Table 1.
In vitro Anticancer Effects of SV or Peptides on Human Cancer Cells
| Species | Venom/Peptide | Action | Target | Ref. |
| Androctonus crassicauda | Whole venom | Inhibits proliferation of human neuroblastoma (SH-SY5Y) and human breast (MCF-7) cancer cell lines | Induces apoptosis through increasing nitric oxide production, caspase-3 activity and depolarizing mitochondrial membrane and arrests S phase | 35 |
| Androctonus crassicauda | Non-disulphide-bridged peptides (NDBP), AcrAP1 and AcrAP2, and their high cationic analogues (HC-AcrAP) (0.001-100 µM) | HC-AcrAP analogues inhibit the proliferation of human lung adenocarcinoma (H460), breast carcinoma (MB435s) breast tumorigenic (MCF-7) and prostate carcinoma (PC-3) cell lines (IC50 2-3.6 µM) | Probably inducing cell lysis | 68 |
| Androctonus bicolor Androctonus crassicauda | Whole venom (500-1000 µg/ml) |
Inhibits proliferation of human breast (MDA-MB-231), and colorectal (HCT-8) cancer cells | Induces apoptosis more than necrotic death, and arrests cells at G0/G1 phase, upregulate p53, downregulate Bcl-xL | 29-31 |
| Androctonus crassicauda, Androctonus bicolor | Whole venom (20-100 µg/ml) |
Inhibits cell motility, and prevents colony mitosis of human breast, (MDA-MB-231), and colorectal (HCT-8 and HCT116) cancer cells | Two mechanisms proposed are i) a decrease in the expression of MMPs, and ii) a reduction in the phosphorylation levels of FAK, which is involved in cell migration and invasion. | 31 |
| Androctonus mauritanicus | Gonearrestide peptide (18 aa, 2192 Da) 2-200 µM |
Inhibits the proliferation of human colon cancer cell line HCT116 in dose-dependent | Arrests cancer cell cycle in G1 phase via modulating cell cycle checkpoint proteins (down-regulate CDK4, and upregulate cyclin D3, p21, p27) | 36 |
| Buthus martensii Karsch | BmK 70-80kDa SVCIII (1-50 µg/ml) |
Inhibits proliferation of human acute monocytic leukemia cell line (THP-1) and the human T lymphoma (Jurkat cell line) and induces cell cycle arrest at G1 phase | Inhibits NF-κB activation through inhibition of IκBα phosphorylation, degradation and p65 nuclear translocation | 44 |
| BmK 50-60 aa 65 kDa (10-200 µg/ml) | Inhibits proliferation of DU145 human prostate cancer cell line | Enhances expression of apoptotic gene, Bax, reduces anti-apoptotic, Bcl-2, expression, and arrests cancer cells at G1/S | 28 | |
| BmK AGAP 71.42KDa with 66 aa (5-60 µM) (IC50 = 40µM for MCF-7 and 50µM for MDA-MB-231 cells) | Inhibits proliferation, stemness, sphere formation, colony formation epithelial-mesenchymal transition, migration and invasion of human breast MCF-7 and MDA-MB-231 cells | Reduces gene and protein expression of Oct4, SOX2, Nanog, N-cadherin, Snail and PTX3, and increased the expression of E-cadherin | 47 | |
| Buthus tumulus | Iberiotoxin (IbTX) (34 aa, 36.07 kDa) | Inhibits growth and proliferation of human cervical cancer (HeLa) and human ovarian cancer (A2780) cell lines | Blocks calcium-activated potassium channels KCNMA1 (KCa1.1, BK) *Found to be expressed in cervical cancer-hormone dependent | 42-43 |
| Centruroides margartatus | Margatoxin (MgTX, 39 aa, 41.92 kDa) | Inhibits proliferation of human lung adenocarcinoma cells and decreases tumor volume in vivo following intra-tumoral injection | Blocks Kv1.3, and increases expression level of p21Waf1/Cip1 and decreases the expression level of Cdk4 and cyclin D3. | 61 |
| Heterometrus bengalensis | Bengalin 72kDa IC50 3.7 and 4.1 µg/ml |
Inhibits proliferation of human leukemic cells (U937) and K562 chronic myelogenous leukemia (K562) and has no effect on normal human lymphocytes | Increases expression of Bax/Bcl-2 ratio, caspase 3 and 9, reduces mitochondrial membrane potential, heat shock proteins 70 and 90 | 32 |
| Leiurus quinquestriatus | Chlorotoxin (ClTx) (36 aa, MW 4.02 KDa) | Inhibits migration and invasion of human glioma (D54-MG and CCF-STTG-1) cells | Binds to matrix metalloproteinase-2 (MMP-2) and modulates the surface expression of an active MMP-2 and increase the uptake of Cl-channel receptors (CIC-3) | 7, 53 |
| Leiurus quinquestriatus | Whole venom (20-100 µg/ml) | Inhibits cell motility, and prevents colony mitosis of human breast, (MDA-MB-231) and colorectal (HCT-8 and HCT116) cancer cells | Two mechanisms proposed are i) a decrease in the expression of MMPs, and ii) a reduction in the phosphorylation levels of FAK, which is involved in cell migration and invasion | 31 |
| Odontobuthus doriae | Whole venom (20-100 µg/ml) | Inhibits proliferation and inhibits DNA synthesis in human breast cancer cell line, MCF-7 | Depolarizes mitochondria, activates Caspase-3, and depletes antioxidant activities | 26 |
| Inhibits proliferation and inhibits DNA synthesis in human neuroblastoma cells, SH-SY5Y | 27 | |||
| Rhopalurus junceus | Whole venom (100-1000 µg/ml) | Inhibits proliferation on a panel of human cancer cell lines (HeLa, SiHa, Hep-2, NCI-H292, A549, MDA-MB-231, MDA-MB-468, HT-29), but has no effect on hematologic malignant cell lines (U937, K562, Raji) or normal cells (MRC-5, MDCK, Vero) | Increased expression of P53, Bax, Caspase 3, 8, & 9 and reduced Bcl-2 in HeLa (apoptosis > necrosis) whereas reduced expression p53, did not affect Bax but reduced Bcl-2 in A549 (necrosis>apoptosis) reflecting concentration used >IC50 or <IC50. | 25 |
| Tityus discrepans | Neopladine peptides 1 (29.918kDa) and 2 (30.388 kDa) | Both peptides induce apoptosis in human breast carcinoma SKBR3 cells | Bind to SKBR3 cell surface and induce FasL and BcL-2 expression | 33 |
| Tityus serrulatus | TsAp-1 and TsAp-2 (17 aa) High Cationic TsAP-1 and TsAP-2 | High cationic analogue of TsAP-1 and 2 induce high anti-proliferative activity against several human cell lines: squamous carcinoma (H157), lung adenocarcinoma (H838), prostate adenocarcinoma (PC-3); breast carcinoma (MCF-7), glioblastoma (U251-MG) | 67 |