The pressing need to discover more effective drugs for various CNS disorders has resurrected the idea of investigating the effectiveness of traditional medicines in modern science. Tongluojiunao (TLJN) is an example of revived modern herbal preparation based on traditional Chinese medicine (TCM) with a long history of administration for various types of cerebrovascular injuries and neurodegenerative diseases. TLJN is prepared from the herbal roots of Panax notoginseng (Sanchi) and dried fruits of Gardenia jasminoides (Cape Jasmine), and so far, it has demonstrated promising results in patients with vascular dementia and cerebral ischemic stroke. TLJN has also demonstrated therapeutic ability regarding the slowly-progressed neurodegenerative diseases like Alzheimer’s disease. So it tempted us to undertake a thorough review of various features of TLJN therapeutic effects on the mentioned CNS conditions, including the cellular and molecular targets, inflammatory responses, neurogenesis and angiogenesis mediators and cognitive function. For this purpose, multiple global and local databases, including China National Knowledge Infrastructure (CNKI) were checked out and the retrieved information was grouped according to their scope of studies. Among these, TLJN is reported to restore the deregulated cell-cell communication in the neurovascular unit, prevent the stress-related challenges imposed by ischemia/reperfusion insult, help with the cerebral tissue recovery after traumatic brain damage, avoid the epileptic seizure attack and limit the progression of Alzheimer’s disease. We hope that the current review provides new insights into TLJN medication as a prospective neuroprotective medication for further more in-depth investigation in the future.