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11

抑制剂 & 化合物

37

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T71289	9-O-Demethyltrigonostemone
	9-O-Demethyltrigonostemone is a natural IDO1 inhibitor, cytotoxic and antiplasmodial agent from the Roots of Strophioblachia fimbricalyx.
T25402	Fagaramide AI330755,AI3 30755,AI3-30755
	Fagaramide possesses Antiplasmodial activity.
T14656	Bis-propargyl-PEG3	Others	Others
	Bis-propargyl-PEG3 is a PEG-based PROTAC linker utilized for the synthesis of PROTACs. It is also employed in the synthesis of antiplasmodial zinc-dipicolylamine (ZnDPA) complexes[1] [2].
T75640	Thalifendine chloride
	Thalifendine chloride 是 Berberine 的一种代谢物，具有抗疟原虫和抗阿米巴虫活性。Thalifendine chloride 对 P. falciparum 和 E. histolytica 作用的 IC50值分别为 7.91 μM 和 116 μM。
T116970	TLC3407-3786
	MMV665916 是一种喹唑啉二酮衍生物，是一种抗疟药。MMV665916 对恶性疟原虫 FcB1 菌株具有显著的抗疟原虫生长抑制活性，EC50值为 0.4 μM，并呈现出高选择性指数 (SI>250)。
T79460	Antimalarial agent 28	Parasite	Microbiology/Virology
	Antimalarial agent 28 (Compound 2i)为具有针对P. berghei三个发育阶段活性的化合物。该化合物的IC50s针对肝期P. berghei为0.561 μM，对早期配子体为0.14 μM，以及对环期P. berghei为4.34 μM，表明其具有抑制该寄生虫的潜力。
T75536	Koshidacin B
	Koshidacin B为针对疟原虫的环四肽类化合物，其针对抗疟原虫(P. falciparum) FCR3和K1系的IC50值分别为0.89 μM与0.83 μM。此化合物在体内能有效抑制疟原虫，适用于疟疾感染的科学研究。
T60998	Anticancer agent 75
	Anticancer agent 75 具有良好的抗疟原虫活性。Anticancer agent 75 是有效的抗癌剂，在癌细胞系中表现出细胞毒性和选择性。Anticancer agent 75 对正常人肾细胞系的细胞毒性比阿霉素标准品至少低 35 倍。
T83044	Antimalarial agent 33	Parasite	Microbiology/Virology
	Antimalarial agent 33 (compound 5g) 显示针对红细胞期和肝期疟原虫的抗活性，特别是对 K1 恶性疟原虫株，其EC50为1.1 μM。Antimalarial agent 33 还展示出提升的微粒体稳定性（T1/2=29分钟），并且对原代肝细胞未表现出明显的细胞毒效应。
T9763	MMV666810
	MMV666810 是一种类似于 MMV390048 的2-氨基吡嗪，5.94 nM 的 MMV666810 对无性寄生虫有效。与早期相比，MMV666810 对晚期配子体细胞的选择性是早期的3.3倍（早期配子体:IC50603 ± 88 nM; 晚期配子体:IC50179 ± 8 nM）。
T35757	Beauvericin A
	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.Antimycob...

化合物

9-O-Demethyltrigonostemone

Cat.No: T71289

Cat.No: T25402

Synonym: AI330755,AI3 30755,AI3-30755

Bis-propargyl-PEG3

Cat.No: T14656

Target: Others

Thalifendine chloride

Cat.No: T75640

Cat.No: T116970

Antimalarial agent 28

Cat.No: T79460

Target: Parasite

Cat.No: T75536

Anticancer agent 75

Cat.No: T60998

Antimalarial agent 33

Cat.No: T83044

Target: Parasite

Cat.No: T9763

Cat.No: T35757

Cat. No.	Product Name	Target	Signaling Pathways
TN1610	Epimagnolin A	Parasite	Microbiology/Virology
	Epimagnolin A 是一种糠醛木脂素，具有中等的抗疟原虫活性，IC50值为5.7 μg/mL。
TN3466	Atherosperminine	cAMP; Calcium Channel; AChR; Parasite	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience
	Atherosperminine 是一种天然生物碱，在体外表现出抗疟原虫活性，IC50为 5.80 μM。它具有DPPH 自由基清除活性，其IC50值为 29.56 µg/mL。它对气管有非特异性的弛缓作用。它是一种良好的还原剂，具有螯合金属的能力。
TN2239	Strictosamide 异长春花苷内酰胺	ATPase; Potassium Channel; Sodium Channel; Parasite; Antifungal	Membrane transporter/Ion channel; Microbiology/Virology
	Strictosamide 具有抗炎、抗疟原虫和抗真菌活性。
T3933	Jatrorrhizine Yatrorizine,neprotin,药根碱	MAO; 5-HT Receptor; Antibacterial; AChE	GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
	Jatrorrhizine (neprotin) 是一种从黄连中分离得到的生物碱，具有抗菌、抗氧化、抗疟原虫和神经保护活性。它通过抑制 uptake-2 transporter 的活性减少血清素和去甲肾上腺素的摄取。它是一种有口服活性的乙酰胆碱酯酶制剂。
T4912	Jatrorrhizine chloride 盐酸药根碱,Yatrorhizine chloride,Neprotine chloride	Others; 5-HT Receptor; OCT; Antibacterial; AChE	GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Others
	Jatrorrhizine chloride (Neprotine chloride) 是从黄连中分离得到的生物碱，具有神经保护、抗菌、抗氧化和抗疟原虫活性。它通过抑制摄取2转运蛋白的活性减少血清素和去甲肾上腺素的摄取。它是具有口服活性的乙酰胆碱酯酶抑制剂。
T11811	Laetanine	Parasite	Microbiology/Virology
	Laetanine 是从Litsea laeta 提取到的一种去甲马飞生物碱，有抗疟原虫活性。
T3832	11-O-Galloylbergenin	Antioxidant; Immunology/Inflammation related	Immunology/Inflammation; oxidation-reduction
	11-O-Galloylbergenin 是从 Mallotus philippinensis 中分离出来的，具有抗氧化和抗疟原虫活性。
T8206	Cycleanine	Others	Others
	Cycleanine 是一种高效血管选择性Ca- 拮抗剂，具有缓解疼痛、肌肉松弛和抗炎作用。它还具有有效的抗菌、抗真菌、抗疟原虫和细胞毒活性。
T3682	(-)-Catechin gallate (-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate	Others; COX	Immunology/Inflammation; Neuroscience; Others
	(-)-Catechin gallate ((-)-Catechin 3-O-gallate) 是绿茶儿茶素中的微量组分，可抑制COX-1和COX-2活性。它抑制人 Beta-secretase，对氯喹敏感的恶性疟原虫 NF54 和耐氯喹的恶性疟原虫 K1 具有抗疟原虫活性。
TL0013	Heraclenin 独活内酯	Anti-infection; Immunology/Inflammation related	Immunology/Inflammation; Microbiology/Virology
	Heraclenin 是一种天然呋喃香豆素。它浓度依赖性的靶向激活的 T 细胞核因子 (NFAT) ，抑制人原代 T 细胞中 T 细胞受体介导的增殖。
T2S1635	3-Isomangostin	MTH1	DNA Damage/DNA Repair
	3-Isomangostin 可从莽吉柿壳中提取的一种天然产物，是一种乙酰胆碱酯酶选择性抑制剂，也是一种有效的人醛糖还原酶抑制剂，IC50 为 3.48 uM。它抑制 MutT 同源物 1 (MTH1)，IC50 为 52 nM。它具有清除自由基、抗疟原虫和抗癌的活性。
T37345	5,7-Dihydroxycoumarin	Antibacterial	Microbiology/Virology
	5,7-Dihydroxycoumarin 是分离自Macaranga triloba 花序的香豆素，具有抗菌活性。
TN3583	Canophyllal	Antifection	Microbiology/Virology
	Canophyllal shows antiplasmodial activity against the W2 strain of Plasmodium falciparum which is resistant to chloroquine and other antimalarial drugs.
TN3707	Coronarin B	Antifection	Microbiology/Virology
	Coronarin B has cytotoxic activity, it also has modest antiplasmodial activity.
TN2418	Cassiachromone	Others	Others
	Cassiachromone has antiplasmodial activity
TN5327	11(13)-Dehydroivaxillin
	11(13)-Dehydroivaxillin possesses a promising antiplasmodial activity, which can be exploited in malaria therapy.
TN2650	16-Oxocleroda-3,13E-dien-15-oic acid	Antifection	Microbiology/Virology
	16-Oxocleroda-3,13E-dien-15-oic acid shows antiplasmodial activity.
TN2380	Glycerol 1-(26-hydroxyhexacosanoate)	Others	Others
	Glycerol 1-(26-hydroxyhexacosanoate) has weak activities antiplasmodial
TN4443	Lipiferolide	Telomerase; Antifection	DNA Damage/DNA Repair; Microbiology/Virology
	Lipiferolide is an inhibitor of farnesyl protein transferase(FPTase), it inhibits the FPTase activity in a dose-dependent manner, and shows cell growth inhibitory activity against several tumor cells, it possesses cytotoxic activity against KB cells. Liriodenine also has antiplasmodial activity.
TN6009	Pseudopalmatine
	Pseudopalmatine exhibits antiplasmodial activity. It also shows anti-acetylcholinesterase (AChE) activity, with IC50 values of 1.8uM.
TN3456	Artoheterophyllin B	Antifection	Microbiology/Virology
	Artoheterophyllin B has antiplasmodial activity.
TN4218	Homaloside D	Antifection	Microbiology/Virology
	Homaloside D has antiplasmodial activity.
TN4387	Khellactone	Antifection	Microbiology/Virology
	Khellactone shows antitumor activity,it can suppress the growth of NCI-H460 tumor cells. (+)-4'-cis-Khellactone and (+)-3'-cis-khellactone have antiplasmodial activities, they show notable inhibitory activity against -sensitive strains of with IC(50) values from 1.5 and 2.4 microM.
T11681	Isochondrodendrine Isochondrodendrin	Others	Others
	Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum. Isochondrodendrine is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina.
TN2413	Diacetylpiptocarphol	Others	Others
	Diacetylpiptocarphol has antiplasmodial activity
TN1930	Methylenetanshinquinone	Antifection	Microbiology/Virology
	Methylenetanshinquinone shows antiplasmodial and antitrypanosomal activity, it is active against both Trypanosoma brucei rhodesiense and Plasmodium falciparum.
TN2867	3,4,5-Trimethoxyphenyl-(6-O-galloyl)-O-beta-D-glucopyranoside	Antifection	Microbiology/Virology
	3,4,5-Trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside shows in vitro antiplasmodial activity.
TN5657	Goniotriol
	Goniotriol shows antimycobacterial activity against Mycobacterium tuberculosis (MIC =100 microg/mL). It exhibits antiplasmodial activity against Plasmodium falciparum (IC50=2.6 microg/mL). Goniotriol shows cytotoxicity against cancer cells, KB, BC1, NCI-H
T11509	Guanfu base H Atisinium chloride	Others	Others
	Guanfu base H is a diterpenoid alkaloid isolated from Aconitum coreanum. It has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 (IC50s: 4 μM and 3.6 μM).
T75568	Z-Antiepilepsirine
	Z-Antiepilepsirine 是一种酰胺生物碱，存在于 Piper capense L.f 中。Z-Antiepilepsirine 显示抗疟原虫活性，对 PlasmodiumfalciparumW2 菌株的 IC50值为 27 µM。
TN1442	Betulinic acid methyl ester	Antifection	Microbiology/Virology
	Betulinic acid methyl ester showed antiplasmodial activity against chloroquine-resistant Plasmodium falciparum parasites in vitro.It also inhibited B16 2F2 cell proliferation by induction of apoptosis.
TN3124	5-Hydroxysophoranone	Antibacterial; Parasite; Antifection	Microbiology/Virology
	5-Hydroxysophoranone 从 Erythrina subumbrans 茎中提取，对恶性疟原虫具有高抗疟原虫活性 (IC50 = 2.5 μg/mL)。
TN1834	Kobusin 去甲槟郎碱,自旋七叶素	Others; NOS; NF-κB	Immunology/Inflammation; NF-κB; Others
	Kobusin, a Calmodulin inhibitor, shows mild antiplasmodial,anti-inflammatory, and cytotoxic activities; it may be beneficial for the treatment of neuro-inflammatory diseases through the inhibition of iNOS expression and peroxynitrite scavenging potential. Kobusin can mildly reduce gastrointestinal motility in mice, it activates CFTR and CaCCgie chloride channel activities in mouse colonic epithelia and shows inhibitory effects toward ANO1/CaCC-mediated short-circuit currents in ANO1/CaCC-express...
TN5061	Stephanine	Adrenergic Receptor; Antifection	GPCR/G Protein; Microbiology/Virology; Neuroscience
	l-Stephanine is a potent and highly selective alpha 1 adrenoceptor blocker, inhibits anococcygeus muscle contraction induced by phenylephrine with pA2 values of 6.76. Stephanine shows significant antiplasmodial activities with IC(50) ranged from 1.2 uM to 52.3 uM. Stephanine and crebanine have high inhibitory activity against gram-positive animal pathogenic bacteria, with MIC values of 0.078-0.312g/l, but low inhibitory activity against gram-negative animal pathogenic bacteria, they also inhibit...
TN5201	Uncarinic acid E	BCL; MEK; Caspase; PI3K; Antifection; p53	Apoptosis; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Uncarinic acid E has anti-cancer activity, it induces apoptosis in HepG2 cells via accumulation of p53, alters the Bax/Bcl-2 ratio, and activates caspases, resulting in cytochrome c release from the mitochondria. A mixture of uncarinic acid E and 27-O-p-(
T75436	Jatrorrhizine hydroxide
	Jatrorrhizine hydroxide, 一种从黄连中提取的生物碱，展现了神经保护、抗菌、抗疟原虫及抗氧化的活性。作为一种高效的乙酰胆碱酯酶(AChE)抑制剂(IC50=872 nM)，其对BuChE的选择性高达115倍。此外，Jatrorrhizine hydroxide还能通过抑制uptake-2 transporter活性来减少血清素(5-HT)和去甲肾上腺素(NE)的摄取，表现出口服活性。
TN2190	Scoulerine	Apoptosis; Beta-Secretase; BACE; Parasite	Apoptosis; Microbiology/Virology; Neuroscience
	Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖，阻止细胞周期，并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。

天然产物

Cat.No: TN1610

Target: Parasite

Atherosperminine

Cat.No: TN3466

Target: cAMP, Calcium Channel, AChR, Parasite

Cat.No: TN2239

Synonym: 异长春花苷内酰胺

Target: ATPase, Potassium Channel, Sodium Channel, Parasite, Antifungal

Cat.No: T3933

Synonym: Yatrorizine,neprotin,药根碱

Target: MAO, 5-HT Receptor, Antibacterial, AChE

Jatrorrhizine chloride

Cat.No: T4912

Synonym: 盐酸药根碱,Yatrorhizine chloride,Neprotine chloride

Target: Others, 5-HT Receptor, OCT, Antibacterial, AChE

Cat.No: T11811

Target: Parasite

11-O-Galloylbergenin

Cat.No: T3832

Target: Antioxidant, Immunology/Inflammation related

Cat.No: T8206

Target: Others

(-)-Catechin gallate

Cat.No: T3682

Synonym: (-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate

Target: Others, COX

Cat.No: TL0013

Synonym: 独活内酯

Target: Anti-infection, Immunology/Inflammation related

Cat.No: T2S1635

Target: MTH1

5,7-Dihydroxycoumarin

Cat.No: T37345

Target: Antibacterial

Cat.No: TN3583

Target: Antifection

Cat.No: TN3707

Target: Antifection

Cat.No: TN2418

Target: Others

11(13)-Dehydroivaxillin

Cat.No: TN5327

16-Oxocleroda-3,13E-dien-15-oic acid

Cat.No: TN2650

Target: Antifection

Glycerol 1-(26-hydroxyhexacosanoate)

Cat.No: TN2380

Target: Others

Cat.No: TN4443

Target: Telomerase, Antifection

Pseudopalmatine

Cat.No: TN6009

Artoheterophyllin B

Cat.No: TN3456

Target: Antifection

Cat.No: TN4218

Target: Antifection

Cat.No: TN4387

Target: Antifection

Isochondrodendrine

Cat.No: T11681

Synonym: Isochondrodendrin

Target: Others

Diacetylpiptocarphol

Cat.No: TN2413

Target: Others

Methylenetanshinquinone

Cat.No: TN1930

Target: Antifection

3,4,5-Trimethoxyphenyl-(6-O-galloyl)-O-beta-D-glucopyranoside

Cat.No: TN2867

Target: Antifection

Cat.No: TN5657

Cat.No: T11509

Synonym: Atisinium chloride

Target: Others

Z-Antiepilepsirine

Cat.No: T75568

Betulinic acid methyl ester

Cat.No: TN1442

Target: Antifection

5-Hydroxysophoranone

Cat.No: TN3124

Target: Antibacterial, Parasite, Antifection

Cat.No: TN1834

Synonym: 去甲槟郎碱,自旋七叶素

Target: Others, NOS, NF-κB

Cat.No: TN5061

Target: Adrenergic Receptor, Antifection

Uncarinic acid E

Cat.No: TN5201

Target: BCL, MEK, Caspase, PI3K, Antifection, p53

Jatrorrhizine hydroxide

Cat.No: T75436

Cat.No: TN2190

Target: Apoptosis, Beta-Secretase, BACE, Parasite

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