The Safety and Tolerability of Lumbrokinase DLBS1033 in Healthy Adult Subjects

Tjandrawinata, Raymond R.; Yunaidi, Danang Agung; Susanto, Liana W

doi:10.1055/s-0035-1569406

Cited by 14 publications

(12 citation statements)

References 12 publications

(18 reference statements)

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“…Many of the nature-derived compounds have been directly utilized as drug entities; while many others can also serve as chemical models for the design, synthesis or semi-synthesis of novel drug molecules. A tremendous number of natural compounds are currently in various stages of clinical development, highlighting the significance and persisting viability of the nature-derived products as sources of new drug candidates [1][2][3][4][5][6][7][8]. This paper reviews Phyllanthus niruri L. (P. niruri), one herb species among the gigantic number of medicinal plants that have widely been studied worldwide.…”

Section: Introductionmentioning

confidence: 99%

The use of Phyllanthus niruri L. as an immunomodulator for the treatment of infectious diseases in clinical settings

Tjandrawinata¹,

Susanto²,

Nofiarny³

2017

APJTD

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Section: Introductionmentioning

confidence: 99%

The use of Phyllanthus niruri L. as an immunomodulator for the treatment of infectious diseases in clinical settings

Tjandrawinata¹,

Susanto²,

Nofiarny³

2017

APJTD

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“…22 However, the half-life of LK is very short, and a high dose of LK can increase the severity of its side effects while improving the curative effect. 23,24 The current delivery systems for LK mainly only include the maleic anhydride methylvinyl ether copolymer, which can immobilize LK to polyurethane (immobilized LK retained about 34% of its activity) for antithrombogenicity in the artificial organ field. 25 Therefore, a DDS that can strengthen the drug delivery efficacy and decrease the dose of drugs while not decreasing the anti-cancer efficacy may overcome the shortcomings of these drugs.…”

Section: Introductionmentioning

confidence: 99%

Lumbrokinase/paclitaxel nanoparticle complex: potential therapeutic applications in bladder cancer

Yan

Tong

et al. 2018

IJN

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BackgroundLumbrokinase (LK) is an enzyme complex with antithrombotic, antioxidant, antitumor, and immunomodulatory effects. It has been extensively studied and used in clinical anti-tumor therapy. However, its half-life is short, its bioavailability is low, and its toxicity and side effects are great, which greatly limit its clinical application. Therefore, LK is often combined with other drugs (such as immune agents, hormones, or Chinese herbal medicine) to reduce its dosage and side effects and to improve its anti-tumor effects.Methods and resultsHere, we described an LK/paclitaxel (PTX) nanocarrier based on poly(ethylene glycol)-b-(poly(ethylenediamine l-glutamate)-g-poly(ε-benzyoxycarbonyl-l-lysine)-r-poly(l-lysine)) (PEG-b-(PELG-g-(PZLL-r-PLL))). In the present study, LK and PTX were loaded by electrostatic and/or hydrophobic effects under mild conditions, thereby increasing the half-life and bioavailability of the drugs via the sustained release and enhancement of tumor site enrichment by the LK/PTX/PEG-b-(PELG-g-(PZLL-r-PLL)) complex through passive targeting. In this study, using bladder cancer cells (J82 cells) and rat bladder cancer model as the object, the structure of the nanocarrier, the relationship between drugs composition and antitumor properties were systematically studied.ConclusionWe propose that the block copolymer PEG-b-(PELG-g-(PZLL-r-PLL)) may function as a potent nanocarrier for augmenting anti-bladder cancer pharmacotherapy, with unprecedented clinical benefits.

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“…The chances of non-specific fibrinolysis are eliminated because lumbrokinase precisely targets fibrin clots. These earthworm fibrinolytic enzymes (EFEs) lessen platelet coagulation and prevent thrombosis without blood loss [8]. The mode of action involves direct dissolution of fibrin or it can induce endogenous tissue plasminogen activator (t-PA) which converts plasminogen to plasmin [9, 10].…”

Section: Introductionmentioning

confidence: 99%

Isolation, purification and functional characterization of fibrinolytic Protease from an Earthworm Eisenia foetida

Joyia¹

2018

PAB

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Isolation, purification and functional characterization of fibrinolytic Protease from an Earthworm Eisenia foetida.Abstract Thrombosis (development of clots in blood vessels) may cause vascular blockade culminating into serious consequences broadly known as cardiovascular diseases (CVDs). CVDs are causing more than 31% of total deaths globally. 'Thrombolysis' is the term used for dissolution of such blood clots. Numerous protein molecules called thrombolytics mediate the process of thrombolysis. Such thrombolytics are not only expensive but also cause non-specific fibrinolysis as the main side-effect, instigating excessive internal bleeding (haemorrhage) and substantial blood loss ultimately leading to death. On the other hand, lumbrokinase (LK), an earthworm-derived fibrinolytic agent being very specific, dissolves fibrin itself or convert plasminogen to plasmin by inducing endogenous tissue plasminogen activator (t-PA) to degrade fibrin clots without any ill-effects. In present study we describe the isolation of a fibrinolytic protease namely Lumbrokinase from indigenous earthworm Eisenia foetida. Protein precipitation was carried out by using various concentrations of (NH4)2SO4, desalted and concentrated by dialysis and purified by gel filtration chromatography. Furthermore, its kinetic characterization and in vitro estimation of caseinolytic activity was carried out. Characterization of earthworm-derived fibrinolytic enzyme reveals that it can serve as an ideal therapeutic molecule for oral delivery in CVD patients.

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The Safety and Tolerability of Lumbrokinase DLBS1033 in Healthy Adult Subjects

Abstract: DLBS1033 given at the dose of 490 mg 3 times daily was safe and tolerable in healthy adults.

Cited by 14 publications

References 12 publications

The use of Phyllanthus niruri L. as an immunomodulator for the treatment of infectious diseases in clinical settings

The use of Phyllanthus niruri L. as an immunomodulator for the treatment of infectious diseases in clinical settings

Lumbrokinase/paclitaxel nanoparticle complex: potential therapeutic applications in bladder cancer

Isolation, purification and functional characterization of fibrinolytic Protease from an Earthworm Eisenia foetida

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