance liquid chromatography to fractionate S. baicalensis and identified four compounds capable of inhibiting prostate cancer cell proliferation; baicalein, wogonin, neobaicalein, and skullcapflavone. Comparisons of the cellular effects induced by the entire extract versus the four-compound combination produced comparable cell cycle changes, levels of growth inhibition, and global gene expression profiles (r(2) = 0.79). Individual compounds exhibited antiandrogenic activities with reduced expression of the androgen receptor and androgen-regulated genes. In vivo, baicalein (20 mg/kg/d p.o.) reduced the growth of prostate cancer xenografts in nude mice by 55% at 2 weeks compared with placebo and delayed the average time for tumors to achieve a volume of approximately 1,000 mm(3) from 16 to 47 days (P < 0.001). Most of the anticancer activities of S. baicalensis can be recapitulated with four purified constituents that function in part through inhibition of the androgen receptor signaling pathway. We conclude that clinical studies evaluating the efficacy of these agents in the context of chemoprevention or the treatment of prostate cancer are warranted. (source)

The study is to verify the inhibitory effect of a chemically standardized extract from Scutellariae radix in liver cancer cell lines (HepG2). The botanical extract was prepared using pressurized liquid extraction (PLE). A method using proteolytic digest with single dimensional and two-dimensional liquid chromatography with tandem mass spectrometry was used to characterize differential protein expression in mammalian cells in response to the botanical extract. The whole cell lysates were digested with trypsin, and the peptides were separated by one-dimensional (reversed phase) or by two-dimensional (cation exchange and reversed phase) solid-phase extraction (SPE) cleanup and separated by liquid chromatography with UV detection and mass spectrometry. In the presence of the botanical extracts, drug-induced apoptosis was not observed, and a number of proteins that played an important role in the metabolic pathways in HepG2 cell line had been affected. The data, as presented, suggest that the inhibitory effects of the standardized extracts from Scutellariae radix resulted from expression of heat shock protein and other proteins related to energy metabolism. The proposed platform had the potential to provide significant information about the particular proteome such as human hepatoma HepG2. At the molecular level, it was possible to study the proteins and how their levels and modifications change in response to the effects of the botanical extract. (source)

Cisplatin at 3 mg/kg induced significant pica accompanied by reduced food intake, suggesting the presence of nausea. Hence, this cisplatin dose was selected for testing the antinausea activity of SbE. Cisplatin-induced pica decreased significantly when animals were pretreated with SbE at doses of 1 mg/kg and 3 mg/kg ( P<0.01). At a higher SbE dose (10 mg/kg), kaolin consumption increased, rather than further decreased, and was significantly different from that in the groups treated with low SbE doses. CONCLUSIONS: SbE pretreatment decreased cisplatin-induced kaolin intake in the rat model of simulated nausea, suggesting that SbE and its active constituent(s) may play a therapeutic role in chemotherapy-induced emesis. Absence of therapeutic effect at the highest tested SbE dose could have been a result of prooxidant activity often associated with excess antioxidant concentration. (source)

IN VITRO:

  1. Hu Z, et al., Herb-drug interactions: a literature review. Drugs. 2005; 65(9):1239-82.
  2. Lee SW, et al., Beneficial effect of flavonoid baicalein in cisplatin-induced cell death of human glioma cells. Neurosci Lett. 2005 Jul 1-8; 382(1-2):71-5. Epub 2005 Mar 21.
  3. Bonham M, et al., Characterization of chemical constituents in Scutellaria baicalensis with antiandrogenic and growth-inhibitory activities toward prostate carcinoma. Clin Cancer Res. 2005 May 15; 11(10):3905-14.
  4. Ong ES, et al., Differential protein expression of the inhibitory effects of a standardized extract from Scutellariae radix in liver cancer cell lines using liquid chromatography and tandem mass spectrometry. J Agric Food Chem. 2005 Jan 12;53(1):8-16.
  5. Lee Y, et al., Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. J Med Chem. 2004 Oct 21; 47(22):5555-66.
  6. Ciesielska E, et al., In vitro antileukemic, antioxidant and prooxidant activities of Antoksyd S (C/E/XXI): a comparison with baicalin and baicalein. In Vivo. 2004 Jul-Aug; 18(4):497-503.
  7. Ha KT, et al., Inhibitory effect of Sihoga-Yonggol-Moryo-Tang on matrix metalloproteinase-2 and -9 activities and invasiveness potential of hepatocellular carcinoma. Pharmacol Res. 2004 Sep; 50(3):279-85.
  8. Ye F, et al., Inhibition of cyclooxygenase-2 activity in head and neck cancer cells by genistein. Cancer Lett. 2004 Jul 28; 211(1):39-46.
  9. Sonoda M, et al., Cytotoxic activities of flavonoids from two Scutellaria plants in Chinese medicine. J Ethnopharmacol. 2004 Mar; 91(1):65-8.
  10. Cheng KT, et al., Baicalin induces differential expression of cytochrome C oxidase in human lung H441 cell. J Agric Food Chem. 2003 Dec 3; 51(25):7276-9.
  11. Zhang DY, et al., Inhibition of cancer cell proliferation and prostaglandin E2 synthesis by Scutellaria baicalensis. Cancer Res. 2003 Jul 15; 63(14):4037-43.
  12. Ciesielska E, et al., Anticancer, antiradical and antioxidative actions of novel Antoksyd S and its major components, baicalin and baicalein. Anticancer Res. 2002 Sep-Oct; 22(5):2885-91.
  13. Martin J, et al., [The Baikal scullcap (Scutellaria baicalensis Georgi)--a potential source of new drugs], Ceska Slov Farm. 2002 Nov; 51(6):277-83. Review. Czech.
  14. Ye F, et al., Anticancer activity of Scutellaria baicalensis and its potential mechanism. J Altern Complement Med. 2002 Oct; 8(5):567-72.
  15. Hsieh TC, et al., Prevention and management of prostate cancer using PC-SPES: a scientific perspective. J Nutr. 2002 Nov; 132(11 Suppl):3513S-3517S.
  16. Chang WH, et al., Different effects of baicalein, baicalin and wogonin on mitochondrial function, glutathione content and cell cycle progression in human hepatoma cell lines. Planta Med. 2002 Feb; 68(2):128-32.
  17. Hsieh TC, et al., Mechanism of action of herbal supplement PC-SPES: elucidation of effects of individual herbs of PC-SPES on proliferation and prostate specific gene expression in androgen-dependent LNCaP cells. Int J Oncol. 2002 Mar; 20(3):583-8.
  18. Chan FL, et al., Induction of apoptosis in prostate cancer cell lines by a flavonoid, baicalin. Cancer Lett. 2000 Nov 28; 160(2):219-28.
  19. Park HJ, et al., Induction of quinone reductase by a methanol extract of Scutellaria baicalensis and its flavonoids in murine Hepa 1c1c7 cells. Eur J Cancer Prev. 1998 Dec; 7(6):465-71.
  20. Kyo R, et al., Effects of Sho-saiko-to, San'o-shashin-to and Scutellariae Radix on intracellular Ca2+ mobilization in C6 rat glioma cells. Biol Pharm Bull. 1998 Oct; 21(10):1067-71.
  21. Kyo R, et al., Baicalin and baicalein, constituents of an important medicinal plant, inhibit intracellular Ca2+ elevation by reducing phospholipase C activity in C6 rat glioma cells. J Pharm Pharmacol. 1998 Oct; 50(10):1179-82.
  22. Razina TG, et al., [A semisynthetic flavonoid from the Baikal skullcap (Scutellaria baicalensis) as an agent to enhance the efficacy of chemotherapy in experimental tumors]. Eksp Klin Farmakol. 1998 Mar-Apr; 61(2):54-6. Russian.
  23. Smolianinov ES, et al., [Effect of Scutellaria baicalensis extract on the immunologic status of patients with lung cancer receiving antineoplastic chemotherapy], Eksp Klin Farmakol. 1997 Nov-Dec; 60(6):49-51. Russian.
  24. Goldberg VE, et al., [Dry extract of Scutellaria baicalensis as a hemostimulant in antineoplastic chemotherapy in patents with lung cancer]. Eksp Klin Farmakol. 1997 Nov-Dec; 60(6):28-30. Russian.
  25. Konoshima T, et al., Studies on inhibitors of skin tumor promotion. XI. Inhibitory effects of flavonoids from Scutellaria baicalensis on Epstein-Barr virus activation and their anti-tumor-promoting activities. Chem Pharm Bull (Tokyo). 1992 Feb; 40(2):531-3.
  26. Razina TG, et al., [The role of thrombocyte aggregation function in the mechanism of the antimetastatic action of an extract of Baikal skullcap]. Vopr Onkol. 1989; 35(3):331-5. Russian.
  27. Razina TG, et al., [Enhancement of the selectivity of the action of the cytostatics cyclophosphane and 5-fluorouracil by using an extract of the Baikal skullcap in an experiment]. Vopr Onkol. 1987; 33(2):80-4. Russian.

IN VIVO:

  1. Aung HH, et al., Scutellaria baicalensis extract decreases cisplatin-induced pica in rats. Cancer Chemother Pharmacol. 2003 Dec; 52(6):453-8. Epub 2003 Aug 27.
  2. Zhang DY, et al., Inhibition of cancer cell proliferation and prostaglandin E2 synthesis by Scutellaria baicalensis. Cancer Res. 2003 Jul 15; 63(14):4037-43.

 

Safety

用药忌宜: 脾肺虚热者忌之。 《本草经疏》：“脾肺虚热者忌之。凡中寒作泄，中寒腹痛，肝肾虚而少腹痛，血虚腹痛，脾虚泄泻，肾虚溏泻，脾虚水肿，血枯经闭，气虚小水不利，肺受寒邪喘咳，及血虚胎不安，阴虚淋露，法并禁用。”

　
   
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