| Summary: | Approximately 400 Garcinia species are distributed around the world. Previous studies have reported the extracts from bark, seed, fruits, peels, leaves, and stems of <i>Garcinia mangostana, G. xanthochymus</i>, and <i>G. cambogia</i> that were used to treat adipogenesis, inflammation, obesity, cancer, cardiovascular diseases, and diabetes. Moreover, the hypoglycemic effects and underlined actions of different species such as <i>G. kola</i>, <i>G. pedunculata</i>, and <i>G. prainiana</i> have been elucidated. However, the anti-hyperglycemia of <i>G. linii</i> remains to be verified in this aspect. In this article, the published literature was collected and reviewed based on the medicinal characteristics of the species Garcinia, particularly in diabetic care to deliberate the known constituents from Garcinia and further focus on and isolate new compounds of <i>G. linii</i> (Taiwan distinctive species) on various hypoglycemic targets including α-amylase, α-glucosidase, 5′-adenosine monophosphate-activated protein kinase (AMPK), insulin receptor kinase, peroxisome proliferator-activated receptor gamma (PPARγ), and dipeptidyl peptidase-4 (DPP-4) via the molecular docking approach with Gold program to explore the potential candidates for anti-diabetic treatments. Accordingly, benzopyrans and triterpenes are postulated to be the active components in <i>G. linii</i> for mediating blood glucose. To further validate the potency of those active components, <i>in vitro</i> enzymatic and cellular function assays with <i>in vivo</i> animal efficacy experiments need to be performed in the near future.
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