mic-10

Mahanimbine 存在于Murraya koenigii 的根、叶和茎中，是从Murraya koenigii 中的提取的一种具有口服活性的生物碱。Mahanimbine 具有乙酰胆碱酯酶抑制活性，可抑制了高脂肪饮食（HFD）引起的小鼠代谢并发症的发展，对科尼氏分枝杆菌叶对链脲佐菌素诱导的糖尿病大鼠胰腺β细胞组织病理学变化有作用。

Chlamydia pneumoniae-IN-1 是一种对衣原体有抑制作用的苯并咪唑类化合物，在低浓度下即可对肺炎衣原体产生抑制作用。Chlamydia pneumoniae-IN-1 具有抗菌活性，对CV-6菌株的 MIC 为12.6 μM，可用于研究肺部感染。

Quinine sulfate dihydrate 在钾通道阻滞剂中起主要作用。它也被用作抗疟疾、抗胆碱能、抗高血压和降糖药。它抑制线粒体atp 调节的钾通道。它也被用来研究生物结晶血红素，血红素，在疟疾寄生虫的代谢和研究血红素(FP)复合物的毒性。

2,6-Dichlorodiphenylamine 是双氯芬酸钠的一种结构类似物，显示出抗白色念珠菌活性。2,6-Dichlorodiphenylamine 是非选择性抗炎剂，为COX 的抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC50分别为 4 和 1.3 nM。

ALPHA-PINENE ((-)-Alpha-Pinene) 是一种双环单萜，存在于松树和其他植物中，包括具有多种生物活性的大麻。它减少了 7 种革兰氏阳性菌、7 种革兰氏阴性菌和 8 种酵母菌株的生长，MIC 值分别为 0.75-1.29、1.05-1.59 和 0.7-1.17%。它对 C. molestus 幼虫具有杀虫活性，LC50 值范围为 47 至 49 mg L。它(100 μg ml) 可诱导细胞凋亡，增加阴离子超氧化物的产生和 DNA 片段化，并激活 B16 中的 caspase-3 F10 黑色素瘤细胞 。在 B16 F10 小鼠异种移植模型中，它（100 ml 的 10 mg ml 溶液）可将转移性肺结节的数量减少约 7 倍。它（8.6 mg L，气溶胶）还使小鼠在高架十字迷宫的张开臂​​中花费的时间增加了大约 2 倍，表明具有抗焦虑活性。

TunR2 is an antibiotic and derivative of tunicamycin .1It is active againstB. subtilis(MIC = 0.3 μg ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G againstB. subtiliswhen used at a concentration of 0.4 μg ml. Unlike tunicamycin, TunR2 is non-toxic toS. cerevisiae(MIC = >10 μg ml) and does not inhibit glycosylation in a protein N-glycosylation assay. TunR2 also has reduced antiproliferative activity against MDA-MB-231 and CHO cells compared with tunicamycin. 1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg ml) and Kurono (MIC: 0.0005 μg ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1 2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg kg to 2.5 mg kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Leucomycin A13 is a macrolide antibiotic and a component of the leucomycin complex originally isolated from S. kitasatoensis. It is active against B. subtilis, S. aureus, M. luteus, and E. coli with MIC values of 0.16, 0.16, 0.08 and >10 μg ml, respectively. It binds to ribosomes with an IC50 value of 1.2 μM in a radioligand binding assay.

Antifungalagent 85 (compound 24f)是一种抗真菌剂，对多种革兰氏阳性菌表现出良好的活性，其最小抑制浓度(MIC)范围为2.5 - 10?μM。

Im5 是一种具有针对 Escherichia coli、Staphylococcus aureus、Bacillus subtilis 的抗菌活性（MIC:10、2.5-5、0.5-1 μM)的抗菌肽，同时表现出溶血性（EC50: 28 μM）。

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone，为喹诺酮类生物碱，作用为二酰基甘油酰基转移酶抑制剂与血管紧张素II受体阻断剂，其IC50值依次为20.1 μM与34.1 μM。此化合物亦展现对幽门螺杆菌的有效抗活性，MIC值达10 μg mL。

IT-143A is a bacterial metabolite originally isolated fromStreptomycessp. IT-143.1It is active against the bacteriumM. luteus(MIC = 6.25 μg/ml) and the fungiA. fumigatusandT. rubrumin vitro(MICs = 12.5-25 μg/ml). 1.Urakawa, A., Sasaki, T., Yoshida, K., et al.IT-143-A and B, novel piericidin-group antibiotics produced by Streptomyces SpJ. Antibiot. (Tokyo)49(10)1052-1055(1996)

ent-8(14),15-pimaradien-3beta-ol (8(14),15-Isopimaradien-3-ol) can induce vascular relaxation. It displays high antibacterial activities (MIC values lower than 10 microg mL for most pathogens).

Glyasperin C acts as a partial estrogen antagonist, it shows tyrosinase inhibitory activity (IC (50) = 0.13 + - 0.01 microg mL), it could be a promising candidate in the design of skin-whitening agents. Glyasperin C shows potent anti-vancomycin-resistant

19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM.

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg ml) and induces efflux of potassium ions from B. subtilis without affecting Na+ K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg ml. It inhibits the growth of B. halodurans (MIC = 10 ng ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).

Peptide 5g 是一种具有广谱抗菌特性的化合物。它对 E. coli, S. aureus 和 C. albicans 的最小抑制浓度 (MIC) 值显著，分别为 30 μg mL、10 μg mL 和 12.5 μg mL。

Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4 1.Lopez, J.A.V., Nogawa, T., Futamura, Y., et al.Nocardamin glucuronide, a new member of the ferrioxamine siderophores isolated from the ascamycin-producing strain Streptomyces sp. 80H647J. Antibiot. (Tokyo)72(12)991-995(2019) 2.Ishida, S., Arai, M., Niikawa, H., et al.Inhibitory effect of cyclic trihydroxamate siderophore, desferrioxamine E, on the biofilm formation of Mycobacterium speciesBiol. Pharm. Bull.34(6)917-920(2011) 3.Kalinovskaya, N.I., Romaneko, L.A., Irisawa, T., et al.Marine isolate Citricoccus sp. KMM 3890 as a source of a cyclic siderophore nocardamine with antitumor activityMicrobiol. Res.166(8)654-661(2011) 4.Matsubara, K., Sakuda, S., Tanaka, M., et al.Morphological changes in insect BM-N4 cells induced by nocardamineBiosci. Biotechnol. Biochem.62(10)2049-2051(1998)

Cyclo(Pro-Gly) is an active metabolite of piracetam-N-phenylacetyl-L-prolylglycine (GWS-111), it shows a greater resistance to an enzymatic effect than natural neuropeptides. Cyclo-(Gly-Pro) shows cytotoxicity at the concentration of 10 umol L, it inhibit

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

(+)-δ-Cadinene 是一种从G. hirsutum 中发现的倍半萜，具有抗菌、杀虫、抗癌和抗增殖活性。 它对肺炎双球菌的MIC 值为31.25 μg ml，对 A. stephensi、A. aegypti 和 C. quinquefasciatust 三龄幼虫的LC50s 值分别8.23、9. 2和3。(+)-δ-Cadinene（10、50 和 100 μM）可诱导 OVCAR-3 人类卵巢癌细胞凋亡并抑制其增殖。

Kocurin is a thiazolyl peptide originally isolated fromK. palustrisand has antibiotic activity.1It is active against methicillin-resistantS. aureus(MRSA; MIC = 0.25 μg ml), as well asB. subtilisandE. faeciumin a solid agar test when used at a concentration of 8 μg ml. Kocurin is also active againstE. faecium,E. faecalis,S. epidermidis, and clinical isolates of vancomycin-resistant enterococci (MICs = 0.004-1.025 μg ml).2In vivo, kocurin (2.5, 5, and 10 mg ml) increases survival in a mouse model ofE. faecium-induced septicemia. It decreases the number of colony forming units (CFUs) in a mouse model of MRSA lung infection. 1.Martin, J., da S. Sousa, T., Crespo, G., et al.Kocurin, the true structure of PM181104, an anti-methicillin-resistant Staphylococcus aureus (MRSA) thiazolyl peptide from the marine-derived bacterium Kocuria palustrisMar. Drugs11(2)387-398(2013) 2.Mahajan, G., Thomas, B., Parab, R., et al.In vitro and in vivo activities of antibiotic PM181104Antimicrob. Agents Chemother.57(11)5315-5319(2013)

GLK-19是一种具抗大肠杆菌活性的抗菌肽（MIC: 10 μM）。

TP4（Nile tilapia piscidin）是一种piscidin样的抗菌肽，其口服活性被证实。此化合物对多种革兰氏阳性及阴性菌株均有效（MIC: 0.03-10 μg mL），并展现了溶血性。TP4还能增强免疫响应、提升抗氧化能力和改善肠道健康，助于防御细菌感染。除此之外，TP4显示抗肿瘤效果，并可通过激发癌细胞线粒体功能障碍导致坏死（necrosis）。