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Avocado soybean unsaponifiable (ASU) to treat osteoarthritis: a clarification

Date : 2018-6-11 3:01:25 Views :

Today, a cure for osteoarthritis (OA) remains elusive and the management of OA is largely palliative focussing on the alleviation of symptoms. Current recommendations for the management of OA include a combination of non-pharmacological interventions and pharmacological treat-ments1e3. Until now, the pharmacological management of OA is dominated by non-steroidal anti-inflammatory drugs and analgesic (mainly paracetamol). Beside these conven-tional drugs, some new compounds classified as Symptom-atic Slow Acting Disease Modifying drugs (SYSADOAs) have shown symptomatic efficacy in human hip and knee OA. The term SYSADOA covers a range of agents, includ-ing glucosamine sulphate, chondroitin sulphate, diacerhein, hyaluronic acid and avocado/soybean (A/S) unsaponifi-ables (ASUs), components of PIASCLEDINE300 (Labora-tories Expansciences, Courbevoie, France). The original ASUs are recommended for the treatment of OA symptoms by the American College of Rheumatology (ACR) and by European League Against Rheumatism (EULAR). These recommendations have been elaborated on the basis of clinical, animal and in vitro studies performed with PIASCLEDINE300 (Laboratories Expansciences, Courbe-voie, France). PIASCLEDINE􀀀300 has been used in France as a prescription treatment for OA, subsidized by the government and meticulously tracked for safety for over 15 years. PIASCLEDINE300 pill is composed by 100 mg of avocado unsaponifiables and 200 mg of soybean unsaponifiables. The originality is based on the A/S ratio and avocado specific modified unsaponifiables obtained by a patented process. In other countries, ASUs are deliv-ered as over-the-counter products.

At this time, there are three well-conducted, randomized, placebo-controlled, trials demonstrating a beneficial symp-tomatic effect of PIASCLEDINE300 in the treatment of hip and/or knee OA4e6. Until now, only the ASUs found in PIASCLEDINE300 have demonstrated their clinical effi-ciency. Further, we have demonstrated that in vitro, PIA-SCLEDINE􀀀300 displayed anabolic, anti-catabolic and anti-inflammatory effects on human chondrocytes. It increased the basal synthesis of aggrecan and reversed the interleukin (IL)-1b-induced reduction of aggrecan syn-thesis by human chondrocytes in alginate beads7.It decreased the spontaneous and IL-1b-induced production of stromelysin-1 [matrix metalloproteinase (MMP-3)], IL-6 and -8, and prostaglandin E2 (PGE2) while it weakly re-versed the IL-1-induced decrease of tissue inhibitor of met-alloprotease’s (TIMP)-1 production7,8. It also decreased the spontaneous production of the macrophage inflammatory protein (MIP)-1b but stimulated the production of transform-ing growth factor (TGF)-b17. Finally, this drug fully pre-vented the inhibitory effect of OA osteoblasts on cartilage matrix protein production by human chondrocytes9. All of this clearly demonstrates the therapeutic and biological ef-fects of the ASU from PIASCLEDINE300.

Recently, Au et al.10 have demonstrated that an ASU ex-tract, named ASU-NMX 1000 suppressed tumour necrosis factor (TNF)-a, IL-1b, cyclooxygenase (COX)-2 and inducible nitric oxide (iNOS) gene expression, and PGE2 and nitric oxide production in articular chondrocytes and monocyte/macrophages. They conclude that these observations pro-vide a scientific rationale for the pain-reducing and anti-inflammatory effects of ASU observed in OA patients. In other terms, the authors attempt to explain the therapeutic effect of PIASCLEDINE 300 by in vitro effects obtained with another ASU extract which shows a different chromato-graphic spectrum. Lippielo et al. (Nutramax Laboratories) have recently demonstrated that, compared to ASU-NMX 1000􀀁, PIASCLEDINE􀀀300 contains three major addi-tional peaks11. These peaks result of the particular extr-action process used to prepare PIASCLEDINE 300. In comparison with PIASCLEDINE􀀀300, other ASU formula-tions showed almost the complete absence of specific mol-ecules which are patented. Therefore, while the ability of ASU-NMX 1000 and PIASCLEDINE 300 to reduce PGE2 production or MMP activity or to stimulate glycosami-noglycans seems to be comparable11, different effects of these two formulations on other aspects of the chondrocyte metabolism can not be excluded. Therefore, to extrapolate the data obtained with one ASU formulation to another one remains fully speculative. Further, clinical studies are required before concluding on the safety and the clinical ef-ficacy of ASU-NMX 1000. To use the in vitro and clinical data obtained with PIASCLEDINE􀀀300 to support a poten-tial effect of ASU-NMX 1000 must be done with a great caution.

Product Name

 Avocado soybean unsaponiable

Botanical Source


Part Used





Light yellow

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