Despite　tremendous　advances　in　the　targeted　therapy　for　various　types　of　hematological　malignancies　with　successful　improvements　in　the　survival　rates,　emerging　resistance　issues　are　startlingly　high　and　novel　therapeutic　strategies　are　urgently　needed.　In　addition,　chemoprevention　is　currently　becoming　an　elusive　goal.　Plant-derived　natural　products　have　garnered　considerable　attention　in　recent　years　due　to　the　potential　dual　functions　as　chemotherapeutics　and　dietary　chemoprevention.　One　of　the　particularly　ubiquitous　families　is　the　polyphenolic　flavonoids.　Among　them,　baicalin　and　its　aglycone　baicalein　have　been　widely　investigated　in　hematological　malignancies　because　both　of　them　exhibit　remarkable　pharmacological　properties.　This　review　focuses　on　the　recent　achievements　in　drug　discovery　research　associated　with　baicalin　and　baicalein　for　hematological　malignancy　therapies.　The　promising　anticancer　activities　of　these　two　flavonoids　targeting　diverse　signaling　pathways　and　their　potential　biological　mechanisms　in　different　types　of　hematological　malignancies,　as　well　as　the　combination　strategy　with　baicalin　or　baicalein　as　chemotherapeutic　adjuvants　for　recent　therapies　in　these　intractable　diseases　are　discussed.　Meanwhile,　the　biotransformation　of　baicalin　and　baicalein　and　the　relevant　approaches　to　improve　their　bioavailability　are　also　summarized.　©　2014　Elsevier　Ireland　Ltd.