mic-3

L-161240 是一种与脂质A生物合成有关的抗菌剂，在DEACET测定IC50值为 30 nM，并且对野生型大肠杆菌的MIC值为1-3μg mL。

PF-04753299 是一种有效的、选择性的LpxC 抑制剂。PF-04753299 对淋球菌分离株具有杀菌作用，对大肠杆菌、铜绿假单胞菌和肺炎菌株的抑制的MIC90值分别为 2 μg ml、4 μg ml 和 16 μg ml。PF-04753299 用于革兰氏阴性菌感染的研究。

Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) 具有抗菌、抗氧化作用，有选择性和敏感性的荧光特性，广泛用作食品添加剂。它对 HSV-1，水泡性口炎病毒和脊髓灰质炎病毒有显著的抗病毒作用。

3-Nitropropanoic acid (Bovinocidin) 是一种琥珀酸脱氢酶的不可逆抑制剂。它对分枝杆菌有很强的抗菌活性，MIC 值为 3.3μM。

Methyl indole-3-carboxylate (Methyl 3-indolecarboxylate) 是一种从Sorangium cellulosumSoce895 菌株中分离出来的天然产物。它对革兰氏阳性诺卡氏菌的MIC 值为 33.3 μg mL。

DprE1-IN-11 (compound 3) 作为一种口服活性DprE1抑制剂，针对 MTB H37Rv 和 MDR-MTB 菌株显示出有效的抗结核活性，其最小抑菌浓度 (MIC) 范围为 <0.029-0.095 μM。

JAK05 对 Helicobacter pylori 具有抑制活性，能抑制 J63、J196 和 J107 菌株，其最低抑制浓度（MIC）为 3-5 µg mL。JAK05 对 H+ K+-ATPase、COX-1 2、TNF-α 和 PGE2 具有结合亲和力，具备抗氧化及抗炎特性。该化合物在大鼠乙醇诱发的胃溃疡模型中显示出抗溃疡活性。

Tribuloside (Tiliroside) A 是一种可从 Tribulus terrestris L 中分离得到的黄酮，可抑制非致病性分枝杆菌，MIC 值 为5.0 mg mL。

(+)-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。

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)

IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vitro and in vivo.1 |1. Minami, Y., Yoshida, K., Azuma, R., et al. Structure of a novel macrodiolide antibiotic IKD-8344. Tetrahedron Lett. 33(48), 7373-7376 (1992).|2. Hwang, E.I., Yun, B.S., Yeo, W.H., et al. Compound IKD-8344, a selective growth inhibitor against the mycelial form of Candida albicans, isolated from Streptomyces sp. A6792. J. Microbiol. Biotechnol. 15(4), 909-912 (2005).|3. Loutet, S.A., El-Halfawy, O.M., Jassem, A.N., et al. Identification of synergists that potentiate the action of polymyxin B against Burkholderia cenocepacia. Int. J. Antimicrob. Agents 46(4), 376-380 (2015).

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg ml). It induces apoptosis and cell cycle arrest at the G1 G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyagi, T., Aoyama, T., Kojima, F., et al.Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)45(9)1385-1390(1992) 3.Kakizaki, I., Ookawa, K., Ishikawa, T., et al.Induction of apoptosis and cell cycle arrest in mouse colon 26 cells by benastatin AJpn. J. Cancer Res.91(11)1161-1168(2000)

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).

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)

Nornidulin is a depsidone originally isolated from A. nidulans that has antibacterial activity against M. tuberculosis and M. ranoe as well as antifungal activity against T. tonsurans and M. audouini. It also inhibits the growth of methicillin-resistant S. aureus (MRSA; MIC = 2 μg ml) and has larvicidal activity toward Artemia (LC50 = 1.7 μg ml). Nornidulin has cytotoxic activity in MOLT-3 cells (IC50 = 35.7 μM) but not HuCCA-1, HepG2, or A549 cells (IC50s = >116.4 μM).

3-hydroxy Myristic acid methyl ester is a hydroxylated fatty acid methyl ester that has been found in E. camaldulensis and E. torelliana extracts. [1] It is active against M. tuberculosis (MIC = 49.5 μg ml) and is non-cytotoxic to Vero cells (IC50 = >100 μM). 3-hydroxy Myristic acid methyl ester is also a volatile compound that contributes to the aroma of red wild strawberries (F. pentaphylla) but is not present in cultivated strawberries (Fragaria x ananassa).[2] Reference：[1]. Lawal, T.O., Adeniyi, B.A., Adegoke, A.O., et al. In vitro susceptibility of Mycobacterium tuberculosis to extracts of Eucalyptus camaldulensis and Eucalyptus torelliana and isolated compounds. Pharm. Biol. 50(1), 92-98 (2012).[2]. Duan, W., Sun, P., Chen, L., et al. Comparative analysis of fruit volatiles and related gene expression between the wild strawberry Fragaria pentaphylla and cultivated Fragaria × ananassa. Eur. Food Res. Technol. 244(1), 57-72 (2018).

Previridicatumtoxin is a fungal metabolite that has been found inP. aethiopicumand has diverse biological activities.1,2It is an intermediate in the biosynthesis of the mycotoxin viridicatumtoxin . Previridicatumtoxin is active against methicillin-resistantS. aureus(MRSA) and vancomycin-resistantE. faecalis(IC50s = 4.4 and 4.8 μM, respectively), as well asC. albicansandS. cerevisiae(MIC = 32 μg ml for both).2,1It is cytotoxic to NCI H460, KB-3-1, and SW620 cancer cells (IC50s = 5.3, 4.1, and 6 μM, respectively).2 1.Chooi, Y.H., Wang, P., Fang, J., et al.Discovery and characterization of a group of fungal polycyclic polyketide prenyltransferasesJ. Am. Chem. Soc.134(22)9428-9437(2012) 2.Shang, Z., Salim, A.A., Khalil, Z., et al.Viridicatumtoxins: Expanding on a rare tetracycline antibiotic scaffoldJ. Org. Chem.80(24)12501-12508(2015)

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb MK cells (IC50 = 0.7 μg ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

Nidulin is a depsidone originally isolated from A. nidulans. It is active against the bacteria M. tuberculosis and M. ranoe, as well as the fungi T. tonsurans and M. audouini. It also inhibits the growth of methicillin-resistant S. aureus (MRSA; MIC = 4 μg ml) and has larvicidal activity toward Artemia (LC50 = 2.8 μg ml). Nidulin is cytotoxic to MOLT-3 cells (IC50 = 21.2 μM) but not HuCCA-1, HepG2, or A549 cells (IC50s = >112.7 μM). It inhibits aromatase with an IC50 value of 11.2 μM.

1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 |1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. 74(1), 111-115 (2008).|2. Fernández-Galicia, E., Calada, F., Roman-Romos, R., et al. Monoglycerides and fatty acids from Ibervillea sonorae root: Isolation and hypoglycemic activity. Planta Med. 73(3), 236-240 (2007).|3. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).

Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K., et al.Aquastatin A, an inhibitor of mammalian adenosine triphosphatases from Fusarium aquaeductuum. Taxonomy, fermentation, isolation, structure determination and biological propertiesJ. Antibiot. (Tokyo)46(11)1648-1657(1993) 2.Kwon, Y.-J., Fang, Y., Xu, G.-H., et al.Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611Biol. Pharm. Bull.32(12)2061-2064(2009) 3.Seo, C., Soh, J.H., Oh, H., et al.Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060Bioorg. Med. Chem. Lett.19(21)6095-6097(2009)

Tuberculosis inhibitor 3 (compound 2i)是一种高效和具有口服生物利用度的抗结核药物，对药敏和耐药结核分枝杆菌，M. tuberculosis H37RV与MDR-TB，体外抗药活性均为MIC < 0.016 μg mL。