Review Article

Biomolecules of the Horseshoe Crab’s Hemolymph: Components of an Ancient Defensive Mechanism and Its Impact on the Pharmaceutical and Biomedical Industry

Table 5

Potential drug, antibiotics, and therapeutic effect of hemolymph’s molecules of horseshoe crab.

BiomoleculesPotential effect

Tachystatin(i) Tachystatins A, B, and C are hemocyte-derived antimicrobial peptides in Tachypleus tridentatus. Tachystatin B contains B1 and B2 isopeptides. Tachystatins B1 and B2 are more potent than tachystatins A and C at countering fungi and Gram-positive bacteria [65, 66].
(ii) Stabilized tachystatin B can be a potent antifungal peptide with medicinal applications [66].
Tachyplesin I (TPI)(i) Tachyplesin I (TPI) is a cationic β-hairpin antimicrobial peptide having broad antibacterial efficacy against Gram-positive and Gram-negative bacteria with very low MICs (0.8 to 12.5 g/ml) [17].
(ii) Compared to TPI, the all-d-amino acid derivative (TPAD) demonstrates significantly increased stability against enzymatic degradation and decreased hemolytic activity, indicating greater therapeutic potential. The combination of TPAD and LED209, a QseC/B inhibitor, greatly enhanced the bactericidal effect against three multi-drug-resistant bacterial strains [89].
(iii) Tac has been shown to stop the growth of some tumor cells, such as prostate cancer (TSU), melanoma (B16), hepatocarcinoma (SMMC-7721), human promyelocytic leukemia (HL-60), human gastric adenocarcinoma (BGC-823), and lung cancer (SPCA-1) cells [90]–[91]. Cyclic analogues of tachyplesin I are anticancer and cell penetrating [92].
(iv) Biomaterials surface coated with tachyplesin I and antimicrobial agents. In a bacterial-contaminated mouse skin wound model, wound healing potential was demonstrated [93].
(v) Tachyplesin worked as a nonviral macromolecule nanocarrier in both biological systems, transporting cargo molecules [94].
(vi) Tachyplesin I made Gram-negative bacteria more sensitive to the killing effects of subinhibitory concentrations of novobiocin and nalidixic acid, but tachyplesin I was still able to kill polymyxin B-resistant strains with changed lipopolysaccharides. In 40 minutes, tachyplesin I stopped the growth of bacteria forever. A Salmonella typhimurium phoP strain that was sensitive to defensin was also sensitive to tachyplesin I. The inverted inner membrane vesicles of Escherichia coli were quickly depolarized by tachyplesin I. These results show that tachyplesin-mediated killing of Gram-negative bacteria is linked to the cytoplasmic membrane’s depolarization and the outer membrane’s permeabilization [95].
Tachycitin(i) A chitin-binding antimicrobial protein known as tachycitin demonstrated notable effectiveness against fungus [96].
Big defensin(i) A wide range of uses are demonstrated by the purified big defensin’s antibacterial effectiveness against Gram-negative and Gram-positive bacteria and its antifungal activity. As a result, it may complement the anti-LPS factor in protecting from invasive bacteria [97].
Lectin(i) A Tachypleus tridentatus hemolymph-derived isolated lectin performed significantly against human colon cancer [98].