Static acid   中文名称: 斑点酸

Natural product; secondary metabolite

从地衣Lobaria pulmonaria（L.）Hoffm中分离出的次生代谢产物Stictic acid的生长抑制作用。首次在三种人细胞系上对Lobariaceae进行了体外评估。细胞系HT-29和MCF-7用于测量Stitic酸对癌症细胞的活性，而细胞系MRC-5用于估计其对正常细胞的作用。结果表明，刺参酸具有中等抗癌活性（细胞系HT-29的IC50值为29.29μg/ml），对非恶性细胞的生长抑制作用较低（细胞系MRC-5的IC50值是2478.40μg/ml）。这种天然产物可以被认为是设计新型人类结肠腺癌药物的有前景的先导化合物[1]。

MTT测试[1]
通过四唑比色MTT法评估生长抑制。将细胞接种到96孔微量滴定板中，每孔体积为90μl，在完整的培养基中，最佳接种密度为每孔5×103个细胞，以确保整个测定期间的对数生长率。将浓度在10-8μg至10-4M范围内的受试物质（Stictic acid）添加到除对照孔外的所有孔中。将培养板在37°C下孵育48小时。在孵育期结束前3小时，向所有孔中加入10μl MTT溶液（5mg/ml），在37°℃下孵育3小时，然后通过抽吸去除培养基和MTT。然后将甲赞产物溶解在100μl 0.04 M HCl的异丙醇中。在室温下放置几分钟后，在540/690nm的分光光度计板读数器上读取板。不含完全培养基和MTT的细胞孔仅作为空白。生长抑制以百分比表示，并根据以下公式计算：%C=1−（ODtest/ODcontrol）×100。

[1]. Stictic acid inhibits cell growth of human colon adenocarcinoma HT-29 cells. Arabian Journal of Chemistry. Volume 10, Supplement 1, February 2017, Pages S1240-S1242.

LSM-4387 is an aromatic ether.
Stictic acid has been reported in Dimelaena oreina, Ramalina hierrensis, and other organisms with data available.

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In comparison, the lichen substances such as atranorin, gyrophoric acid, parietin and usnic acid were less active toward the cell line HT-29 (IC50 values >200,>200,>200 and 99.70 ± 8.40 μg/ml, respectively) after 72 h exposition (Bačkorová et al., 2011). Furthermore, through investigation of the mechanisms of cytotoxicity of these four secondary metabolites, the same research group found that usnic acid and atranorin were more effective anticancer compounds on HT-29 cells compared to parietin and gyrophoric acid (Bačkorová et al., 2012). However, our results indicate that stictic acid, a widely distributed depsidone among lichens, can be considered as a more promising lead compound for the design of novel human colon adenocarcinoma drugs in relation to usnic acid and atranorin. Hence, structure–activity relationship (SAR) of stictic acid and its derivatives is worthy of investigation.[1]

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In summary, it may be concluded that stictic acid is more effective anticancer compound on the malignant HT-29 cell line than usnic acid, the most extensively studied lichen metabolite till date (Mitrović et al., 2011). Among the rest, further work should be focused on the molecular mechanism by which this depsidone induces the aforementioned growth inhibition. Taken together, it seems reasonable to assume that stictic acid may inspire new drugs for the treatment of colorectal tumors which are still among the most common and lethal types of cancer worldwide (Botteri et al., 2008).[1]

C19H14O9

386.31

386.064

C, 59.07; H, 3.65; O, 37.27

549-06-4

73677

White to off-white solid powder

1.591g/cm3

744.1ºC at 760mmHg

273.2ºC

1.692

2.316

128.59

2

9

2

28

666

0

SKCUFZLDTAYNBZ-UHFFFAOYSA-N

InChI=1S/C19H14O9/c1-6-4-9(25-3)8(5-20)15-10(6)17(22)27-14-7(2)13(21)11-12(16(14)26-15)19(24)28-18(11)23/h4-5,19,21,24H,1-3H3

13,17-dihydroxy-5-methoxy-7,12-dimethyl-9,15-dioxo-2,10,16-trioxatetracyclo[9.7.0.03,8.014,18]octadeca-1(11),3(8),4,6,12,14(18)-hexaene-4-carbaldehyde

STICTIC ACID; 549-06-4; NSC-87511; NSC87511; NSC 87511; NZR6AX77LP; 1,3-Dihydro-1,4-dihydroxy-10-methoxy-5,8-dimethyl-3,7-dioxo-7H-isobenzofuro(4,5-b)(1,4)benzodioxepin-11-carboxaldehyde; 13,17-Dihydroxy-5-methoxy-7,12-dimethyl-9,15-dioxo-2,10,16-trioxatetracyclo[9.7.0.03,8.014,18]octadeca-1(11),3(8),4,6,12,14(18)-hexaene-4-carbaldehyde;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。